ChEMBL ligand: CHEMBL1232461 (Bet inhibitor gsk525762, GSK-525762, GSK525762, GSK-525762A, GSK525762A, I-BET 762, Molibresib)
ATPase family AAA domain containing 2/ATPase family AAA domain-containing protein 2 in Human [ChEMBL: CHEMBL2150837] [GtoPdb: 2719] [UniProtKB: Q6PL18] 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] 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
ATPase family AAA domain containing 2/ATPase family AAA domain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150837] [GtoPdb: 2719] [UniProtKB: Q6PL18]
ChEMBL	Binding affinity to biotinylated ATAD2A (981 to 1108 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	5	pKd	>10000	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
ChEMBL	Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry	B	6.64	pKd	230	nM	Kd	J Med Chem (2016) 59: 1492-1500 [PMID:26367539]
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	6.8	pKd	159	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to human partial length BRD2-BD1 (K71 to N194 residues) expressed in bacterial expression system by BROMOscan method	B	6.96	pKd	110	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Binding affinity to His6-tagged BRD2 expressed in Escherichia coli by isothermal colorimetric analysis	B	7	pKd	101	nM	Kd	J Med Chem (2012) 55: 587-596 [PMID:22136469]
ChEMBL	Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry	B	7	pKd	100	nM	Kd	J Med Chem (2016) 59: 1492-1500 [PMID:26367539]
ChEMBL	Binding affinity to BRD2-BD1,2 by isothermal titration calorimetry	B	7.21	pKd	61.3	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
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	7.34	pKd	45.4	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to human partial length BRD2-BD2 (E348 to D455 residues) expressed in bacterial expression system by BROMOscan method	B	7.6	pKd	25	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Binding affinity to human recombinant BRD2 BD1 (72 to 205 residues) by fluorescence polarization assay	B	6.82	pKi	150	nM	Ki	Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688]
ChEMBL	Binding affinity to human recombinant BRD2 BD2 (349 to 460 residues) by fluorescence polarization assay	B	7.13	pKi	74	nM	Ki	Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688]
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	7.25	pKi	56.8	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	7.31	pKi	49.2	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Inhibition of His6-tagged BRD2 expressed in Escherichia coli after 60 mins by fluorescence anisotropy assay	B	6.09	pIC50	810	nM	IC50	J Med Chem (2012) 55: 587-596 [PMID:22136469]
ChEMBL	Inhibition of BRD2 (unknown origin) by fluorescence anisotrophy	B	6.1	pIC50	790	nM	IC50	J Med Chem (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL	Inhibition of His6-tagged BRD2 expressed in Escherichia coli assessed as inhibition of binding to SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHGSGSK-biotin after 1 hr by TR-FRET assay	B	6.82	pIC50	150	nM	IC50	J Med Chem (2012) 55: 587-596 [PMID:22136469]
ChEMBL	Displacement of acetylated histone peptide from BRD2-BD1,2 by FRET assay	B	7.49	pIC50	32.5	nM	IC50	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Displacement of tetra-acetylated H4 peptide from human Brd2 bromodomain BD12 after 1 hr by FRET analysis	B	7.49	pIC50	32.5	nM	IC50	J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
GtoPdb	Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD2.	-	7.49	pIC50	32.5	nM	IC50	J Med Chem (2011) 54: 3827-38 [PMID:21568322]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
ChEMBL	Binding affinity to His6-tagged BRD3 expressed in Escherichia coli by isothermal colorimetric analysis	B	7.05	pKd	89	nM	Kd	J Med Chem (2012) 55: 587-596 [PMID:22136469]
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	7.22	pKd	60.7	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to BRD3-BD1,2 by isothermal titration calorimetry	B	7.3	pKd	50.5	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
