Found 7 hits with Last Name = 'kouzarides' and Initial = 't' Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Bromodomain-containing protein 9
(Homo sapiens (Human)) | BDBM50147620
(CHEMBL3769507)Show SMILES CCn1cc(-c2cccc(c2)C(F)(F)F)c2sc(cc2c1=O)C(=N)NC1CCS(=O)(=O)CC1 Show InChI InChI=1S/C22H22F3N3O3S2/c1-2-28-12-17(13-4-3-5-14(10-13)22(23,24)25)19-16(21(28)29)11-18(32-19)20(26)27-15-6-8-33(30,31)9-7-15/h3-5,10-12,15H,2,6-9H2,1H3,(H2,26,27) | PDB
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UniProtKB/SwissProt
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CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D
Curated by ChEMBL
| Assay Description Inhibition of BRD4 bromodomain 1 (unknown origin) incubated in dark for 30 mins by TR-FRET assay |
J Med Chem 59: 1425-39 (2016)
Article DOI: 10.1021/acs.jmedchem.5b00256 BindingDB Entry DOI: 10.7270/Q2W099HJ |
More data for this Ligand-Target Pair | |
Chromatin remodeling regulator CECR2
(Homo sapiens (Human)) | BDBM50147620
(CHEMBL3769507)Show SMILES CCn1cc(-c2cccc(c2)C(F)(F)F)c2sc(cc2c1=O)C(=N)NC1CCS(=O)(=O)CC1 Show InChI InChI=1S/C22H22F3N3O3S2/c1-2-28-12-17(13-4-3-5-14(10-13)22(23,24)25)19-16(21(28)29)11-18(32-19)20(26)27-15-6-8-33(30,31)9-7-15/h3-5,10-12,15H,2,6-9H2,1H3,(H2,26,27) | PDB
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UniProtKB/SwissProt
GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 196 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D
Curated by ChEMBL
| Assay Description Inhibition of BRD3 in human HUT78 cells incubated for 45 mins by chemoproteomic competition binding assay |
J Med Chem 59: 1425-39 (2016)
Article DOI: 10.1021/acs.jmedchem.5b00256 BindingDB Entry DOI: 10.7270/Q2W099HJ |
More data for this Ligand-Target Pair | |
CREB-binding protein
(Homo sapiens (Human)) | BDBM50266292
(CHEMBL3906203)Show SMILES CCC(=O)N1CCOc2c(C1)cc(cc2OCC1CCCN(C)C1)-c1ccc(OC)c(OC)c1 Show InChI InChI=1S/C22H17N3O3/c1-12-10-17-18(24(3)22(28)23(17)2)11-16(12)25-20(26)14-8-4-6-13-7-5-9-15(19(13)14)21(25)27/h4-11H,1-3H3 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
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PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 324 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Oxford
Curated by ChEMBL
| Assay Description Alphascreen assay. Binding to CREBBPA (domain start/stop: R1081-G1197) by alphascreen assay |
Cancer Res 75: 5106-5119 (2015)
Article DOI: 10.1158/0008-5472.CAN-15-0236 BindingDB Entry DOI: 10.7270/Q2HQ43GJ |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Bromodomain-containing protein 4
(Homo sapiens (Human)) | BDBM50266292
(CHEMBL3906203)Show SMILES CCC(=O)N1CCOc2c(C1)cc(cc2OCC1CCCN(C)C1)-c1ccc(OC)c(OC)c1 Show InChI InChI=1S/C22H17N3O3/c1-12-10-17-18(24(3)22(28)23(17)2)11-16(12)25-20(26)14-8-4-6-13-7-5-9-15(19(13)14)21(25)27/h4-11H,1-3H3 | PDB
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UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
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PC cid PC sid PDB UniChem
Similars
| Article PubMed
| n/a | n/a | 2.46E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Oxford
Curated by ChEMBL
| Assay Description Alphascreen assay. Binding to BRD4A (domain start/stop: N44-E168) by alphascreen assay |
Cancer Res 75: 5106-5119 (2015)
Article DOI: 10.1158/0008-5472.CAN-15-0236 BindingDB Entry DOI: 10.7270/Q2HQ43GJ |
More data for this Ligand-Target Pair | |
CREB-binding protein
(Homo sapiens (Human)) | BDBM50147620
(CHEMBL3769507)Show SMILES CCn1cc(-c2cccc(c2)C(F)(F)F)c2sc(cc2c1=O)C(=N)NC1CCS(=O)(=O)CC1 Show InChI InChI=1S/C22H22F3N3O3S2/c1-2-28-12-17(13-4-3-5-14(10-13)22(23,24)25)19-16(21(28)29)11-18(32-19)20(26)27-15-6-8-33(30,31)9-7-15/h3-5,10-12,15H,2,6-9H2,1H3,(H2,26,27) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 3.05E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D
Curated by ChEMBL
| Assay Description Binding affinity to partial length human BRD7 by BROMOscan assay |
J Med Chem 59: 1425-39 (2016)
Article DOI: 10.1021/acs.jmedchem.5b00256 BindingDB Entry DOI: 10.7270/Q2W099HJ |
More data for this Ligand-Target Pair | |
Peregrin
(Homo sapiens (Human)) | BDBM50147620
(CHEMBL3769507)Show SMILES CCn1cc(-c2cccc(c2)C(F)(F)F)c2sc(cc2c1=O)C(=N)NC1CCS(=O)(=O)CC1 Show InChI InChI=1S/C22H22F3N3O3S2/c1-2-28-12-17(13-4-3-5-14(10-13)22(23,24)25)19-16(21(28)29)11-18(32-19)20(26)27-15-6-8-33(30,31)9-7-15/h3-5,10-12,15H,2,6-9H2,1H3,(H2,26,27) | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 5.20E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D
Curated by ChEMBL
| Assay Description Inhibition of BRD9 in human HUT78 cells incubated for 45 mins by chemoproteomic competition binding assay |
J Med Chem 59: 1425-39 (2016)
Article DOI: 10.1021/acs.jmedchem.5b00256 BindingDB Entry DOI: 10.7270/Q2W099HJ |
More data for this Ligand-Target Pair | |
Bromodomain-containing protein 4
(Homo sapiens (Human)) | BDBM50147620
(CHEMBL3769507)Show SMILES CCn1cc(-c2cccc(c2)C(F)(F)F)c2sc(cc2c1=O)C(=N)NC1CCS(=O)(=O)CC1 Show InChI InChI=1S/C22H22F3N3O3S2/c1-2-28-12-17(13-4-3-5-14(10-13)22(23,24)25)19-16(21(28)29)11-18(32-19)20(26)27-15-6-8-33(30,31)9-7-15/h3-5,10-12,15H,2,6-9H2,1H3,(H2,26,27) | PDB
KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 1.12E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D
Curated by ChEMBL
| Assay Description Inhibition of BRD4 bromodomain 1 (unknown origin) incubated in dark for 30 mins by TR-FRET assay |
J Med Chem 59: 1425-39 (2016)
Article DOI: 10.1021/acs.jmedchem.5b00256 BindingDB Entry DOI: 10.7270/Q2W099HJ |
More data for this Ligand-Target Pair | |