ChEMBL ligand: CHEMBL1957266
bromodomain containing 1/Bromodomain-containing protein 1 in Human [ChEMBL: CHEMBL2176774] [GtoPdb: 2724] [UniProtKB: O95696] There should be some charts here, you may need to enable JavaScript!
bromodomain containing 2/Bromodomain-containing protein 2 in Human [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440] There should be some charts here, you may need to enable JavaScript!
bromodomain containing 3/Bromodomain-containing protein 3 in Human [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] There should be some charts here, you may need to enable JavaScript!
bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] There should be some charts here, you may need to enable JavaScript!
bromodomain testis associated/Bromodomain testis-specific protein in Human [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21] bromodomain testis associated in Mouse [GtoPdb: 2729] [UniProtKB: Q91Y44] There should be some charts here, you may need to enable JavaScript!
CREB binding protein/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] There should be some charts here, you may need to enable JavaScript!
E1A binding protein p300/Histone acetyltransferase p300 in Human [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
bromodomain containing 1/Bromodomain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176774] [GtoPdb: 2724] [UniProtKB: O95696]
ChEMBL	Inhibition of recombinant BRD1 (unknown origin) incubated for 120 mins by TR-FRET assay	B	4.35	pIC50	44500	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
ChEMBL	Inhibition of human 6x-His-tagged BRD2 bromodomain 1 expressed in Escherichia coli	B	6.89	pKd	130	nM	Kd	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Binding affinity to BRD2-BD1 by isothermal titration calorimetry	B	6.89	pKd	128.4	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Binding affinity to His-tagged BRD2 bromodomain 2 (unknown origin) by SPR assay	B	6.94	pKd	116	nM	Kd	Bioorg Med Chem (2018) 26: 25-36 [PMID:29170024]
ChEMBL	Binding affinity to BRD2 bromodomain 2 (348 to 455 residues) (unknown origin) by ITC	B	6.95	pKd	112.14	nM	Kd	Bioorg Med Chem (2018) 26: 25-36 [PMID:29170024]
ChEMBL	Binding affinity to recombinant BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.11	pKd	78	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Binding affinity to recombinant BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.28	pKd	52	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Binding affinity to BRD2 D1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry	B	7.47	pKd	34	nM	Kd	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Binding affinity to biotinylated BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	7.83	pKd	14.7	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	8.21	pKd	6.2	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay	B	7.88	pKi	13.2	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 1 (72 to 205 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.88	pKi	13.2	nM	Ki	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Displacement of FAM-labeled ZBA248 from BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay	B	7.9	pKi	12.5	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 2 (349 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.9	pKi	12.5	nM	Ki	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of recombinant BRD2 BD1 (unknown origin) incubated for 120 mins by TR-FRET assay	B	6.41	pIC50	392	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	Inhibition of BRD2 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	6.73	pIC50	185	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Inhibition of recombinant human BRD2 bromodomain 2 (342 to 460 residues) using biotin labeled peptide substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by TR-FRET assay	B	6.77	pIC50	170	nM	IC50	Bioorg Med Chem (2018) 26: 25-36 [PMID:29170024]
ChEMBL	Inhibition of human recombinant His-tagged BRD2 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay	B	6.81	pIC50	155	nM	IC50	J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL	Inhibition of BRD2 D1 (unknown origin) by competitive fluorescence anisotropy assay	B	6.85	pIC50	140	nM	IC50	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Inhibition of BRD2 D2 (unknown origin) by competitive fluorescence anisotropy assay	B	6.92	pIC50	120	nM	IC50	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Inhibition of recombinant BRD2 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay	B	6.95	pIC50	112	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	Inhibition of BRD2 BD1 (unknown origin) after 1 hr by TR-FRET assay	B	7.11	pIC50	78	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Binding affinity BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL	Binding affinity BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.27	pIC50	54	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 2 (349 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.27	pIC50	53.3	nM	IC50	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of BRD2 BD2 (unknown origin) after 1 hr by TR-FRET assay	B	7.28	pIC50	52	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 1 (72 to 205 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.44	pIC50	36.1	nM	IC50	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of BRD2 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	7.49	pIC50	32	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Inhibition of BRD2 BD1 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay	B	7.54	pIC50	29	nM	IC50	Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