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	7.39	pKd	40.7	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to human partial length BRD3-BD2 (G306 to P416 residues) expressed in bacterial expression system by BROMOscan method	B	7.64	pKd	23	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Binding affinity to human partial length BRD3-BD1 (P24 to E144 residues) expressed in bacterial expression system by BROMOscan method	B	7.66	pKd	22	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Binding affinity to human recombinant BRD3 BD2 (306 to 417 residues) by fluorescence polarization assay	B	7.03	pKi	94	nM	Ki	Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688]
ChEMBL	Binding affinity to human recombinant BRD3 BD1 (24 to 144 residues) by fluorescence polarization assay	B	7.16	pKi	68.5	nM	Ki	Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688]
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	7.27	pKi	53.9	nM	Ki	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	7.52	pKi	30.3	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Inhibition of BRD3 (unknown origin) by fluorescence anisotrophy	B	6.4	pIC50	400	nM	IC50	J Med Chem (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL	Inhibition of His6-tagged BRD3 expressed in Escherichia coli after 60 mins by fluorescence anisotropy assay	B	6.41	pIC50	390	nM	IC50	J Med Chem (2012) 55: 587-596 [PMID:22136469]
ChEMBL	Inhibition of His6-tagged BRD3 expressed in Escherichia coli assessed as inhibition of binding to SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHGSGSK-biotin after 1 hr by TR-FRET assay	B	6.8	pIC50	160	nM	IC50	J Med Chem (2012) 55: 587-596 [PMID:22136469]
GtoPdb	Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD3.	-	7.37	pIC50	42.2	nM	IC50	J Med Chem (2011) 54: 3827-38 [PMID:21568322]
ChEMBL	Displacement of acetylated histone peptide from BRD3-BD1,2 by FRET assay	B	7.37	pIC50	42.4	nM	IC50	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Displacement of tetra-acetylated H4 peptide from human Brd3 bromodomain BD12 after 1 hr by FRET analysis	B	7.37	pIC50	42.4	nM	IC50	J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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	pKd	99.4	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry	B	7.02	pKd	95	nM	Kd	J Med Chem (2016) 59: 1492-1500 [PMID:26367539]
ChEMBL	Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry	B	7.19	pKd	65	nM	Kd	J Med Chem (2016) 59: 1492-1500 [PMID:26367539]
ChEMBL	Binding affinity to BRD4-BD1,2 by isothermal titration calorimetry	B	7.26	pKd	55.2	nM	Kd	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Binding affinity to His6-tagged BRD4 expressed in Escherichia coli by isothermal colorimetric analysis	B	7.31	pKd	49	nM	Kd	J Med Chem (2012) 55: 587-596 [PMID:22136469]
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	7.32	pKd	47.6	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to human partial length BRD4-BD1 (N44 to E168 residues) expressed in bacterial expression system by BROMOscan method	B	7.39	pKd	41	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Displacement of biotinylated acetylated peptide from recombinant human partial length BRD4 long isoform bromodomain 1/2 (N44 to E460 residues) expressed in Escherichia coli BL21 measured after 1 hr by Bromoscan method	B	7.43	pKd	37	nM	Kd	Bioorg Med Chem Lett (2018) 28: 3483-3488 [PMID:30268702]
ChEMBL	Competitive binding affinity to human partial length BRD4 (BD1,2) (N44 to E460 residues) expressed in bacterial expression system by BROMOscan assay	B	7.43	pKd	37	nM	Kd	Bioorg Med Chem Lett (2019) 29: 1220-1226 [PMID:30905542]
ChEMBL	Binding affinity to human partial length BRD4-BD2 (K333 to E460 residues) expressed in bacterial expression system by BROMOscan method	B	7.72	pKd	19	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Inhibition of Cy5-linked JQ1 probe binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain1 after 60 mins by HTRF assay	B	6.7	pKi	200	nM	Ki	Bioorg Med Chem (2019) 27: 457-469 [PMID:30606676]
ChEMBL	Inhibition of tetra-acetylated Histone H4 peptide binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain1 after 60 mins by ALPHA screen assay	B	6.79	pKi	163	nM	Ki	Bioorg Med Chem (2019) 27: 457-469 [PMID:30606676]
ChEMBL	Inhibition of Cy5-linked JQ1 probe binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain2 after 60 mins by HTRF assay	B	7.03	pKi	94	nM	Ki	Bioorg Med Chem (2019) 27: 457-469 [PMID:30606676]
ChEMBL	Binding affinity to human recombinant BRD4 BD1 (44 to 168 residues) by fluorescence polarization assay	B	7.13	pKi	73.5	nM	Ki	Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688]
