reactant_set_id
int64
7.11k
51.6M
pmid
int64
42.8k
39.4M
protein
stringlengths
4
182
ligand
dict
affinity_data
dict
DESCRIPTION
stringlengths
29
1.83k
search_path
listlengths
0
7
supplementary_source
listlengths
0
2
references_previous
stringlengths
4
3.72k
original_paragraph
stringlengths
2
88.8k
structured_description
stringlengths
529
2.87k
assay_type
stringclasses
4 values
source_filename
stringlengths
10
13
source_record_key
stringlengths
4
8
50,470,071
26,367,539
Bromodomain-containing protein 4
{ "smiles": "COc1cc(OC)c2c(c1)nc([nH]c2=O)-c1cc(C)c(OCCO)c(C)c1" }
{ "type": "Kd", "value": 303, "relation": "=", "unit": "nM" }
Binding affinity to human BRD4 bromodomain 2 by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26367539.json
50470071
50,470,075
26,367,539
Bromodomain-containing protein 4
{ "smiles": "COc1cc(OC)c2c(c1)nc([nH]c2=O)-c1cc(C)c(OCCO)c(C)c1" }
{ "type": "Kd", "value": 140, "relation": "=", "unit": "nM" }
Binding affinity to human BRD4 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26367539.json
50470075
50,470,082
26,367,539
Bromodomain-containing protein 2
{ "smiles": "CC(=O)NCCCCn1c2CCNC(=O)c2c2ccccc12" }
{ "type": "Kd", "value": 8600, "relation": "=", "unit": "nM" }
Binding affinity to recombinant poly-His-tagged BRD2 bromodomain 1 (unknown origin) by isothermal titration calorimetry
[ "main", "supplementary" ]
[ "main" ]
Reference 27 not found in bibliography
{"Data Analysis": "Data Analysis: All the data was fitted to a single binding site model using the Microcal LLC ITC200 Origin software provided by the manufacturer to yield enthalpies of binding (ΔH) and binding constants (Ka). Further thermodynamical parameters were calculated from these values (changes in entropy ΔS,...
{"assay_conditions": {"buffer_composition": "20 mM HEPES, 100 mM NaCl", "control_method": null, "injection_parameters": {"duration": "4", "first_volume": "0.4", "spacing": "120", "subsequent_volume": "2", "total_count": "20"}, "pH": 7.5, "reference_cell_content": null, "stirring_speed": "1000", "temperature_c": "15"}, ...
itc
26367539.json
50470082
50,470,081
26,367,539
Bromodomain-containing protein 2
{ "smiles": "CC(=O)NCCCCn1c2CCNC(=O)c2c2ccccc12" }
{ "type": "Kd", "value": 300000, "relation": ">", "unit": "nM" }
Binding affinity to recombinant poly-His-tagged BRD2 bromodomain 2 (unknown origin) by isothermal titration calorimetry
[ "main", "supplementary" ]
[ "main" ]
none
{"Data Analysis": "Data Analysis: All the data was fitted to a single binding site model using the Microcal LLC ITC200 Origin software provided by the manufacturer to yield enthalpies of binding (ΔH) and binding constants (Ka). Further thermodynamical parameters were calculated from these values (changes in entropy ΔS,...
{"assay_conditions": {"buffer_composition": "20 mM HEPES, 100 mM NaCl", "control_method": null, "injection_parameters": {"duration": "4", "first_volume": "0.4", "spacing": "120", "subsequent_volume": "2", "total_count": "20"}, "pH": 7.5, "reference_cell_content": null, "stirring_speed": "1000", "temperature_c": "15"}, ...
itc
26367539.json
50470081
50,470,080
26,367,539
Bromodomain-containing protein 4
{ "smiles": "CC(=O)NCCCCn1c2CCNC(=O)c2c2ccccc12" }
{ "type": "Kd", "value": 3400, "relation": "=", "unit": "nM" }
Binding affinity to recombinant poly-His-tagged BRD4 bromodomain 1 (unknown origin) by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26367539.json
50470080
50,470,079
26,367,539
Bromodomain-containing protein 4
{ "smiles": "CC(=O)NCCCCn1c2CCNC(=O)c2c2ccccc12" }
{ "type": "Kd", "value": 300000, "relation": ">", "unit": "nM" }
Binding affinity to recombinant poly-His-tagged BRD4 bromodomain 2 (unknown origin) by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26367539.json
50470079
324,058
26,598,975
Protein arginine N-methyltransferase 6
{ "smiles": "CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN" }
{ "type": "Kd", "value": 6, "relation": "=", "unit": "nM" }
Isothermal titration calorimetry (ITC) was performed at 25 °C in a Nano ITC instrument (TA Instruments, USA). The cell was loaded with 25 μM PRMT6, 100 μM SAMand 2.5% DMSO in 50 mM Tris-HCl (pH 8.5) containing 150 mM NaCl. The syringe wasloaded with 200 μM MS023, 100 μM SAM and 2.5% DMSO prepared in...
[ "main" ]
[]
none
{"Figure 2 Caption (Page E)": "(B) Isothermal titration calorimetry (ITC) was used to assess binding of PRMT6 to MS023 (Kd = 6 nM). (C) Differential scanning fluorimetry (DSF) was used to confirm the binding of PRMT6 to MS023. Experiments were performed for PRMT6 (●) in the absence of any compound as a control (Tm = 52...