ChEMBL	Inhibition of BRD2 (unknown origin) by TR-FRET assay	B	7.72	pIC50	19	nM	IC50	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL	Inhibition of human recombinant His-tagged BRD2 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay	B	7.77	pIC50	17	nM	IC50	J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL	Inhibition of BRD2 BD2 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay	B	8.17	pIC50	6.7	nM	IC50	Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
ChEMBL	Inhibition of human 6x-His-tagged BRD3 bromodomain 2 expressed in Escherichia coli	B	7.09	pKd	82	nM	Kd	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Binding affinity to BRD3-BD2 by isothermal titration calorimetry	B	7.09	pKd	82	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Binding affinity to recombinant BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.09	pKd	81	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Binding affinity to recombinant BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.16	pKd	69	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Binding affinity to BRD3-BD1 by isothermal titration calorimetry	B	7.23	pKd	59.5	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Inhibition of human 6x-His-tagged BRD3 bromodomain 1 expressed in Escherichia coli	B	7.23	pKd	59	nM	Kd	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Binding affinity to biotinylated BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	7.87	pKd	13.6	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to biotinylated BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	7.93	pKd	11.7	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay	B	8.05	pKi	8.9	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 2 (306 to 417residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	8.05	pKi	8.9	nM	Ki	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Displacement of FAM-labeled ZBA248 from BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay	B	8.18	pKi	6.6	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 1 (24 to 144 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	8.18	pKi	6.6	nM	Ki	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of recombinant BRD3 BD1 (unknown origin) incubated for 120 mins by TR-FRET assay	B	6.89	pIC50	129	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	Inhibition of BRD3 D2 (unknown origin) by competitive fluorescence anisotropy assay	B	7.02	pIC50	96	nM	IC50	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Inhibition of BRD3 BD1 (unknown origin) after 1 hr by TR-FRET assay	B	7.09	pIC50	81	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Inhibition of BRD3 D1 (unknown origin) by competitive fluorescence anisotropy assay	B	7.1	pIC50	<80	nM	IC50	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Binding affinity BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.1	pIC50	79	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL	Inhibition of BRD3 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	7.12	pIC50	76	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Binding affinity BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.14	pIC50	72	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL	Inhibition of BRD3 BD2 (unknown origin) after 1 hr by TR-FRET assay	B	7.16	pIC50	69	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Inhibition of human recombinant His-tagged BRD3 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay	B	7.19	pIC50	64	nM	IC50	J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL	Inhibition of BRD3 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	7.21	pIC50	61	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 2 (306 to 417residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.25	pIC50	56.7	nM	IC50	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of recombinant BRD3 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay	B	7.28	pIC50	53	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 1 (24 to 144 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.41	pIC50	39.1	nM	IC50	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of human recombinant His-tagged BRD3 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay	B	7.41	pIC50	39	nM	IC50	J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL	Inhibition of BRD3 (unknown origin) by TR-FRET assay	B	7.64	pIC50	23	nM	IC50	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL	Binding affinity to BRD4 C-terminal bromodomain 2 H437D mutant (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence polarization assay	B	6.7	pKd	200	nM	Kd	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Binding affinity to BRD4 D2 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry	B	6.89	pKd	130	nM	Kd	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Binding affinity to BRD4 C-terminal bromodomain 2 (unknown origin) expressed in Escherichia coli Bl21(DE3)	B	6.92	pKd	120	nM	Kd	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Binding affinity to human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by isothermal titration calorimetry-based assay	B	7	pKd	100	nM	Kd	J Med Chem (2018) 61: 504-513 [PMID:28595007]
