ChEMBL ligand: CHEMBL2017291 (GSK1210151A)
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!
phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] 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 biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	7.15	pKd	70.3	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	7.26	pKd	54.8	nM	Kd	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	7.3	pKi	49.6	nM	Ki	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	8.05	pKi	9	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to human BRD2 assessed as inhibition of Alexa Fluor 488 binding after 60 mins by fluorescence anisotropic analysis	B	6.3	pIC50	501.19	nM	IC50	Bioorg Med Chem Lett (2012) 22: 2968-2972 [PMID:22437115]
GtoPdb	-	-	6.3	pIC50	500	nM	IC50	Nature (2011) 478: 529-33 [PMID:21964340]
ChEMBL	Inhibition of BRD2 (unknown origin) by fluorescence anisotrophy	B	6.3	pIC50	500	nM	IC50	J Med Chem (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL	Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD2 BD2 (1 to 473 residues)/BD1 Y113A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay	B	6.7	pIC50	199.53	nM	IC50	J Med Chem (2020) 63: 9020-9044 [PMID:32787145]
ChEMBL	Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD2 BD1 (1 to 473 residues)/BD2 Y386A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay	B	7.3	pIC50	50.12	nM	IC50	J Med Chem (2020) 63: 9020-9044 [PMID:32787145]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
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	40.5	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	7.53	pKd	29.8	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	7.65	pKi	22.3	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	8.14	pKi	7.2	nM	Ki	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Binding affinity to BRD3 assessed as inhibition of Alexa Fluor 488 binding after 60 mins by fluorescence anisotropic analysis	B	6.6	pIC50	251.19	nM	IC50	Bioorg Med Chem Lett (2012) 22: 2968-2972 [PMID:22437115]
GtoPdb	-	-	6.6	pIC50	250	nM	IC50	Nature (2011) 478: 529-33 [PMID:21964340]
ChEMBL	Inhibition of BRD3 (unknown origin) by fluorescence anisotrophy	B	6.6	pIC50	250	nM	IC50	J Med Chem (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL	Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD3 BD2 (1 to 435 residues)/BD1 Y73A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay	B	7.1	pIC50	79.43	nM	IC50	J Med Chem (2020) 63: 9020-9044 [PMID:32787145]
ChEMBL	Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD3 BD1 (1 to 435 residues)/BD2 Y348A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay	B	7.5	pIC50	31.62	nM	IC50	J Med Chem (2020) 63: 9020-9044 [PMID:32787145]
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 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method	B	6.67	pKd	215	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	7.28	pKd	52.8	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
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	6.41	pKi	385	nM	Ki	Bioorg Med Chem (2019) 27: 457-469 [PMID:30606676]
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	7.13	pKi	74.8	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	7.13	pKi	74.8	nM	Ki	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
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	7.21	pKi	61	nM	Ki	Bioorg Med Chem (2019) 27: 457-469 [PMID:30606676]
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	8.05	pKi	9	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 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay	B	8.05	pKi	9	nM	Ki	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
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	5.9	pIC50	1258.93	nM	IC50	J Med Chem (2021) 64: 12200-12227 [PMID:34387088]
ChEMBL	Binding affinity to BRD4 assessed as inhibition of Alexa Fluor 488 binding after 60 mins by fluorescence anisotropic analysis	B	6.1	pIC50	794.33	nM	IC50	Bioorg Med Chem Lett (2012) 22: 2968-2972 [PMID:22437115]
GtoPdb	-	-	6.1	pIC50	790	nM	IC50	Nature (2011) 478: 529-33 [PMID:21964340]
ChEMBL	Inhibition of BRD4 (unknown origin) by fluorescence polarization assay	B	6.1	pIC50	790	nM	IC50	Bioorg Med Chem (2018) 26: 2937-2957 [PMID:29776834]
ChEMBL	Binding affinity to human BRD4 1/2 bromodomain by fluorescence anisotropic assay	B	6.1	pIC50	790	nM	IC50	J Med Chem (2013) 56: 3217-3227 [PMID:23517011]
ChEMBL	Inhibition of BRD4 (unknown origin) by fluorescence anisotrophy	B	6.1	pIC50	790	nM	IC50	J Med Chem (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL	Inhibition of BRD4 (unknown origin) by fluorescence anisotropy ligand displacement assay	B	6.1	pIC50	790	nM	IC50	Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013]
ChEMBL	Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD2 (1 to 477 residues)/BD1 Y97A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay	B	6.5	pIC50	316.23	nM	IC50	J Med Chem (2020) 63: 9020-9044 [PMID:32787145]
ChEMBL	Displacement of Alexa Fluor 647 labelled ligand from His6-tagged BRD4 BD2 (1 to 477 residues)/BD1 Y97A mutant (unknown origin) after 30 mins by TR-FRET assay	B	6.56	pIC50	274	nM	IC50	J Med Chem (2020) 63: 9045-9069 [PMID:32691589]
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	6.65	pIC50	226	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 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay	B	6.65	pIC50	226	nM	IC50	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
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	6.7	pIC50	199.53	nM	IC50	J Med Chem (2021) 64: 12200-12227 [PMID:34387088]
ChEMBL	Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs	B	6.89	pIC50	130	nM	IC50	ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758]
ChEMBL	Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assay	B	6.97	pIC50	107	nM	IC50	Bioorg Med Chem (2015) 23: 953-959 [PMID:25678016]
ChEMBL	Inhibition of BRD4(1) (unknown origin) incubated for 4 hrs by (+)-JQ1 fluorescent ligand based fluorescence anisotrophy	B	7	pIC50	100	nM	IC50	J Med Chem (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL	Displacement of Alexa Fluor 647 labelled ligand from His6-thr-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant (unknown origin) after 30 mins by TR-FRET assay	B	7.44	pIC50	36	nM	IC50	J Med Chem (2020) 63: 9045-9069 [PMID:32691589]
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	7.5	pIC50	31.7	nM	IC50	J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
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	7.5	pIC50	31.7	nM	IC50	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL	Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay	B	7.6	pIC50	25.12	nM	IC50	J Med Chem (2020) 63: 9020-9044 [PMID:32787145]
ChEMBL	Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal 6His-tagged BRD4-BD1 Y390A mutant (1 to 477 residue) expressed in Escherichia coli incubated for 30 mins by TR-FRET assay	B	7.6	pIC50	25.12	nM	IC50	J Med Chem (2021) 64: 12200-12227 [PMID:34387088]
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	7.74	pIC50	18	nM	IC50	ACS Med Chem Lett (2016) 7: 145-150 [PMID:26985289]
ChEMBL	Inhibition of BRD4 bromodomain 1 (unknown origin)	B	7.74	pIC50	18	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	7.74	pIC50	18	nM	IC50	ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL	Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRDT BD2 (1 to 397 residues)/BD1 Y66A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay	B	5.8	pIC50	1584.89	nM	IC50	J Med Chem (2020) 63: 9020-9044 [PMID:32787145]
ChEMBL	Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRDT BD1 (1 to 397 residues)/BD2 Y309A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay	B	6.9	pIC50	125.89	nM	IC50	J Med Chem (2020) 63: 9020-9044 [PMID:32787145]
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
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	5.51	pKd	3084	nM	Kd	J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
ChEMBL	Inhibition of PDE4B	B	5.4	pIC50	3981.07	nM	IC50	Bioorg Med Chem Lett (2012) 22: 2968-2972 [PMID:22437115]

ChEMBL data shown on this page come from version 32:

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]