ChEMBL	Binding affinity to human recombinant BRD4 BD2 (333 to 460 residues) by fluorescence polarization assay	B	7.18	pKi	65.8	nM	Ki	Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688]
ChEMBL	Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 tandem domain (44 to 460 residues) (unknown origin) incubated for 1 hr by fluorescence polarization assay	B	7.3	pKi	50.12	nM	Ki	J Med Chem (2016) 59: 7801-7817 [PMID:27528113]
ChEMBL	Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 bromodomain 1 (44 to 460 residues) N140A mutant (unknown origin) incubated for 1 hr by fluorescence polarization assay	B	7.3	pKi	50.12	nM	Ki	J Med Chem (2016) 59: 7801-7817 [PMID:27528113]
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	pKi	46.4	nM	Ki	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL	Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 bromodomain 2 (44 to 460 residues) N433A mutant (unknown origin) incubated for 1 hr by fluorescence polarization assay	B	7.4	pKi	39.81	nM	Ki	J Med Chem (2016) 59: 7801-7817 [PMID:27528113]
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	7.41	pKi	38.8	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	7.49	pKi	32.3	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	7.64	pKi	23	nM	Ki	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL	Inhibition of His6-tagged BRD4 expressed in Escherichia coli after 60 mins by fluorescence anisotropy assay	B	6.13	pIC50	740	nM	IC50	J Med Chem (2012) 55: 587-596 [PMID:22136469]
ChEMBL	Inhibition of BRD4 bromodomain-1 (unknown origin) by FRET assay	B	6.2	pIC50	631	nM	IC50	Eur J Med Chem (2018) 152: 542-559 [PMID:29758518]
ChEMBL	Binding affinity to His6-tagged BRD4 (unknown origin) after 60 mins by fluorescence anisotropy binding Assay	B	6.2	pIC50	630.96	nM	IC50	J Med Chem (2013) 56: 7501-7515 [PMID:24015967]
ChEMBL	Inhibition of BRD4 in human whole blood assessed as reduction in LPS-induced IL-6 secretion preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by MSD assay	B	6.2	pIC50	630.96	nM	IC50	J Med Chem (2021) 64: 12200-12227 [PMID:34387088]
ChEMBL	Inhibition of BRD4 (unknown origin) by fluorescence anisotrophy	B	6.2	pIC50	630	nM	IC50	J Med Chem (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL	Inhibition of BRD4 (unknown origin)	B	6.2	pIC50	630	nM	IC50	Bioorg Med Chem (2018) 26: 3399-3405 [PMID:29764756]
ChEMBL	Inhibition of BRD4-BD1 (unknown origin) by TR-FRET assay	B	6.23	pIC50	590	nM	IC50	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Inhibition of BRD4 in human MM1S cells assessed as down regulation of c-Myc expression after 1 hr by Western blot analysis	B	6.48	pIC50	329	nM	IC50	Medchemcomm (2018) 9: 1779-1802 [PMID:30542529]
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	6.49	pIC50	320	nM	IC50	Bioorg Med Chem (2020) 28: 115601-115601 [PMID:32631570]
ChEMBL	Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced IL-6 secretion incubated for 18 to 24 hrs by MSD assay	B	6.5	pIC50	316.23	nM	IC50	J Med Chem (2021) 64: 12200-12227 [PMID:34387088]
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	6.59	pIC50	260	nM	IC50	Eur J Med Chem (2017) 137: 176-195 [PMID:28586718]
ChEMBL	Inhibition of His6-tagged BRD4-BD12 expressed in Escherichia coli assessed as inhibition of binding to SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHGSGSK-biotin after 1 hr by TR-FRET assay	B	6.72	pIC50	190	nM	IC50	J Med Chem (2012) 55: 587-596 [PMID:22136469]
ChEMBL	Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs	B	6.72	pIC50	190	nM	IC50	ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758]
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	6.81	pIC50	156	nM	IC50	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	6.84	pIC50	145	nM	IC50	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL	Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR method	B	6.88	pIC50	132	nM	IC50	Bioorg Med Chem Lett (2018) 28: 1811-1816 [PMID:29657099]
ChEMBL	Inhibition of BRD4 BD1 (unknown origin) measured by TR-FRET assay	B	6.9	pIC50	125.89	nM	IC50	J Med Chem (2022) 65: 15174-15207 [PMID:36378954]
ChEMBL	Inhibition of BRD4 BD2 (unknown origin) measured by TR-FRET assay	B	6.9	pIC50	125.89	nM	IC50	J Med Chem (2022) 65: 15174-15207 [PMID:36378954]