ChEMBL	Binding affinity to recombinant BRD4 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.04	pKd	92	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Binding affinity to human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry method	B	7.04	pKd	92	nM	Kd	ACS Med Chem Lett (2018) 9: 262-267 [PMID:29541371]
ChEMBL	Binding affinity to BRD4-BD2 by isothermal titration calorimetry	B	7.05	pKd	90.1	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coli	B	7.05	pKd	90	nM	Kd	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis	B	7.15	pKd	71	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to recombinant BRD4 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	B	7.21	pKd	62	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Binding affinity to BRD4 by isothermal titration calorimetry	B	7.22	pKd	60	nM	Kd	Bioorg Med Chem (2012) 20: 1878-1886 [PMID:22137933]
GtoPdb	Displacement binding constant to recombinant BRD4-BD1 protein.	-	7.3	pKd	50	nM	Kd	Nature (2010) 468: 1067-73 [PMID:20871596]
ChEMBL	Binding affinity to BRD4 bromodomain 1 (unknown origin) by isothermal titration calorimetry	B	7.3	pKd	50	nM	Kd	Medchemcomm (2018) 9: 1779-1802 [PMID:30542529]
ChEMBL	Binding affinity to BRD4-BD1 by isothermal titration calorimetry	B	7.31	pKd	49	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Binding affinity to BRD4 isoform 1	B	7.31	pKd	49	nM	Kd	J Med Chem (2012) 55: 9393-9413 [PMID:22924434]
ChEMBL	Inhibition of human 6x-His-tagged BRD4 bromodomain 1 expressed in Escherichia coli	B	7.31	pKd	49	nM	Kd	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Binding affinity to BRD4 (unknown origin)	B	7.31	pKd	49	nM	Kd	Bioorg Med Chem Lett (2020) 30: 126958-126958 [PMID:32019712]
ChEMBL	Binding affinity to BRD4-BD1 by isothermal titration calorimetry	B	7.31	pKd	49	nM	Kd	Bioorg Med Chem (2012) 20: 1878-1886 [PMID:22137933]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay	B	7.46	pKd	35	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry	B	7.47	pKd	34	nM	Kd	J Med Chem (2016) 59: 1565-1579 [PMID:26731490]
ChEMBL	Binding affinity to BRD4 D1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry	B	7.72	pKd	19	nM	Kd	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Binding affinity to human BRD4 BD1 (N44 to E168 aa residues) by bromoKdELECT Discover assay	B	7.89	pKd	13	nM	Kd	J Med Chem (2020) 63: 15603-15620 [PMID:33275431]
ChEMBL	Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	7.89	pKd	12.8	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay	B	8.09	pKd	8.2	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	8.17	pKd	6.7	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to human N-terminal His6-tagged BRD4 BD1-BD2 (K57 to K550 residues) after 1 hr using alexa-647 conjugated probe by TR-FRET assay	B	7.11	pKi	77	nM	Ki	J Med Chem (2017) 60: 8369-8384 [PMID:28949521]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.83	pKi	14.9	nM	Ki	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay	B	7.83	pKi	14.9	nM	Ki	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay	B	7.92	pKi	12	nM	Ki	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.92	pKi	12	nM	Ki	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	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 fluorescence polarization assay	B	7.97	pKi	10.7	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	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 fluorescence polarization assay	B	8.12	pKi	7.6	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assay	B	8.28	pKi	5.3	nM	Ki	J Med Chem (2018) 61: 6685-6704 [PMID:30019901]
ChEMBL	Inhibition of BRD4 (unknown origin) by biotinylated-JQ1 based AlphaScreen BRD binding assay	B	4.09	pIC50	81500	nM	IC50	J Med Chem (2014) 57: 9019-9027 [PMID:25314271]
ChEMBL	Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG56 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis	B	5.79	pIC50	1630	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced IL-8 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis	B	5.82	pIC50	1510	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced grobeta RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis	B	5.83	pIC50	1490	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis	B	5.86	pIC50	1380	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible IL-6 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis	B	5.99	pIC50	1020	nM	IC50	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible CIG5 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis	B	6.02	pIC50	950	nM	IC50	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Inhibition of recombinant human N-terminal His-tagged BRD4 bromodomain 1 (49 to 170 residues) expressed in Escherichia coli using biotinylated peptide containing acetylated lysine as substrate pretreated for 15 mins followed by substrate addition after 1 hr by TR-FRET assay	B	6.09	pIC50	820	nM	IC50	Bioorg Med Chem (2017) 25: 3677-3684 [PMID:28549889]
