BindingDB PrimarySearch

null

SMILES: Cc1nnc2[C@H](CC(=O)OC(C)(C)C)N=C(c3c(C)c(C)sc3-n12)c1ccc(Cl)cc1

InChI Key: InChIKey=DNVXATUJJDPFDM-KRWDZBQOSA-N

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 311 hits for monomerid = 50365262
Target/Host (Institution)	Ligand	Target/Host Links	Ligand Links	Trg + Lig Links	Ki nM	ΔG° kcal/mole	IC50 nM	Kd nM	EC50/IC50 nM	k_off s^-1	k_on M^-1s^-1	pH	Temp °C
Bromodomain testis-specific protein (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB MMDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	147	n/a	n/a	n/a	n/a	7.5	25
Dana-Farber Cancer Institute, Inc. US Patent					Assay Description Assays were performed with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 150 mM ...				US Patent US9695172 (2017) BindingDB Entry DOI: 10.7270/Q2JD4TX8
Dana-Farber Cancer Institute, Inc. US Patent					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	8.15E+4	n/a	n/a	n/a	n/a	n/a	n/a
Dana-Farber Institute Curated by ChEMBL					Assay Description Inhibition of BRD4 (unknown origin) by biotinylated-JQ1 based AlphaScreen BRD binding assay				J Med Chem 57: 9019-27 (2014) Article DOI: 10.1021/jm501120z BindingDB Entry DOI: 10.7270/Q2FN17T7
Dana-Farber Institute Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	58	n/a	n/a	n/a	n/a	n/a	n/a
Shanghai Institute of Materia Medica Curated by ChEMBL					Assay Description Inhibition of BRD4(1) (unknown origin) incubated for 4 hrs by (+)-JQ1 fluorescent ligand based fluorescence anisotrophy				J Med Chem 58: 1281-97 (2015) Article DOI: 10.1021/jm501504k BindingDB Entry DOI: 10.7270/Q2P270TX
Shanghai Institute of Materia Medica Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	29	n/a	n/a	n/a	n/a	n/a	n/a
University of Michigan Curated by ChEMBL					Assay Description Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fl...				J Med Chem 58: 4927-39 (2015) Article DOI: 10.1021/acs.jmedchem.5b00613 BindingDB Entry DOI: 10.7270/Q2XD13FK
University of Michigan Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	36	n/a	n/a	n/a	n/a	n/a	n/a
University of Michigan Curated by ChEMBL					Assay Description Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by f...				J Med Chem 58: 4927-39 (2015) Article DOI: 10.1021/acs.jmedchem.5b00613 BindingDB Entry DOI: 10.7270/Q2XD13FK
University of Michigan Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 2 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	15	n/a	n/a	n/a	n/a	n/a
University of Michigan Curated by ChEMBL					Assay Description Binding affinity to biotinylated BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometr...				J Med Chem 58: 4927-39 (2015) Article DOI: 10.1021/acs.jmedchem.5b00613 BindingDB Entry DOI: 10.7270/Q2XD13FK
University of Michigan Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 2 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	6.20	n/a	n/a	n/a	n/a	n/a
University of Michigan Curated by ChEMBL					Assay Description Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferomet...				J Med Chem 58: 4927-39 (2015) Article DOI: 10.1021/acs.jmedchem.5b00613 BindingDB Entry DOI: 10.7270/Q2XD13FK
University of Michigan Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 3 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	14	n/a	n/a	n/a	n/a	n/a
University of Michigan Curated by ChEMBL					Assay Description Binding affinity to biotinylated BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometr...				J Med Chem 58: 4927-39 (2015) Article DOI: 10.1021/acs.jmedchem.5b00613 BindingDB Entry DOI: 10.7270/Q2XD13FK
University of Michigan Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 3 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	12	n/a	n/a	n/a	n/a	n/a
University of Michigan Curated by ChEMBL					Assay Description Binding affinity to biotinylated BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferomet...				J Med Chem 58: 4927-39 (2015) Article DOI: 10.1021/acs.jmedchem.5b00613 BindingDB Entry DOI: 10.7270/Q2XD13FK
University of Michigan Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	13	n/a	n/a	n/a	n/a	n/a
University of Michigan Curated by ChEMBL					Assay Description Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometr...				J Med Chem 58: 4927-39 (2015) Article DOI: 10.1021/acs.jmedchem.5b00613 BindingDB Entry DOI: 10.7270/Q2XD13FK
University of Michigan Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	6.70	n/a	n/a	n/a	n/a	n/a
University of Michigan Curated by ChEMBL					Assay Description Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferomet...				J Med Chem 58: 4927-39 (2015) Article DOI: 10.1021/acs.jmedchem.5b00613 BindingDB Entry DOI: 10.7270/Q2XD13FK
University of Michigan Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	8	n/a	n/a	n/a	n/a	n/a	n/a