{"assay_conditions": {"buffer_composition": "50 mM Tris-HCl, 150 mM NaCl, 2.5% DMSO", "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": "180", "subsequent_volume": "2", "total_count": "25"}, "pH": 8.5, "reference_cell_content": null, "stirring_speed": null, "temperature...
itc
26598975.json
324058
51,218,805
26,685,880
Structural capsid protein
{ "smiles": "CC[C@H](C)[C@H](N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N1CCC[C@H]1C(N)=O" }
{ "type": "Kd", "value": 3000, "relation": "=", "unit": "nM" }
Binding affinity to HIV1 NL4-3 capsid C-terminal domain (146 to 231 residues) by isothermal titration calorimetry
[ "main" ]
[]
(22) Bartonova, V.; Igonet, S.; Sticht, J.; Glass, B.; Habermann, A.; Vaney, M. C.; Sehr, P.; Lewis, J.; Rey, F. A.; Krausslich, H. G. Residues in the HIV-1 capsid assembly inhibitor binding site are essential for maintaining the assembly-competent quaternary structure of the capsid protein. J. Biol. Chem. 2008, 283 (4...
{"Figure 6 Caption": "Figure 6. Isothermal titrations of CAI (A,B) and compound 33 (C,D) to HIV-1 CA or CA CTD. Experimental details are described in Experimental Section.", "Materials and Methods - Isothermal Titration Calorimetry": "Isothermal Titration Calorimetry. The binding characteristics of CAI peptide were det...
{"assay_conditions": {"buffer_composition": "30 mM MES, 10% glycerol, 2 mM 2-mercaptoethanol, 2% DMSO", "control_method": "Titration of ligand into buffer alone", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "2", "total_count": null}, "pH": 6.0, "reference_cell_...
itc
26685880.json
51218805
51,218,807
26,685,880
Structural capsid protein
{ "smiles": "CN(C(=O)[C@H](Cc1ccccc1)NC(=O)Cc1c(C)[nH]c2ccccc12)c1ccccc1" }
{ "type": "Kd", "value": 2200, "relation": "=", "unit": "nM" }
Binding affinity to HIV1 NL4-3 capsid N-terminal domain by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 6 Caption": "Figure 6. Isothermal titrations of CAI (A,B) and compound 33 (C,D) to HIV-1 CA or CA CTD. Experimental details are described in Experimental Section.", "Figure 6 Data (Panel A)": "KD = 4.0 ± 0.5 uM; ΔH = -12.5 ± 0.2 kcal·mol⁻¹; -TΔS = 5.1 ± 0.3 kcal·mol⁻¹", "Figure 6 Data (Panel B)": "KD = 3.0 ± 0...
{"assay_conditions": {"buffer_composition": "30 mM MES, 10% glycerol, 2 mM 2-mercaptoethanol, 2% DMSO", "control_method": "Titration of ligand into buffer alone", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "2", "total_count": null}, "pH": 6.0, "reference_cell_...
itc
26685880.json
51218807
51,218,821
26,685,880
Structural capsid protein
{ "smiles": "CCOC(=O)c1ccc(Nc2nc(nc3ccccc23)-c2ccncc2)cc1" }
{ "type": "Kd", "value": 38, "relation": "=", "unit": "nM" }
Binding affinity to HIV1 NL4-3 dimeric capsid C-terminal domain (146 to 231 residues) by isothermal titration calorimetry
[ "main" ]
[]
(22) Bartonova, V.; Igonet, S.; Sticht, J.; Glass, B.; Habermann, A.; Vaney, M. C.; Sehr, P.; Lewis, J.; Rey, F. A.; Krausslich, H. G. Residues in the HIV-1 capsid assembly inhibitor binding site are essential for maintaining the assembly-competent quaternary structure of the capsid protein. J. Biol. Chem. 2008, 283 (4...
{"Figure 6 Caption": "Figure 6. Isothermal titrations of CAI (A,B) and compound 33 (C,D) to HIV-1 CA or CA CTD. Experimental details are described in Experimental Section.", "Materials and Methods - Isothermal Titration Calorimetry": "Isothermal Titration Calorimetry. The binding characteristics of CAI peptide were det...
{"assay_conditions": {"buffer_composition": "30 mM MES, 10% glycerol, 2 mM 2-mercaptoethanol, 2% DMSO", "control_method": "Titration of ligand into buffer alone", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "2", "total_count": null}, "pH": 6.0, "reference_cell_...
itc
26685880.json
51218821
51,218,804
26,685,880
Structural capsid protein
{ "smiles": "CC[C@H](C)[C@H](N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N1CCC[C@H]1C(N)=O" }
{ "type": "Kd", "value": 4000, "relation": "=", "unit": "nM" }
Binding affinity to full length HIV1 NL4-3 capsid (1 to 231 residues) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 6 Caption": "Figure 6. Isothermal titrations of CAI (A,B) and compound 33 (C,D) to HIV-1 CA or CA CTD. Experimental details are described in Experimental Section.", "Figure 6 Data (Panel A)": "KD = 4.0 ± 0.5 uM; ΔH = -12.5 ± 0.2 kcal·mol⁻¹; -TΔS = 5.1 ± 0.3 kcal·mol⁻¹", "Figure 6 Data (Panel B)": "KD = 3.0 ± 0...
{"assay_conditions": {"buffer_composition": "30 mM MES, 10% glycerol, 2 mM 2-mercaptoethanol, 2% DMSO", "control_method": "Titration of ligand into buffer alone", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "2", "total_count": null}, "pH": 6.0, "reference_cell_...
itc
26685880.json
51218804
51,218,820
26,685,880
Structural capsid protein
{ "smiles": "CCOC(=O)c1ccc(Nc2nc(nc3ccccc23)-c2ccncc2)cc1" }
{ "type": "Kd", "value": 140, "relation": "=", "unit": "nM" }
Binding affinity to full length HIV1 NL4-3 capsid (1 to 231 residues) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 6 Caption": "Figure 6. Isothermal titrations of CAI (A,B) and compound 33 (C,D) to HIV-1 CA or CA CTD. Experimental details are described in Experimental Section.", "Figure 6 Data (Panel A)": "KD = 4.0 ± 0.5 uM; ΔH = -12.5 ± 0.2 kcal·mol⁻¹; -TΔS = 5.1 ± 0.3 kcal·mol⁻¹", "Figure 6 Data (Panel B)": "KD = 3.0 ± 0...