ChEMBL	Displacement of Fl-JQ1 from BRD4 C-terminal bromodomain 2 H437D mutant (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence polarization assay	B	6.23	pIC50	590	nM	IC50	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Inhibition of BRD4 bromodomain 2 (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence anisotropy	B	6.31	pIC50	490	nM	IC50	J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL	Inhibition of fluorescent-tagged ligand from nanoLuc fused full length BRD4 (unknown origin) expressed in 293T cells by luciferase reporter gene based BRET engagement assay	B	6.52	pIC50	300	nM	IC50	J Med Chem (2018) 61: 9301-9315 [PMID:30289257]
ChEMBL	Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human BRD4 bromodomain 1 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured after 1 hr under dark condition by TR-FRET assay	B	6.7	pIC50	199	nM	IC50	J Med Chem (2020) 63: 7186-7210 [PMID:32453591]
ChEMBL	Inhibition of biotinylated H4 K5,8,12,16Ac peptide binding to GST-tagged BRD4 bromodomain1 (unknown origin) measured after 60 mins by AlphaScreen assay	B	6.77	pIC50	170	nM	IC50	Bioorg Med Chem (2019) 27: 1871-1881 [PMID:30926312]
ChEMBL	Inhibition of BRD4 (unknown origin) by TR-FRET assay	B	6.84	pIC50	144	nM	IC50	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL	Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human BRD4 bromodomain 2 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured after 1 hr under dark condition by TR-FRET assay	B	6.9	pIC50	126	nM	IC50	J Med Chem (2020) 63: 7186-7210 [PMID:32453591]
ChEMBL	Displacement of FITC-conjugated JQ1 from BRD4 BD2 (unknown origin) expressed in Escherichia coli BL21-DE3 rosetta cells incubated for 15 mins by competitive fluorescence polarization assay	B	6.91	pIC50	123	nM	IC50	J Med Chem (2021) 64: 11637-11650 [PMID:34279939]
ChEMBL	Inhibition of His6-tagged human BRD4 bromodomain-1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) using biotinylated-H4KAc4 as substrate by AlphaScreen assay	B	6.92	pIC50	120	nM	IC50	Eur J Med Chem (2018) 152: 542-559 [PMID:29758518]
ChEMBL	Inhibition of human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells using H-SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK-Biotin-OH as substrate after 2.5 hrs by AlphaScreen assay	B	6.92	pIC50	120	nM	IC50	ACS Med Chem Lett (2018) 9: 262-267 [PMID:29541371]
ChEMBL	Inhibition of human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells using biotin-H4KAc4 as substrate incubated for 2 hrs by alphascreen assay	B	6.92	pIC50	120	nM	IC50	J Med Chem (2016) 59: 1565-1579 [PMID:26731490]
ChEMBL	Inhibition of BRD4 D2 (unknown origin) by competitive fluorescence anisotropy assay	B	7.03	pIC50	94	nM	IC50	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Binding affinity recombinant human BRD4 BD1 (42 to 168 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr by TR-FRET assay	B	7.04	pIC50	92	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL	Inhibition of BRD4 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	7.04	pIC50	92	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Inhibition of BRD4 D1 (unknown origin) by competitive fluorescence anisotropy assay	B	7.04	pIC50	<92	nM	IC50	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Inhibition of BRD4 BD1 (unknown origin) after 1 hr by TR-FRET assay	B	7.04	pIC50	92	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	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 30 mins followed by substrate addition measured after 30 mins by TR-FRET assay	B	7.04	pIC50	91	nM	IC50	Eur J Med Chem (2016) 121: 294-299 [PMID:27266999]
ChEMBL	Inhibition of BRD4 bromodomain 1/2 (unknown origin) by alphascreen assay	B	7.05	pIC50	90	nM	IC50	Bioorg Med Chem Lett (2019) 29: 126577-126577 [PMID:31421967]
ChEMBL	Inhibition of human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 by bromodomain alphascreen peptide displacement assay	B	7.05	pIC50	90	nM	IC50	Bioorg Med Chem Lett (2016) 26: 2931-2935 [PMID:27142751]
ChEMBL	Inhibition of recombinant BRD4 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay	B	7.05	pIC50	89	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	Inhibition of BRD4-BD1 (44 to 168 residues) (unknown origin) using histone H4 peptide as substrate preincubated for 15 mins followed by addition of substrate measured after 60 mins by AlphaScreen assay	B	7.06	pIC50	88	nM	IC50	Bioorg Med Chem (2017) 25: 2482-2490 [PMID:28314513]
ChEMBL	Inhibition of BRD4-BD2 (333 to 460 residues) (unknown origin) using histone H4 peptide as substrate preincubated for 15 mins followed by addition of substrate measured after 60 mins by AlphaScreen assay	B	7.06	pIC50	87	nM	IC50	Bioorg Med Chem (2017) 25: 2482-2490 [PMID:28314513]
ChEMBL	Inhibition of BRD4 bromodomain1 (unknown origin) using peptide H4 as substrate incubated for 15 mins followed by substrate addition and measured after 1 hr by alphascreen assay	B	7.06	pIC50	87	nM	IC50	ACS Med Chem Lett (2019) 10: 1680-1685 [PMID:31857846]
ChEMBL	Inhibition of BRD4 in human HL60 cells assessed as reduction in C-myc production after 24 hrs by ELISA	B	7.07	pIC50	86	nM	IC50	Bioorg Med Chem (2017) 25: 3677-3684 [PMID:28549889]
ChEMBL	Inhibition of BRD4 BD1/BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	7.08	pIC50	84	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Inhibition of recombinant BRD4 (unknown origin) incubated for 120 mins by TR-FRET assay	B	7.08	pIC50	83	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	Inhibition of biotinylated H4 K5,8,12,16Ac peptide binding to GST-tagged BRD4 bromodomain2 (unknown origin) measured after 60 mins by AlphaScreen assay	B	7.1	pIC50	80	nM	IC50	Bioorg Med Chem (2019) 27: 1871-1881 [PMID:30926312]