The University of Tokyo Curated by ChEMBL					Assay Description Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assay				Bioorg Med Chem 23: 953-9 (2015) Article DOI: 10.1016/j.bmc.2015.01.022 BindingDB Entry DOI: 10.7270/Q26Q201X
The University of Tokyo Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	120	n/a	n/a	n/a	n/a	n/a	n/a
Guangzhou Institutes of Biomedicine and Health Curated by ChEMBL					Assay Description Inhibition of human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells using biotin-H4KAc4 as substr...				J Med Chem 59: 1565-79 (2016) Article DOI: 10.1021/acs.jmedchem.5b01511 BindingDB Entry DOI: 10.7270/Q2N87CPF
					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	77	n/a	n/a	n/a	n/a	n/a	n/a
Guangzhou Institutes of Biomedicine and Health Curated by ChEMBL					Assay Description Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using biotin-H4K5acK8acK12acK16ac as substr...				J Med Chem 59: 1565-79 (2016) Article DOI: 10.1021/acs.jmedchem.5b01511 BindingDB Entry DOI: 10.7270/Q2N87CPF
					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	34	n/a	n/a	n/a	n/a	n/a
Guangzhou Institutes of Biomedicine and Health Curated by ChEMBL					Assay Description Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration...				J Med Chem 59: 1565-79 (2016) Article DOI: 10.1021/acs.jmedchem.5b01511 BindingDB Entry DOI: 10.7270/Q2N87CPF
					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	24	n/a	n/a	n/a	n/a	n/a	n/a
Genentech Curated by ChEMBL					Assay Description Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged BRD4 bromodomain1 by alphascreen assay				J Med Chem 59: 1271-98 (2016) Article DOI: 10.1021/acs.jmedchem.5b01514 BindingDB Entry DOI: 10.7270/Q2X92D6H
Genentech Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	77	n/a	n/a	n/a	n/a	n/a	n/a
China Pharmaceutical University Curated by ChEMBL					Assay Description Inhibition of BRD4(1) (unknown origin)				Bioorg Med Chem Lett 26: 2931-2935 (2016) Article DOI: 10.1016/j.bmcl.2016.04.034 BindingDB Entry DOI: 10.7270/Q2MW2K2V
China Pharmaceutical University Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	90	n/a	n/a	n/a	n/a	n/a	n/a
China Pharmaceutical University Curated by ChEMBL					Assay Description Inhibition of human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 by bromodomain alphascreen peptide displacement assay				Bioorg Med Chem Lett 26: 2931-2935 (2016) Article DOI: 10.1016/j.bmcl.2016.04.034 BindingDB Entry DOI: 10.7270/Q2MW2K2V
China Pharmaceutical University Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	49	n/a	n/a	n/a	n/a	n/a
University of Oxford Curated by ChEMBL					Assay Description Binding affinity to BRD4-BD1 by isothermal titration calorimetry				Bioorg Med Chem 20: 1878-86 (2012) Article DOI: 10.1016/j.bmc.2011.10.080 BindingDB Entry DOI: 10.7270/Q2NC61PZ
University of Oxford Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	60	n/a	n/a	n/a	n/a	n/a
University of Oxford Curated by ChEMBL					Assay Description Binding affinity to BRD4 by isothermal titration calorimetry				Bioorg Med Chem 20: 1878-86 (2012) Article DOI: 10.1016/j.bmc.2011.10.080 BindingDB Entry DOI: 10.7270/Q2NC61PZ
University of Oxford Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 2 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	128	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Binding affinity to BRD2-BD1 by isothermal titration calorimetry				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 3 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	59.5	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Binding affinity to BRD3-BD1 by isothermal titration calorimetry				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 3 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	82	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Binding affinity to BRD3-BD2 by isothermal titration calorimetry				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	49	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Binding affinity to BRD4-BD1 by isothermal titration calorimetry				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	90.1	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Binding affinity to BRD4-BD2 by isothermal titration calorimetry				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain testis-specific protein (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB MMDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	190	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Binding affinity to BRDT-BD1 by isothermal titration calorimetry				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	77	n/a	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Displacement of acetylated histone peptide from BRD4-BD1 by luminescence proximity homogenous assay				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	33	n/a	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Displacement of acetylated histone peptide from BRD4-BD2 by luminescence proximity homogenous assay				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