{"assay_conditions": {"buffer_composition": "30 mM MES, 10% glycerol, 2 mM 2-mercaptoethanol, 2% DMSO", "control_method": "Titration of ligand into buffer alone", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "2", "total_count": null}, "pH": 6.0, "reference_cell_...
itc
26685880.json
51218820
51,218,806
26,685,880
Structural capsid protein
{ "smiles": "CN(C(=O)[C@H](Cc1ccccc1)NC(=O)Cc1c(C)[nH]c2ccccc12)c1ccccc1" }
{ "type": "Kd", "value": 2800, "relation": "=", "unit": "nM" }
Binding affinity to full length HIV1 NL4-3 capsid by isothermal titration calorimetry
[ "main" ]
[]
(22) Bartonova, V.; Igonet, S.; Sticht, J.; Glass, B.; Habermann, A.; Vaney, M. C.; Sehr, P.; Lewis, J.; Rey, F. A.; Krausslich, H. G. Residues in the HIV-1 capsid assembly inhibitor binding site are essential for maintaining the assembly-competent quaternary structure of the capsid protein. J. Biol. Chem. 2008, 283 (4...
{"Figure 6 Caption": "Figure 6. Isothermal titrations of CAI (A,B) and compound 33 (C,D) to HIV-1 CA or CA CTD. Experimental details are described in Experimental Section.", "Materials and Methods - Isothermal Titration Calorimetry": "Isothermal Titration Calorimetry. The binding characteristics of CAI peptide were det...
{"assay_conditions": {"buffer_composition": "30 mM MES, 10% glycerol, 2 mM 2-mercaptoethanol, 2% DMSO", "control_method": "Titration of ligand into buffer alone", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "2", "total_count": null}, "pH": 6.0, "reference_cell_...
itc
26685880.json
51218806
51,218,823
26,685,880
Structural capsid protein
{ "smiles": "CCOC(=O)c1ccc(Nc2nc(nc3ccccc23)-c2ccncc2)cc1" }
{ "type": "Kd", "value": 135, "relation": "=", "unit": "nM" }
Binding affinity to full length HIV1 NL4-3 dimeric capsid (1 to 231 residues) by isothermal titration calorimetry
[ "main" ]
[]
(22) Bartonova, V.; Igonet, S.; Sticht, J.; Glass, B.; Habermann, A.; Vaney, M. C.; Sehr, P.; Lewis, J.; Rey, F. A.; Krausslich, H. G. Residues in the HIV-1 capsid assembly inhibitor binding site are essential for maintaining the assembly-competent quaternary structure of the capsid protein. J. Biol. Chem. 2008, 283 (4...
{"Figure 6 Caption": "Figure 6. Isothermal titrations of CAI (A,B) and compound 33 (C,D) to HIV-1 CA or CA CTD. Experimental details are described in Experimental Section.", "Materials and Methods - Isothermal Titration Calorimetry": "Isothermal Titration Calorimetry. The binding characteristics of CAI peptide were det...
{"assay_conditions": {"buffer_composition": "30 mM MES, 10% glycerol, 2 mM 2-mercaptoethanol, 2% DMSO", "control_method": "Titration of ligand into buffer alone", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "2", "total_count": null}, "pH": 6.0, "reference_cell_...
itc
26685880.json
51218823
50,474,711
26,701,186
Bromodomain-containing protein 4
{ "smiles": "COc1ccc2CCCN(CCCNC(=O)c3cccc4NC(=O)[C@@H](C)Nc34)c2c1" }
{ "type": "Kd", "value": 1400, "relation": "=", "unit": "nM" }
Inhibition of human BRD4 by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26701186.json
50474711
50,474,712
26,701,186
CREB-binding protein
{ "smiles": "C[C@@H](Cn1c(CCc2ccccc2)nc2cc(ccc12)-c1c(C)noc1C)N1CCOCC1" }
{ "type": "Kd", "value": 21, "relation": "=", "unit": "nM" }
Inhibition of human CREBBP expressed in competent escherichia coli BL21(DE3)-R3-pRARE2 cells by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26701186.json
50474712
50,474,713
26,701,186
CREB-binding protein
{ "smiles": "CCC(=O)N1CCOc2c(C1)cc(cc2OC[C@H]1CCCN(C)C1)-c1ccc(OC)c(OC)c1" }
{ "type": "Kd", "value": 151, "relation": "=", "unit": "nM" }
Inhibition of human CREBBP expressed in competent escherichia coli BL21(DE3)-R3-pRARE2 cells by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26701186.json
50474713
50,474,710
26,701,186
CREB-binding protein
{ "smiles": "COc1ccc2CCCN(CCCNC(=O)c3cccc4NC(=O)[C@@H](C)Nc34)c2c1" }
{ "type": "Kd", "value": 390, "relation": "=", "unit": "nM" }
Inhibition of human His6-tagged CREBBP expressed in competent Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26701186.json
50474710
50,474,714
26,701,186
Histone acetyltransferase p300
{ "smiles": "CCC(=O)N1CCOc2c(C1)cc(cc2OC[C@H]1CCCN(C)C1)-c1ccc(OC)c(OC)c1" }
{ "type": "Kd", "value": 167, "relation": "=", "unit": "nM" }
Inhibition of human p300 expressed in competent escherichia coli BL21(DE3)-R3-pRARE2 cells by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26701186.json
50474714
50,886,179
26,702,435
Transcription activator BRG1
{ "smiles": "Oc1ccccc1C(=O)C=CN1C[C@H]2C[C@@H]1CN2c1ccccn1" }
{ "type": "Kd", "value": 89, "relation": "=", "unit": "nM" }
Reverse ITC (compound as receptor). Domain start/stop: L1451-E1580
[]
[]
none
{}
null
itc
26702435.json
50886179
50,886,178
26,702,435
Protein polybromo-1
{ "smiles": "Oc1ccccc1C(=O)C=CN1C[C@H]2C[C@@H]1CN2c1ccccn1" }
{ "type": "Kd", "value": 48, "relation": "=", "unit": "nM" }
Reverse ITC (compound as receptor). Domain start/stop: S613-D734
[]
[]
none
{}
null
itc
26702435.json
50886178
50,467,244
26,727,270
Protein S100-B
{ "smiles": "NC(=N)c1ccc(OCCCCCOc2ccc(cc2)C(N)=N)cc1" }