ChEMBL	Inhibition of BRD4 bromodomain2 (unknown origin) using peptide H4 as substrate incubated for 15 mins followed by substrate addition and measured after 1 hr by alphascreen assay	B	7.1	pIC50	79	nM	IC50	ACS Med Chem Lett (2019) 10: 1680-1685 [PMID:31857846]
ChEMBL	Inhibition of BRD4 bromodomain-1 (unknown origin) by AlphaScreen assay	B	7.11	pIC50	77	nM	IC50	Eur J Med Chem (2018) 152: 542-559 [PMID:29758518]
ChEMBL	Binding affinity to first bromodomain of BRD4	B	7.11	pIC50	77	nM	IC50	ACS Med Chem Lett (2012) 3: 691-694 [PMID:24900532]
ChEMBL	Displacement of H4(1-21)KAc5,8,12,16 peptide from BRD4 isoform 1 bead based amplified luminescent proximity homogeneous assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2012) 55: 9393-9413 [PMID:22924434]
ChEMBL	Inhibition of human N-terminal BRD4 bromodomain expressed in Escherichia coli BL21(DE3) after 30 mins by luminescence proximity homogeneous assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2012) 55: 587-596 [PMID:22136469]
ChEMBL	Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2013) 56: 3217-3227 [PMID:23517011]
ChEMBL	Inhibition of BRD4 bromodomain 1 (unknown origin)-acetylated histone H4 interaction by luminescence proximity homogeneous assay	B	7.11	pIC50	77	nM	IC50	Medchemcomm (2012) 3: 123-134
ChEMBL	Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using biotin-H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by alphascreen assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2016) 59: 1565-1579 [PMID:26731490]
ChEMBL	Inhibition of BRD4(1) (unknown origin)	B	7.11	pIC50	77	nM	IC50	Bioorg Med Chem Lett (2016) 26: 2931-2935 [PMID:27142751]
ChEMBL	Inhibition of recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac peptide substrate addition after 30 mins by alphascreen assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2017) 60: 4533-4558 [PMID:28195723]
ChEMBL	Inhibition of recombinant His-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac substrate addition measured after 30 mins by AlphaScreen assay	B	7.11	pIC50	77	nM	IC50	Bioorg Med Chem (2018) 26: 2937-2957 [PMID:29776834]
ChEMBL	Displacement of acetylated histone peptide from BRD4-BD1 by luminescence proximity homogenous assay	B	7.11	pIC50	77	nM	IC50	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Inhibition of BRD4 bromodomain 1 (unknown origin) by alpha-screen method	B	7.11	pIC50	77	nM	IC50	Medchemcomm (2018) 9: 1779-1802 [PMID:30542529]
ChEMBL	Inhibition of HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH binding to recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21 (DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH addition and measured after 30 mins by Alphascreen assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2020) 63: 3956-3975 [PMID:32208600]
ChEMBL	Inhibition of BRD4 (unknown origin)	B	7.11	pIC50	77	nM	IC50	Bioorg Med Chem Lett (2020) 30: 126958-126958 [PMID:32019712]
ChEMBL	Inhibition of human His-tagged BRD4 BD1 domain using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay	B	7.11	pIC50	77	nM	IC50	Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
ChEMBL	Inhibition of HYSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH binding to recombinant human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells measured after 2 hrs by Alphascreen assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2018) 61: 3037-3058 [PMID:29566488]
ChEMBL	Binding affinity to BRD4 BD1 (unknown origin) by fluorescence anisotropy method	B	7.11	pIC50	77	nM	IC50	J Med Chem (2021) 64: 10497-10511 [PMID:34236185]
ChEMBL	Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human N-terminal GST-tagged BRD4 bromodomain 1 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured after 1 hr under dark condition by TR-FRET assay	B	7.13	pIC50	74	nM	IC50	Bioorg Med Chem (2020) 28: 115601-115601 [PMID:32631570]
ChEMBL	Binding affinity to BRD4 BD2 (unknown origin) by fluorescence anisotropy method	B	7.14	pIC50	72	nM	IC50	J Med Chem (2021) 64: 10497-10511 [PMID:34236185]
ChEMBL	Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in dark for 4 hrs by fluorescence anisotropy assay	B	7.15	pIC50	70	nM	IC50	Eur J Med Chem (2017) 137: 176-195 [PMID:28586718]
ChEMBL	Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs	B	7.16	pIC50	69	nM	IC50	ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758]
ChEMBL	Inhibition of human recombinant His-tagged BRD4 BD2 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay	B	7.16	pIC50	69	nM	IC50	J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL	Binding affinity to recombinant human N-terminal His-tagged BRD4 BD1 (44 to 170 residues) expressed in Escherichia coli using H4K5AcK8Ac as substrate measured after 30 mins by AlphaScreen assay	B	7.2	pIC50	62.57	nM	IC50	Bioorg Med Chem (2020) 28: 115181-115181 [PMID:31767403]
ChEMBL	Inhibition of BRD4 BD2 (unknown origin) after 1 hr by TR-FRET assay	B	7.21	pIC50	62	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Binding affinity human BRD4 BD2 incubated for 1 hr by TR-FRET assay	B	7.21	pIC50	62	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL	Inhibition of N-terminal His-tagged BRD4 (BD1) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay	B	7.22	pIC50	60	nM	IC50	J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