CREB-binding protein (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	>1.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Japan Science and Technology Agency Curated by ChEMBL					Assay Description Displacement of acetylated histone peptide from CREBBP by luminescence proximity homogenous assay				Bioorg Med Chem 20: 1887-92 (2012) Article DOI: 10.1016/j.bmc.2012.01.018 BindingDB Entry DOI: 10.7270/Q2TX3FTN
Japan Science and Technology Agency Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	33	n/a	n/a	n/a	n/a	n/a	n/a
GlaxoSmithKline R&D Curated by ChEMBL					Assay Description Inhibition of human C-terminal BRD4 bromodomain expressed in Escherichia coli BL21(DE3) after 30 mins by luminescence proximity homogeneous assay				J Med Chem 55: 587-96 (2012) Article DOI: 10.1021/jm201283q BindingDB Entry DOI: 10.7270/Q22R3SSS
GlaxoSmithKline R&D Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	77	n/a	n/a	n/a	n/a	n/a	n/a
GlaxoSmithKline R&D Curated by ChEMBL					Assay Description Inhibition of human N-terminal BRD4 bromodomain expressed in Escherichia coli BL21(DE3) after 30 mins by luminescence proximity homogeneous assay				J Med Chem 55: 587-96 (2012) Article DOI: 10.1021/jm201283q BindingDB Entry DOI: 10.7270/Q22R3SSS
GlaxoSmithKline R&D Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	77	n/a	n/a	n/a	n/a	n/a	n/a
University of Oxford Curated by ChEMBL					Assay Description Displacement of H4(1-21)KAc5,8,12,16 peptide from BRD4 isoform 1 bead based amplified luminescent proximity homogeneous assay				J Med Chem 55: 9393-413 (2012) Article DOI: 10.1021/jm300915b BindingDB Entry DOI: 10.7270/Q25B03NC
University of Oxford Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	n/a	49	n/a	n/a	n/a	n/a	n/a
University of Oxford Curated by ChEMBL					Assay Description Binding affinity to BRD4 isoform 1				J Med Chem 55: 9393-413 (2012) Article DOI: 10.1021/jm300915b BindingDB Entry DOI: 10.7270/Q25B03NC
University of Oxford Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	69	n/a	n/a	n/a	n/a	n/a	n/a
Constellation Pharmaceuticals Curated by ChEMBL					Assay Description Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs				ACS Med Chem Lett 4: 835-40 (2013) Article DOI: 10.1021/ml4001485 BindingDB Entry DOI: 10.7270/Q2DV1MB8
Constellation Pharmaceuticals Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	24	n/a	n/a	n/a	n/a	n/a	n/a
Constellation Pharmaceuticals Curated by ChEMBL					Assay Description Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISA				ACS Med Chem Lett 4: 835-40 (2013) Article DOI: 10.1021/ml4001485 BindingDB Entry DOI: 10.7270/Q2DV1MB8
Constellation Pharmaceuticals Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	21	n/a	n/a	n/a	n/a	n/a	n/a
Zhejiang University Curated by ChEMBL					Assay Description Inhibition of human BRD4 BD2 (342 to 460 residues) at 30 uM preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET...				Eur J Med Chem 121: 294-299 (2016) Article DOI: 10.1016/j.ejmech.2016.05.057 BindingDB Entry DOI: 10.7270/Q2K0766Q
Zhejiang University Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	91	n/a	n/a	n/a	n/a	n/a	n/a
Zhejiang University Curated by ChEMBL					Assay Description Inhibition of human His-tagged BRD4 BD1 (49 to 170 residues) using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated for 3...				Eur J Med Chem 121: 294-299 (2016) Article DOI: 10.1016/j.ejmech.2016.05.057 BindingDB Entry DOI: 10.7270/Q2K0766Q
Zhejiang University Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	77	n/a	n/a	n/a	n/a	n/a	n/a
University of Oxford Curated by ChEMBL					Assay Description Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assay				J Med Chem 56: 3217-27 (2013) Article DOI: 10.1021/jm301588r BindingDB Entry DOI: 10.7270/Q2B859GC
University of Oxford Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	n/a	3.60E+3	n/a	n/a	n/a	n/a	n/a
Tensha Therapeutics, Inc. US Patent					Assay Description A BROMOscan binding assay was utilized to test the in vitro binding activity of (S)-Compounds 1, 2, 3, 4, 5 and 7 to the first and second bromodomain...				US Patent US10124009 (2018) BindingDB Entry DOI: 10.7270/Q26975MC
Tensha Therapeutics, Inc. US Patent					More data for this Ligand-Target Pair
Isoform C of Bromodomain-containing protein 4 (Short) (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	n/a	3.80E+3	n/a	n/a	n/a	n/a	n/a
Tensha Therapeutics, Inc. US Patent									US Patent US10124009 (2018) BindingDB Entry DOI: 10.7270/Q26975MC
Tensha Therapeutics, Inc. US Patent					More data for this Ligand-Target Pair