{ "type": "Kd", "value": 50000, "relation": "=", "unit": "nM" }
Binding affinity to recombinant rat calcium loaded S100-B by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26727270.json
50467244
50,472,558
26,731,131
Histone acetyltransferase KAT2B
{ "smiles": "CNC(=O)c1cc(OCC(=O)Nc2ccccc2)ccc1OC1CCOCC1" }
{ "type": "Kd", "value": 6800, "relation": "=", "unit": "nM" }
Binding affinity to N-terminal His-tagged PCAF (715 to 831 residues) (unknown origin) expressed in Escherichia coli Rosetta cells by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. Compounds identified as PCAF binders. a) Chemical structures of three in-house available compounds that contain the fragment-related Kac mimetic scaffolds. b) Average Tm shift values from triplicate experiments for the selected compounds. c) ITC binding data for the interactions between ...
{"assay_conditions": {"buffer_composition": "25 mM HEPES, 150 mM NaCl, 0.5 mM TCEP", "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": 7.5, "reference_cell_content": null, "stirring_speed": null, "temperature_...
itc
26731131.json
50472558
50,472,559
26,731,131
Histone acetyltransferase KAT2B
{ "smiles": "Cc1cc(=O)n(C)c2cc(NS(C)(=O)=O)ccc12" }
{ "type": "Kd", "value": 20980, "relation": "=", "unit": "nM" }
Binding affinity to N-terminal His-tagged PCAF (715 to 831 residues) (unknown origin) expressed in Escherichia coli Rosetta cells by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. Compounds identified as PCAF binders. a) Chemical structures of three in-house available compounds that contain the fragment-related Kac mimetic scaffolds. b) Average Tm shift values from triplicate experiments for the selected compounds. c) ITC binding data for the interactions between ...
{"assay_conditions": {"buffer_composition": "25 mM HEPES, 150 mM NaCl, 0.5 mM TCEP", "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": 7.5, "reference_cell_content": null, "stirring_speed": null, "temperature_...
itc
26731131.json
50472559
50,482,272
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(ccc1c23)S(=O)(=O)Nc1ccc(F)cc1" }
{ "type": "Kd", "value": 1234, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482272
50,482,274
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(NS(=O)(=O)c4cc(Cl)ccc4OC)ccc1c23" }
{ "type": "Kd", "value": 180, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482274
50,482,275
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(NS(=O)(=O)c4cc(Br)ccc4OC)ccc1c23" }
{ "type": "Kd", "value": 137, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482275
50,482,276
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(ccc1c23)S(=O)(=O)NCCCCNC(=O)OC(C)(C)C" }
{ "type": "Kd", "value": 421, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482276
50,482,282
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCCNS(=O)(=O)c1ccc2N(CC)C(=O)c3cccc1c23" }
{ "type": "Kd", "value": 224, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482282
50,482,481
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(ccc1c23)S(=O)(=O)NCCCN1CCN(C)CC1" }
{ "type": "Kd", "value": 3751, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482481
50,482,484
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(NS(=O)(=O)c4ccc(F)cc4F)ccc1c23" }
{ "type": "Kd", "value": 275, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482484
50,482,485
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(ccc1c23)S(=O)(=O)Nc1ccccc1C(O)=O" }
{ "type": "Kd", "value": 392, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482485
50,482,519
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(NS(=O)(=O)C4CCCCC4)ccc1c23" }
{ "type": "Kd", "value": 255, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482519
50,482,521
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(NS(=O)(=O)c4ccc(F)cc4)ccc1c23" }
{ "type": "Kd", "value": 390, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482521
50,482,538
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(ccc1c23)S(=O)(=O)NC1CCCCC1" }
{ "type": "Kd", "value": 124, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482538
50,482,539
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCCCS(=O)(=O)Nc1ccc2N(CC)C(=O)c3cccc1c23" }
{ "type": "Kd", "value": 218, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482539
50,482,540
26,731,490
Bromodomain-containing protein 4
{ "smiles": "CCN1C(=O)c2cccc3c(ccc1c23)S(=O)(=O)NCC1CCN(CC1)C(C)=O" }
{ "type": "Kd", "value": 2340, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482540
50,482,543
26,731,490
Bromodomain-containing protein 4
{ "smiles": "Cc1nnc2[C@H](CC(=O)OC(C)(C)C)N=C(c3c(C)c(C)sc3-n12)c1ccc(Cl)cc1" }
{ "type": "Kd", "value": 34, "relation": "=", "unit": "nM" }
Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry
[]
[]
none
{"error": "CUDA out of memory. Tried to allocate 3.03 GiB. GPU 0 has a total capacity of 79.22 GiB of which 2.10 GiB is free. Process 3774929 has 6.98 GiB memory in use. Including non-PyTorch memory, this process has 70.12 GiB memory in use. Of the allocated memory 62.94 GiB is allocated by PyTorch, and 6.51 GiB is res...