ChEMBL	Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR method	B	7.22	pIC50	60	nM	IC50	Bioorg Med Chem Lett (2018) 28: 1811-1816 [PMID:29657099]
ChEMBL	Inhibition of BRD4(1) (unknown origin) incubated for 4 hrs by (+)-JQ1 fluorescent ligand based fluorescence anisotrophy	B	7.24	pIC50	58	nM	IC50	J Med Chem (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL	Inhibition of BRD4 D1 (unknown origin) by alphascreen assay	B	7.29	pIC50	51	nM	IC50	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Displacement of (+)-JQ1 from 6H-Thr BRD4 Y97A mutant BD2 (unknown origin) after 30 mins by TR-FRET assay	B	7.3	pIC50	50.12	nM	IC50	J Med Chem (2018) 61: 4317-4334 [PMID:29656650]
ChEMBL	Inhibition of N-terminal His-tagged BRD4 (BD1/BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay	B	7.3	pIC50	50	nM	IC50	J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
ChEMBL	Displacement of FITC-conjugated JQ1 from wildtype BRD4 BD1 (unknown origin) expressed in Escherichia coli BL21-DE3 rosetta cells incubated for 15 mins by competitive fluorescence polarization assay	B	7.31	pIC50	49	nM	IC50	J Med Chem (2021) 64: 11637-11650 [PMID:34279939]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.33	pIC50	46.7	nM	IC50	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay	B	7.33	pIC50	46.7	nM	IC50	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL	Inhibition of BRD4 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	7.36	pIC50	44	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Displacement of tetra-acetylated histone H4 peptide (1-21) from recombinant human N-terminal His-tagged BRD4 BD1 (44 to 170 residues) expressed in Escherichia coli incubated for 30 mins followed by further incubation with tetra-acetylated histone H4 peptide (1-21) for 30 mins by Alphascreen assay	B	7.37	pIC50	42.24	nM	IC50	J Med Chem (2019) 62: 11080-11107 [PMID:31789032]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay	B	7.37	pIC50	42.2	nM	IC50	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL	Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay	B	7.37	pIC50	42.2	nM	IC50	J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL	Inhibition of BRD4-BD1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 1 hr	B	7.38	pIC50	42	nM	IC50	Bioorg Med Chem (2021) 39: 116133-116133 [PMID:33862375]
ChEMBL	Inhibition of BRD4 bromodomain1 (unknown origin) using peptide histone H4 (SGRGACKGGACKGLGAC-KGGAACKRHGSGSK-biotin) as substrate incubated for 15 mins followed by substrate addition measured after 1 hr by alphascreen assay	B	7.38	pIC50	42	nM	IC50	ACS Med Chem Lett (2020) 11: 2174-2181 [PMID:33214826]
ChEMBL	Inhibition of N-terminal His-tagged BRD4 (BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay	B	7.4	pIC50	40	nM	IC50	J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
ChEMBL	Inhibition of recombinant human His-tagged BRD4 bromodomain 1/2 (2 to 1362 residues) expressed in s9f insect cells using biotinylated H4(1 to 21)K5/8/12/16Ac peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by Alpha screen assay	B	7.4	pIC50	40	nM	IC50	Eur J Med Chem (2019) 179: 502-514 [PMID:31276895]
ChEMBL	Displacement of (+)-JQ1 from 6H-Thr BRD4 Y390A mutant BD1 (unknown origin) after 30 mins by TR-FRET assay	B	7.4	pIC50	39.81	nM	IC50	J Med Chem (2018) 61: 4317-4334 [PMID:29656650]
ChEMBL	Binding affinity to recombinant human N-terminal His-tagged BRD4 BD2 (349 to 460 residues) expressed in Escherichia coli measured after 30 mins by AlphaScreen assay	B	7.41	pIC50	39.09	nM	IC50	Bioorg Med Chem (2020) 28: 115181-115181 [PMID:31767403]
ChEMBL	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 fluorescence polarization assay	B	7.45	pIC50	35.7	nM	IC50	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Inhibition of BRD4 bromodomain 2 (unknown origin)-acetylated histone H4 interaction by luminescence proximity homogeneous assay	B	7.48	pIC50	33	nM	IC50	Medchemcomm (2012) 3: 123-134
ChEMBL	Inhibition of BRD4 (unknown origin)	B	7.48	pIC50	33	nM	IC50	Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013]
ChEMBL	Inhibition of recombinant human His6-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH peptide substrate addition after 30 mins by alphascreen assay	B	7.48	pIC50	33	nM	IC50	J Med Chem (2017) 60: 4533-4558 [PMID:28195723]
ChEMBL	Inhibition of human recombinant N-terminal 6his-tagged BRD4 expressed in Escherichia coli BL21(DE3) using H4 peptide as substrate by alphascreen assay	B	7.48	pIC50	33	nM	IC50	Bioorg Med Chem Lett (2019) 29: 126577-126577 [PMID:31421967]
ChEMBL	Inhibition of human C-terminal BRD4 bromodomain expressed in Escherichia coli BL21(DE3) after 30 mins by luminescence proximity homogeneous assay	B	7.48	pIC50	33	nM	IC50	J Med Chem (2012) 55: 587-596 [PMID:22136469]
ChEMBL	Inhibition of human His-tagged BRD4 BD2 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay	B	7.48	pIC50	33	nM	IC50	Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