ChEMBL	Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged BRD4 bromodomain1 by FRET assay	B	6.92	pIC50	120	nM	IC50	J Med Chem (2016) 59: 1271-1298 [PMID:26572217]
ChEMBL	Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISA	B	6.92	pIC50	120	nM	IC50	ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758]
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	7.01	pIC50	98.4	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	7.03	pIC50	93.4	nM	IC50	Eur J Med Chem (2018) 150: 156-175 [PMID:29525435]
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	7.11	pIC50	77.5	nM	IC50	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL	Inhibition of His-tagged human BRD4-BD1 using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay	B	7.17	pIC50	68	nM	IC50	Bioorg Med Chem Lett (2018) 28: 1811-1816 [PMID:29657099]
ChEMBL	Inhibition of BRD4 BD1-BD2 (unknown origin) using tetraacetylated histone peptide as substrate after 2 hrs by alphascreen assay	B	7.21	pIC50	61	nM	IC50	Bioorg Med Chem Lett (2017) 27: 4606-4613 [PMID:28939121]
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	7.4	pIC50	40	nM	IC50	J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
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	7.4	pIC50	40	nM	IC50	J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
GtoPdb	Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD4.	-	7.44	pIC50	36.1	nM	IC50	J Med Chem (2011) 54: 3827-38 [PMID:21568322]
ChEMBL	Displacement of acetylated histone peptide from BRD4-BD1,2 by FRET assay	B	7.44	pIC50	36.1	nM	IC50	Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL	Displacement of tetra-acetylated H4 peptide from human Brd4 bromodomain BD12 after 1 hr by FRET analysis	B	7.44	pIC50	36.1	nM	IC50	J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL	Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assay	B	7.44	pIC50	36	nM	IC50	J Med Chem (2016) 59: 1565-1579 [PMID:26731490]
ChEMBL	Inhibition of human His-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assay	B	7.44	pIC50	36	nM	IC50	J Med Chem (2016) 59: 1565-1579 [PMID:26731490]
ChEMBL	Binding affinity to human BRD4 1/2 bromodomain by FRET assay	B	7.44	pIC50	36	nM	IC50	J Med Chem (2013) 56: 3217-3227 [PMID:23517011]
ChEMBL	Displacement of tetra-acetylated Histone H4 peptide from BRD4 (unknown origin) incubated for 1 hr by FRET analysis	B	7.49	pIC50	32.5	nM	IC50	J Med Chem (2020) 63: 14243-14275 [PMID:32870008]
ChEMBL	Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using histone H4 peptide as substrate by alpha screen assay	B	7.49	pIC50	32.5	nM	IC50	Eur J Med Chem (2019) 163: 281-294 [PMID:30529546]
ChEMBL	Inhibition of BRD4 (unknown origin)	B	7.52	pIC50	30	nM	IC50	Eur J Med Chem (2021) 213: 113137-113137 [PMID:33460833]
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	7.7	pIC50	20	nM	IC50	J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
GtoPdb	Measured in a ApoA1 reporter gene assay.	-	6.15	pEC50	700	nM	EC50	J Med Chem (2011) 54: 3827-38 [PMID:21568322]
ChEMBL	Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced TNFalpha secretion preincubated for 1 hr followed by LPS-stimulation and measured after 20 hrs by magnetic beads technique based assay	B	6.36	pEC50	440	nM	EC50	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL	Binding affinity to human partial length BRDT-BD1 (N21 to E137 residues) expressed in bacterial expression system by BROMOscan method	B	6.95	pKd	112	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Binding affinity to human partial length BRDT-BD2 (K250 to E382 residues) expressed in bacterial expression system by BROMOscan method	B	7.22	pKd	60	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
ChEMBL	Binding affinity to human partial length CREBBP (R1081 to G1197 residues) expressed in bacterial expression system by BROMOscan method	B	4.08	pKd	83000	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]
ChEMBL	Binding affinity to biotinylated CREBBP (1043 to 1159 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	5	pKd	>10000	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
ChEMBL	Binding affinity to human partial length EP300 (A1040 to G1161 residues) expressed in bacterial expression system by BROMOscan method	B	4.15	pKd	71000	nM	Kd	Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]