null
itc
26731490.json
50482543
50,487,431
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2CC)c1" }
{ "type": "Kd", "value": 2900, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, S066−S073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487431
50,487,432
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(=O)CO)c2CC)c1" }
{ "type": "Kd", "value": 4900, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, S066−S073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487432
50,487,433
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)Nc1ccc(F)c(c1)S(=O)(=O)N1CCOCC1" }
{ "type": "Kd", "value": 6100, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, S066−S073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487433
50,487,434
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)Nc1cccc(OCC(N)=O)c1" }
{ "type": "Kd", "value": 41000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, S066−S073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487434
50,487,435
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)N(C)Cc1cccc(c1)C(N)=O" }
{ "type": "Kd", "value": 50000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, S066−S073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487435
50,487,436
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2CC)c1" }
{ "type": "Kd", "value": 2400, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 2 by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26731611.json
50487436
50,487,437
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(=O)CO)c2CC)c1" }
{ "type": "Kd", "value": 11000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 2 by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26731611.json
50487437
50,487,438
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)Nc1ccc(F)c(c1)S(=O)(=O)N1CCOCC1" }
{ "type": "Kd", "value": 18000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 2 by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26731611.json
50487438
50,487,439
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)Nc1cccc(OCC(N)=O)c1" }
{ "type": "Kd", "value": 23000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 2 by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26731611.json
50487439
50,487,440
26,731,611
Bromodomain-containing protein 3
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)N(C)Cc1cccc(c1)C(N)=O" }
{ "type": "Kd", "value": 19000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD3 bromodomain 2 by isothermal titration calorimetry
[]
[]
none
{}
null
itc
26731611.json
50487440
50,487,416
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2CC)c1" }
{ "type": "Kd", "value": 240, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487416
50,487,417
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2C)c1" }
{ "type": "Kd", "value": 460, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487417
50,487,418
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(N)=O)c2CC)c1" }
{ "type": "Kd", "value": 810, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487418
50,487,419
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(=O)CO)c2CC)c1" }
{ "type": "Kd", "value": 7900, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487419
50,487,420
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2C(C)C)c1" }
{ "type": "Kd", "value": 7200, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487420
50,487,421
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCN(CC)S(=O)(=O)c1cccc(NC(=O)c2[nH]c(C)c(C(C)=O)c2CC)c1" }
{ "type": "Kd", "value": 5700, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487421
50,487,422
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)Nc1cc(ccc1C)S(=O)(=O)NC" }
{ "type": "Kd", "value": 9200, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487422
50,487,423
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCN(CC)C(=O)c1cccc(NC(=O)c2[nH]c(C)c(C(C)=O)c2CC)c1" }
{ "type": "Kd", "value": 6800, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487423
50,487,424
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)N1CCc2ccc(cc12)S(=O)(=O)NC" }
{ "type": "Kd", "value": 7400, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487424
50,487,425
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)Nc1ccc(F)c(c1)S(=O)(=O)N1CCOCC1" }
{ "type": "Kd", "value": 1300, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487425
50,487,426
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCN(CC)S(=O)(=O)c1cc(NC(=O)c2[nH]c(C)c(C(C)=O)c2CC)c(O)cc1C" }
{ "type": "Kd", "value": 880, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487426
50,487,427
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)Nc1cccc(OCC(N)=O)c1" }
{ "type": "Kd", "value": 5800, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487427
50,487,428
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)Nc1cc(ccc1O)S(=O)(=O)Nc1ccccc1OC" }
{ "type": "Kd", "value": 3900, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487428
50,487,429
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)N(C)Cc1cccc(c1)C(N)=O" }
{ "type": "Kd", "value": 12000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487429
50,487,430
26,731,611
Bromodomain-containing protein 4
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)NC" }
{ "type": "Kd", "value": 6800, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRD4 bromodomain 1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487430
50,487,441
26,731,611
Peregrin
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2CC)c1" }
{ "type": "Kd", "value": 38000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRPF1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487441
50,487,442
26,731,611
Peregrin
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2C)c1" }
{ "type": "Kd", "value": 5900, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRPF1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487442
50,487,443
26,731,611
Peregrin
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(N)=O)c2CC)c1" }
{ "type": "Kd", "value": 48000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRPF1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487443
50,487,444
26,731,611
Peregrin
{ "smiles": "CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2C(C)C)c1" }
{ "type": "Kd", "value": 36000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRPF1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487444
50,487,445
26,731,611
Peregrin
{ "smiles": "CCc1c([nH]c(C)c1C(C)=O)C(=O)NC" }
{ "type": "Kd", "value": 30000, "relation": "=", "unit": "nM" }
Binding affinity to partial length human BRPF1 by isothermal titration calorimetry
[ "main" ]
[]
(24) Keller, S.; Vargas, C.; Zhao, H.; Piszczek, G.; Brautigam, C. A.; Schuck, P. High-precision isothermal titration calorimetry with automated peak-shape analysis. Anal. Chem. 2012, 84, 5066−5073. (25) Houtman, J. C. D.; Brown, P. H.; Bowden, B.; Yamaguchi, H.; Appella, E.; Samelson, L. E.; Schuck, P. Studying multis...