CREB-binding protein (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	>5.00E+3	n/a	n/a	n/a	n/a	n/a	n/a
CELGENE QUANTICEL RESEARCH, INC. US Patent					Assay Description Determination of the IC50 for the CREBBP inhibitors disclosed herein was performed as follows: CREBBP was cloned and expressed in E. Coli as His-tag ...				US Patent US10202360 (2019) BindingDB Entry DOI: 10.7270/Q2R213HG
CELGENE QUANTICEL RESEARCH, INC. US Patent					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 [42-168] (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	<500	n/a	n/a	n/a	n/a	n/a	n/a
CELGENE QUANTICEL RESEARCH, INC. US Patent					Assay Description Inhibition of BRD4 was determined as previously described in U.S. Pat. No. 9,034,900.				US Patent US10202360 (2019) BindingDB Entry DOI: 10.7270/Q2R213HG
CELGENE QUANTICEL RESEARCH, INC. US Patent					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 [44-167] (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB MMDB UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	27.1	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description Inhibitory activity can be determined routinely using known methods and also from commercial vendors offering this service for kinases and bromodomai...				J Med Chem 50: 2647-54 (2007) BindingDB Entry DOI: 10.7270/Q24170D7
Pfizer					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 [349-460] (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	39.1	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description Inhibitory activity can be determined routinely using known methods and also from commercial vendors offering this service for kinases and bromodomai...				J Med Chem 50: 2647-54 (2007) BindingDB Entry DOI: 10.7270/Q24170D7
Pfizer					More data for this Ligand-Target Pair
Phosphatidylinositol 3-kinase regulatory subunit alpha (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	>5.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description Inhibitory activity can be determined routinely using known methods and also from commercial vendors offering this service for kinases and bromodomai...				J Med Chem 50: 2647-54 (2007) BindingDB Entry DOI: 10.7270/Q24170D7
Pfizer					More data for this Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	>5.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description Inhibitory activity can be determined routinely using known methods and also from commercial vendors offering this service for kinases and bromodomai...				J Med Chem 50: 2647-54 (2007) BindingDB Entry DOI: 10.7270/Q24170D7
Pfizer					More data for this Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	US Patent	n/a	n/a	>5.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description Inhibitory activity can be determined routinely using known methods and also from commercial vendors offering this service for kinases and bromodomai...				J Med Chem 50: 2647-54 (2007) BindingDB Entry DOI: 10.7270/Q24170D7
Pfizer					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	70	n/a	n/a	n/a	n/a	n/a	n/a
Chinese Academy of Sciences Curated by ChEMBL					Assay Description Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in da...				Eur J Med Chem 137: 176-195 (2017) Article DOI: 10.1016/j.ejmech.2017.05.049 BindingDB Entry DOI: 10.7270/Q2X069J5
Chinese Academy of Sciences Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	77	n/a	n/a	n/a	n/a	n/a	n/a
University of Oxford Curated by ChEMBL					Assay Description Inhibition of recombinant His-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins follow...				Bioorg Med Chem 26: 2937-2957 (2018) Article DOI: 10.1016/j.bmc.2018.05.003 BindingDB Entry DOI: 10.7270/Q2Z89FXZ
University of Oxford Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE MMDB PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	820	n/a	n/a	n/a	n/a	n/a	n/a
The University of Tokyo Curated by ChEMBL					Assay Description Inhibition of BRD4 in human HL60 cells assessed as reduction in C-myc production after 24 hrs by ELISA				Bioorg Med Chem 25: 3677-3684 (2017) Article DOI: 10.1016/j.bmc.2017.04.043 BindingDB Entry DOI: 10.7270/Q2TB199N
The University of Tokyo Curated by ChEMBL					More data for this Ligand-Target Pair

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Activity Spreadsheet -- ITC Data from BindingDB

Found 1 hit for monomerid = 50365262
Cell (A)	Syringe (B)	Cell Links	Syringe Links	Cell + Syr Links	ΔG° kcal/mole	-TΔS° kcal/mole	ΔH° kcal/mole	log K	pH	Temp °C
Bromodomain-containing protein 4 (BRD4) (Homo sapiens (Human))	BDBM50365262 ((+)-JQ1 \| (S)-JQ1 (1) \| CHEMBL1957266 \| JQ1 \| US10...)	GoogleScholar PDB	CHEBI MMDB PC cid PC sid		-10.1	-3.31	-6.80	7.42	n/a	25
Dana-Farber Cancer Institute		GoogleScholar PDB	CHEBI MMDB PC cid PC sid		Nat Chem Biol 12: 1089-1096 (2016)