ChEMBL	Displacement of acetylated histone peptide from BRD4-BD2 by luminescence proximity homogenous assay	B	7.48	pIC50	33	nM	IC50	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Inhibition of BRD4-BD1 (unknown origin) incubated for 1 hr by AlphaScreen biotin-JQ1 competition assay	B	7.49	pIC50	32	nM	IC50	J Med Chem (2018) 61: 7785-7795 [PMID:30125504]
ChEMBL	Inhibition of recombinant BRD4 BD1 (unknown origin) incubated for 120 mins by TR-FRET assay	B	7.54	pIC50	29	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	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 fluorescence polarization assay	B	7.54	pIC50	28.7	nM	IC50	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Displacement of FITC-JQ1 from His6-tagged BRD4 bromodomain-1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 4 hrs by fluorescence anisotropy method	B	7.55	pIC50	28.5	nM	IC50	Eur J Med Chem (2018) 150: 156-175 [PMID:29525435]
ChEMBL	Displacement of 5-FITC labelled (+)-JQ1 from His6-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) )-codon plus-RIL cells incubated for 4 hrs in dark condition by fluorescence anisotropy binding assay	B	7.55	pIC50	28.5	nM	IC50	J Med Chem (2019) 62: 8642-8663 [PMID:31490070]
ChEMBL	Inhibition of recombinant human GST-tagged BRD4 BD1 (44 to 168 residues) expressed in Escherichia coli incubated for 60 mins by alphascreen assay	B	7.55	pIC50	27.9	nM	IC50	Bioorg Med Chem (2020) 28: 115228-115228 [PMID:31813613]
ChEMBL	Displacement of tetra-acetylated histone H4 peptide (1-21) from recombinant human N-terminal His-tagged BRD4 BD2 (349 to 460 residues) expressed in Escherichia coli incubated for 30 mins followed by further incubation with tetra-acetylated histone H4 peptide (1-21) for 30 mins by Alphascreen assay	B	7.61	pIC50	24.71	nM	IC50	J Med Chem (2019) 62: 11080-11107 [PMID:31789032]
ChEMBL	Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged BRD4 bromodomain1 by alphascreen assay	B	7.62	pIC50	24	nM	IC50	J Med Chem (2016) 59: 1271-1298 [PMID:26572217]
ChEMBL	Inhibition of His/FLAG-tagged BRD4 BD1 (unknown origin) using histone H4-TetraAcetylated-biotin peptide as substrate incubated for 20 mins by AlphaLISA assay	B	7.62	pIC50	24	nM	IC50	ACS Med Chem Lett (2016) 7: 145-150 [PMID:26985289]
ChEMBL	Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISA	B	7.62	pIC50	24	nM	IC50	ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758]
ChEMBL	Inhibition of human recombinant His-tagged BRD4 BD1 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay	B	7.66	pIC50	22	nM	IC50	J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL	Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assay	B	7.66	pIC50	22	nM	IC50	J Med Chem (2018) 61: 6685-6704 [PMID:30019901]
ChEMBL	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 assay	B	7.68	pIC50	21	nM	IC50	Eur J Med Chem (2016) 121: 294-299 [PMID:27266999]
ChEMBL	Alpha Assay: BRD4(1): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 100 mM NaCl, 0.1% BSA, pH 7.4 supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature prior to addition to plates. A 24-point 1:2 serial dilution of the ligands was prepared over the range of 150-0 μM and 4 μl transferred to low-volume 384-well plates (ProxiPlate™-384 Plus, PerkinElmer, USA), followed by 4 μl of HIS-tagged protein (BRD4/1, 250 nM, BRD4/2 and CREBBP, 2000 nM). Plates were sealed and incubated at room temperature for 30 minutes, before the addition of 4 μl of biotinylated peptide at equimolar concentration to the protein [peptide for BRD4(1) & BRD4(2): H4K5acK8acK12acK16ac, H-SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH (SEQ ID NO: 5); peptide for CREBBP: H3K36ac, Biotin-KSAPATGGVK(Ac)KPHRYRPGT-OH (SEQ ID NO: 6) (Cambridge Research Biochemicals, UK)]. Plates were sealed and incubated for a further 30 minutes, before the addition of 4 μl of streptavidin-coated donor beads (25 μg/ml) and 4 μl nickel chelate acceptor beads (25 μg/ml) under low light conditions. Plates were foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader (BMG Labtech, Germany) using an AlphaScreen 680 excitation/570 emission filter set. IC50 values were calculated in Prism 5 (GraphPad Software, USA) after normalization against corresponding DMSO controls and are given as the final concentration of compound in the 20 μl reaction volume.	B	7.74	pIC50	18	nM	IC50	US-9320741-B2. Compositions and methods for treating neoplasia, inflammatory disease and other disorders (2016)
ChEMBL	Alpha Assay: BRD4(2): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 100 mM NaCl, 0.1% BSA, pH 7.4 supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature prior to addition to plates. A 24-point 1:2 serial dilution of the ligands was prepared over the range of 150-0 μM and 4 μl transferred to low-volume 384-well plates (ProxiPlate™-384 Plus, PerkinElmer, USA), followed by 4 μl of HIS-tagged protein (BRD4/1, 250 nM, BRD4/2 and CREBBP, 2000 nM). Plates were sealed and incubated at room temperature for 30 minutes, before the addition of 4 μl of biotinylated peptide at equimolar concentration to the protein [peptide for BRD4(1) & BRD4(2): H4K5acK8acK12acK16ac, H-SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH (SEQ ID NO: 5); peptide for CREBBP: H3K36ac, Biotin-KSAPATGGVK(Ac)KPHRYRPGT-OH (SEQ ID NO: 6) (Cambridge Research Biochemicals, UK)]. Plates were sealed and incubated for a further 30 minutes, before the addition of 4 μl of streptavidin-coated donor beads (25 μg/ml) and 4 μl nickel chelate acceptor beads (25 μg/ml) under low light conditions. Plates were foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader (BMG Labtech, Germany) using an AlphaScreen 680 excitation/570 emission filter set. IC50 values were calculated in Prism 5 (GraphPad Software, USA) after normalization against corresponding DMSO controls and are given as the final concentration of compound in the 20 μl reaction volume.	B	7.85	pIC50	14	nM	IC50	US-9320741-B2. Compositions and methods for treating neoplasia, inflammatory disease and other disorders (2016)