{"ITC Data Analysis (Methods Section)": "According to Microcal’s manual “ITC Data Analysis in Origin” (September 1998) as a function describing the sum of heat of each individual injection. A correction term was included to compensate for displacement of volume of the sample cell in the course of subsequent injections ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": "12", "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26731611.json
50487445
339,342
26,808,391
Aurora kinase B
{ "smiles": "CCOC(=O)C1=C(NC(=C([C@H]1c2cccc(c2Cl)Cl)C(=O)OC)C)C" }
{ "type": "Kd", "value": 1140, "relation": "=", "unit": "nM" }
Calorimetric titrations were performed in a Microcal iTC 200 microcalorimeter. Freshly purified 5 uM protein (Aurora A/B kinases) was titrated against 100 uM ligand (felodipine/ PTK66) in each case at 25 °C. Proteins and the ligandswere diluted in the final dialysate (20 mM Tris-HCl, pH 8.0, 0.2 mM EDTA and 100 mM KCl)...
[ "main" ]
[]
none
{"Isothermal Titration Calorimetry (ITC) section": "Calorimetric titrations were performed in a Microcal iTC 200 microcalorimeter. Freshly purified 5 uM protein (Aurora A/B kinases) was titrated against 100 uM ligand (felodipine/ PTK66) in each case at 25 °C. Proteins and the ligands were diluted in the final dialysate...
{"assay_conditions": {"buffer_composition": "20 mM Tris-HCl, 0.2 mM EDTA, 100 mM KCl", "control_method": "Dilutions of 100 uM felodipine/PTK66 in dialysate containing equal percentage of DMSO served as controls", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null...
itc
26808391.json
339342
339,343
26,808,391
Aurora kinase B
{ "smiles": "Cc1cc(O)cc(O)c1\\N=N\\c1nccs1" }
{ "type": "Kd", "value": 1750, "relation": "=", "unit": "nM" }
Calorimetric titrations were performed in a Microcal iTC 200 microcalorimeter. Freshly purified 5 uM protein (Aurora A/B kinases) was titrated against 100 uM ligand (felodipine/ PTK66) in each case at 25 °C. Proteins and the ligandswere diluted in the final dialysate (20 mM Tris-HCl, pH 8.0, 0.2 mM EDTA and 100 mM KCl)...
[ "main" ]
[]
none
{"Isothermal Titration Calorimetry (ITC) section": "Calorimetric titrations were performed in a Microcal iTC 200 microcalorimeter. Freshly purified 5 uM protein (Aurora A/B kinases) was titrated against 100 uM ligand (felodipine/ PTK66) in each case at 25 °C. Proteins and the ligands were diluted in the final dialysate...
{"assay_conditions": {"buffer_composition": "20 mM Tris-HCl, 0.2 mM EDTA, 100 mM KCl", "control_method": "Dilutions of 100 uM felodipine/PTK66 in dialysate containing equal percentage of DMSO served as controls", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null...
itc
26808391.json
339343
339,344
26,808,391
Aurora kinase B
{ "smiles": "Cc1cc(O)cc(O)c1\\N=N\\c1nccs1" }
{ "type": "Kd", "value": 500, "relation": "=", "unit": "nM" }
Calorimetric titrations were performed in a Microcal iTC 200 microcalorimeter. Freshly purified 5 uM protein (Aurora A/B kinases) was titrated against 100 uM ligand (felodipine/ PTK66) in each case at 25 °C. Proteins and the ligandswere diluted in the final dialysate (20 mM Tris-HCl, pH 8.0, 0.2 mM EDTA and 100 mM KCl)...
[ "main" ]
[]
none
{"Isothermal Titration Calorimetry (ITC) section": "Calorimetric titrations were performed in a Microcal iTC 200 microcalorimeter. Freshly purified 5 uM protein (Aurora A/B kinases) was titrated against 100 uM ligand (felodipine/ PTK66) in each case at 25 °C. Proteins and the ligands were diluted in the final dialysate...
{"assay_conditions": {"buffer_composition": "20 mM Tris-HCl, 0.2 mM EDTA, 100 mM KCl", "control_method": "Dilutions of 100 uM felodipine/PTK66 in dialysate containing equal percentage of DMSO served as controls", "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null...
itc
26808391.json
339344
50,485,232
26,824,386
Protein arginine N-methyltransferase 6
{ "smiles": "NCCN1CCC(Cc2ccccc2)CC1" }
{ "type": "Kd", "value": 970, "relation": "=", "unit": "nM" }
Binding affinity to Inhibition of N-terminal hexa-His tagged human PRMT6 expressed in Sf9 cells by ITC method
[ "main" ]
[]
(20) Murray, C. W.; Verdonk, M. L. The consequences of translational and rotational entropy lost by small molecules on binding to proteins. J. Comput.-Aided Mol. Des. 2002, 16, 741−53.
{"Experimental Section - Isothermal Titration Calorimetry": "Isothermal Titration Calorimetry. Isothermal titration calorimetry (ITC) was performed at 25 °C in a Nano ITC instrument (TA Instruments, USA). The cell was loaded with 33 uM PRMT6 and 3.3% DMSO in PBS buffer. The syringe was loaded with 100 uM fragment 7 and...
{"assay_conditions": {"buffer_composition": "PBS, 3.3% DMSO", "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": "180", "subsequent_volume": "2", "total_count": "25"}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analy...
itc
26824386.json
50485232
50,504,441
26,914,985
Bromodomain-containing protein 4
{ "smiles": "COc1cc(c(OC)cc1CN(C)C)-c1cn(C)c(=O)c2cnccc12" }
{ "type": "Kd", "value": 20000, "relation": ">", "unit": "nM" }
Binding affinity to human BRD4-BD1 expressed in Escherichia coli L21(DE3)-R3-pRARE2 cells by VP-ITC method
[]
[]
none
{}
null
itc
26914985.json
50504441
50,504,442
26,914,985
Bromodomain-containing protein 4
{ "smiles": "COc1cc(cc(OC)c1CN(C)C)-c1cn(C)c(=O)c2cnccc12" }
{ "type": "Kd", "value": 20000, "relation": ">", "unit": "nM" }
Binding affinity to human BRD4-BD1 expressed in Escherichia coli L21(DE3)-R3-pRARE2 cells by VP-ITC method
[]
[]
none
{}
null
itc
26914985.json
50504442
50,504,447
26,914,985
Bromodomain-containing protein 7
{ "smiles": "COc1cc(c(OC)cc1CN(C)C)-c1cn(C)c(=O)c2cnccc12" }
{ "type": "Kd", "value": 239, "relation": "=", "unit": "nM" }
Binding affinity to human BRD7 expressed in Escherichia coli L21(DE3)-R3-pRARE2 cells by VP-ITC method
[]
[]
none
{}
null
itc
26914985.json
50504447
50,503,916
26,914,985
Bromodomain-containing protein 9
{ "smiles": "COc1cc(c(OC)cc1CN(C)C)-c1cn(C)c(=O)c2cnccc12" }
{ "type": "Kd", "value": 14, "relation": "=", "unit": "nM" }
Binding affinity to human BRD9 expressed in Escherichia coli L21(DE3)-R3-pRARE2 cells by VP-ITC method
[ "main" ]
[]
none
{"Figure 3 Caption": "Figure 3. ITC analysis of compounds 1 and 2 (T = 293.15 K). (a) Compound 1 binds with a KD value of 15.4 nM (ΔH = −12.1 kcal/mol) and (b) 2 binds with a KD value of 14.1 nM (ΔH = −11.2 kcal/mol).", "Results Section": "Finally, binding affinities of 1 and 2 toward BRD9 were measured by isothermal t...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "20"}, "data_analysis": {"bind...
itc
26914985.json
50503916
50,503,917
26,914,985
Bromodomain-containing protein 9
{ "smiles": "COc1cc(cc(OC)c1CN(C)C)-c1cn(C)c(=O)c2cnccc12" }
{ "type": "Kd", "value": 15, "relation": "=", "unit": "nM" }
Binding affinity to human BRD9 expressed in Escherichia coli L21(DE3)-R3-pRARE2 cells by VP-ITC method
[ "main" ]
[]
none
{"Figure 3 Caption": "Figure 3. ITC analysis of compounds 1 and 2 (T = 293.15 K). (a) Compound 1 binds with a KD value of 15.4 nM (ΔH = −12.1 kcal/mol) and (b) 2 binds with a KD value of 14.1 nM (ΔH = −11.2 kcal/mol).", "Results Section": "Finally, binding affinities of 1 and 2 toward BRD9 were measured by isothermal t...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "20"}, "data_analysis": {"bind...
itc
26914985.json
50503917
50,504,434
26,914,985
Chromatin remodeling regulator CECR2
{ "smiles": "COc1cc(c(OC)cc1CN(C)C)-c1cn(C)c(=O)c2cnccc12" }
{ "type": "Kd", "value": 200, "relation": "=", "unit": "nM" }
Binding affinity to human CECR2 expressed in Escherichia coli L21(DE3)-R3-pRARE2 cells by VP-ITC method
[]
[]
none
{}
null
itc
26914985.json
50504434
50,504,435
26,914,985
Chromatin remodeling regulator CECR2
{ "smiles": "COc1cc(cc(OC)c1CN(C)C)-c1cn(C)c(=O)c2cnccc12" }
{ "type": "Kd", "value": 187, "relation": "=", "unit": "nM" }
Binding affinity to human CECR2 expressed in Escherichia coli L21(DE3)-R3-pRARE2 cells by VP-ITC method
[]
[]
none
{}
null
itc
26914985.json
50504435
50,504,356
26,914,985
Bromodomain-containing protein 7
{ "smiles": "CC(C)CS(=O)(=O)N[C@H]1CCC(=O)N([C@@H]1c1ccc(Cl)cc1)c1ccc2c(C)cc(=O)n(C)c2c1" }
{ "type": "Kd", "value": 909, "relation": "=", "unit": "nM" }
Inhibition of human BRD7 by VP-ITC method
[]
[]
none
{}
null
itc
26914985.json
50504356
50,504,362
26,914,985
Bromodomain-containing protein 9
{ "smiles": "CC(C)CS(=O)(=O)N[C@H]1CCC(=O)N([C@@H]1c1ccc(Cl)cc1)c1ccc2c(C)cc(=O)n(C)c2c1" }
{ "type": "Kd", "value": 99, "relation": "=", "unit": "nM" }
Inhibition of human BRD9 isoform 1 by VP-ITC method
[]
[]
none
{}
null
itc
26914985.json
50504362
51,218,848
26,944,615
Transcription factor 4
{ "smiles": "Cc1ccc(\\C=N\\NC(=O)c2ccccc2Oc2ccccc2)o1" }
{ "type": "Kd", "value": 450, "relation": "=", "unit": "nM" }
Inhibition of His6 tagged Tcf4 1-53/beta catenin (unknown origin) interaction by VP-ITC titration calorimeter method
[]
[]
none
{}
null
itc
26944615.json
51218848
50,491,985
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CCOC(=O)CNC(=O)NCc1ccc(cc1)-c1ccncc1" }
{ "type": "Kd", "value": 97300, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50491985
50,491,986
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CCOC(=O)CNC(=O)NCc1ccccc1" }
{ "type": "Kd", "value": 97300, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50491986
50,491,989
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "Nc1ccc(CNC(=O)NCC(=O)N2CCCC2)cc1" }
{ "type": "Kd", "value": 22700, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50491989
50,491,990
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CSCC[C@H](NC(=O)NCc1ccc(N)cc1)C(=O)N1CCC[C@H]1c1ccccc1SC" }
{ "type": "Kd", "value": 410, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50491990
50,491,993
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "Nc1ccc(CNC(=O)NCC(=O)N2CCC[C@@H]2c2ccccc2Br)cc1" }