ChEMBL	Inhibition of BRD4 BD1 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay	B	7.92	pIC50	12	nM	IC50	Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
ChEMBL	Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assay	B	8.1	pIC50	8	nM	IC50	Bioorg Med Chem (2015) 23: 953-959 [PMID:25678016]
ChEMBL	Inhibition of BRD4 BD2 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay	B	8.41	pIC50	3.9	nM	IC50	Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
ChEMBL	Inhibition of BRD4 in human H1299 cells assessed as decrease in HPV LCR-E2-EP400-mediated transcriptional repression after 24 hrs by Bright-Glo luciferase reporter gene assay	B	6.82	pEC50	153	nM	EC50	J Med Chem (2017) 60: 8369-8384 [PMID:28949521]
ChEMBL	Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay	B	6.84	pEC50	144	nM	EC50	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL	Inhibition of BRD4 in human H1229 cells transfected with HPV-E2 assessed as transrepression of HPV-long control region by luciferase reporter assay	B	7.19	pEC50	64	nM	EC50	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by MST assay	B	6.59	pKd	260	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to recombinant BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	B	6.66	pKd	217	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Binding affinity to BRDT-BD1 by isothermal titration calorimetry	B	6.72	pKd	190.1	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by ITC analysis	B	6.73	pKd	188	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to recombinant BRDT BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	B	6.74	pKd	183	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assay	B	7.66	pKd	22	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Inhibition of recombinant BRDT BD1 (unknown origin) incubated for 120 mins by TR-FRET assay	B	6.23	pIC50	588	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	Inhibition of recombinant BRDT BD2 (unknown origin) incubated for 120 mins by TR-FRET assay	B	6.49	pIC50	325	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL	Binding affinity BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	B	6.65	pIC50	224	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL	Inhibition of BRDT BD2 (unknown origin) after 1 hr by TR-FRET assay	B	6.66	pIC50	217	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Inhibition of BRDT BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	6.68	pIC50	207	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Inhibition of BRDT BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay	B	6.73	pIC50	185	nM	IC50	J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL	Inhibition of BRDT BD1 (unknown origin) after 1 hr by TR-FRET assay	B	6.74	pIC50	183	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Binding affinity BRDT BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	B	6.75	pIC50	178	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL	Inhibition of human recombinant His-tagged BRDT BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay	B	6.87	pIC50	134	nM	IC50	J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL	Inhibition of BRDT D1 (unknown origin) by competitive fluorescence anisotropy assay	B	6.92	pIC50	120	nM	IC50	J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL	Inhibition of BRDT-BD1 (unknown origin) incubated for 1 hr by AlphaScreen biotin-JQ1 competition assay	B	6.99	pIC50	103	nM	IC50	J Med Chem (2018) 61: 7785-7795 [PMID:30125504]
GtoPdb	Inhibition of H4Kac4 binding to hBRDT-BD1	-	7.96	pIC50	11	nM	IC50	Cell (2012) 150: 673-84 [PMID:22901802]
bromodomain testis associated in Mouse [GtoPdb: 2729] [UniProtKB: Q91Y44]
GtoPdb	Inhibition of H4Kac4 binding to mBRDT-BD1	-	8	pIC50	10	nM	IC50	Cell (2012) 150: 673-84 [PMID:22901802]
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
ChEMBL	Binding affinity to recombinant CBP (unknown origin) incubated for 1 hr by TR-FRET assay	B	5.02	pKd	9600	nM	Kd	J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL	Displacement of acetylated histone peptide from CREBBP by luminescence proximity homogenous assay	B	5	pIC50	>10000	nM	IC50	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Inhibition of CBP (unknown origin) after 1 hr by TR-FRET assay	B	5.02	pIC50	9600	nM	IC50	Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL	Binding affinity CBP (unknown origin) incubated for 1 hr by TR-FRET assay	B	5.02	pIC50	9546	nM	IC50	J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
ChEMBL	Inhibition of P300 (unknown orign) using acetyl-CoA as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by microplate reader analysis	B	4.71	pIC50	19400	nM	IC50	J Med Chem (2021) 64: 17413-17435 [PMID:34813314]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]