{ "type": "Kd", "value": 1200, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50491993
50,491,994
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CSc1ccccc1[C@H]1CCCN1C(=O)CNC(=O)NCc1ccc(N)cc1" }
{ "type": "Kd", "value": 2800, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50491994
50,491,995
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "Nc1ccc(CNC(=O)NCC(=O)N2CCC[C@@H]2c2ccccc2)cc1" }
{ "type": "Kd", "value": 5400, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50491995
50,491,999
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CCOC(=O)[C@H](CCSC)NC(=O)NCc1ccc(N)cc1" }
{ "type": "Kd", "value": 5120, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50491999
50,492,000
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CCOC(=O)CNC(=O)NCc1ccc(N)cc1" }
{ "type": "Kd", "value": 10000, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50492000
50,492,002
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CSCC[C@H](NC(=O)NCc1ccc(N)cc1)C(=O)N1CCCC1" }
{ "type": "Kd", "value": 57600, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50492002
50,492,003
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CCOC(=O)[C@H](CC(C)C)NC(=O)NCc1ccc(N)cc1" }
{ "type": "Kd", "value": 8800, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50492003
50,492,005
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CCOC(=O)CNC(=O)NCc1ccc(NC(C)=O)cc1" }
{ "type": "Kd", "value": 34100, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50492005
50,492,006
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\\C=C\\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O)C(C)C" }
{ "type": "Kd", "value": 13, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50492006
50,492,007
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CCOC(=O)CNC(=O)NCc1cccc(c1)-c1ccncc1N" }
{ "type": "Kd", "value": 92500, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50492007
50,492,009
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CCOC(=O)CNC(=O)NCc1cccc(c1)-c1cccnc1" }
{ "type": "Kd", "value": 127000, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50492009
50,492,010
26,950,392
Peptidyl-prolyl cis-trans isomerase D
{ "smiles": "CSCC[C@H](NC(=O)NCc1ccc(N)cc1)C(=O)N1CCC[C@@H]1c1ccccc1SC" }
{ "type": "Kd", "value": 82000, "relation": "=", "unit": "nM" }
Binding affinity to Cyclophilin D (unknown origin) by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 4 Caption": "Figure 4. ITC profiles for the binding of selected compounds to CypD. (a) Compound 4, (b) Compound 10, (c) Compound 12, (d) Compound 14, (e) Compound 11, and (f) Compound 19. The top panel shows the raw calorimetric data obtained upon titration of CypD with each ligand; the bottom panel shows the ...
{"assay_conditions": {"buffer_composition": null, "control_method": null, "injection_parameters": {"duration": null, "first_volume": null, "spacing": null, "subsequent_volume": null, "total_count": null}, "pH": null, "reference_cell_content": null, "stirring_speed": null, "temperature_c": "25"}, "data_analysis": {"bind...
itc
26950392.json
50492010
50,501,856
27,031,670
Kelch-like ECH-associated protein 1
{ "smiles": "COc1cc(cc2nnn(C)c12)[C@@H](CC(O)=O)c1ccc(C)c(CN2C[C@@H](C)Oc3ccccc3S2(=O)=O)c1" }
{ "type": "Kd", "value": 1.3, "relation": "=", "unit": "nM" }
Binding affinity to human recombinant N-terminal His6 and Avi-tagged KEAP1 (321 to 609 residues) expressed in baculovirus infected sf9 cells by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 2 caption": "Figure 2. Structure-driven elaboration of fragment 1. (a) Overlay of fragments 1 and 2 bound to the Kelch domain in the context of the elaborated compound 4. The benzotriazole superposes well with the heterocyclic system of fragment 2. Protein−ligand hydrogen bonds are depicted by dashed lines. (b...
{"assay_conditions": {"buffer_composition": "50 mM 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES)-NaOH, 100 mM NaCl, 1 mM TCEP, 5% DMSO", "control_method": "Heats of dilution were estimated using the final injections of each individual titration and subtracted before data analysis", "injection_parameters": ...
itc
27031670.json
50501856
50,501,857
27,031,670
Kelch-like ECH-associated protein 1
{ "smiles": "CN(Cc1cc(ccc1Cl)[C@H](CC(O)=O)c1ccc2n(C)nnc2c1)S(=O)(=O)c1ccccc1" }
{ "type": "Kd", "value": 670, "relation": "=", "unit": "nM" }
Binding affinity to human recombinant N-terminal His6 and Avi-tagged KEAP1 (321 to 609 residues) expressed in baculovirus infected sf9 cells by isothermal titration calorimetry
[ "main" ]
[]
none
{"Figure 2 caption": "Figure 2. Structure-driven elaboration of fragment 1. (a) Overlay of fragments 1 and 2 bound to the Kelch domain in the context of the elaborated compound 4. The benzotriazole superposes well with the heterocyclic system of fragment 2. Protein−ligand hydrogen bonds are depicted by dashed lines. (b...
{"assay_conditions": {"buffer_composition": "50 mM 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES)-NaOH, 100 mM NaCl, 1 mM TCEP, 5% DMSO", "control_method": "Heats of dilution were estimated using the final injections of each individual titration and subtracted before data analysis", "injection_parameters": ...
itc
27031670.json
50501857