ChEMBL ligand: CHEMBL2179387
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!
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!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL	Binding affinity to first bromodomain of BRD4 (unknown origin)	B	6.87	pKd	136	nM	Kd	J Med Chem (2013) 56: 8073-8088 [PMID:24090311]
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	5.45	pIC50	3540	nM	IC50	Eur J Med Chem (2016) 121: 294-299 [PMID:27266999]
ChEMBL	Inhibition of BRD4 in human MOLM-14 cells harboring FLT3-ITD mutant assessed as decrease in metabolic activity measured after 72 hrs by MTT assay	B	5.57	pIC50	2700	nM	IC50	ACS Med Chem Lett (2020) 11: 1928-1934 [PMID:33062175]
ChEMBL	Inhibition of BRD4 in human HEL cells harboring JAK2 V617F mutant assessed as decrease in metabolic activity measured after 72 hrs by MTT assay	B	5.7	pIC50	2000	nM	IC50	ACS Med Chem Lett (2020) 11: 1928-1934 [PMID:33062175]
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	6.01	pIC50	980	nM	IC50	Eur J Med Chem (2016) 121: 294-299 [PMID:27266999]
ChEMBL	Inhibition of BRD4 (unknown origin) by Alphascreen assay	B	6.66	pIC50	220	nM	IC50	Eur J Med Chem (2018) 152: 264-273 [PMID:29730189]
ChEMBL	Inhibition of BRD4 bromodomain (unknown origin)	B	6.66	pIC50	220	nM	IC50	Bioorg Med Chem Lett (2019) 29: 126577-126577 [PMID:31421967]
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	6.66	pIC50	220	nM	IC50	Bioorg Med Chem (2018) 26: 2937-2957 [PMID:29776834]
ChEMBL	Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assay	B	6.66	pIC50	220	nM	IC50	J Med Chem (2013) 56: 3217-3227 [PMID:23517011]
ChEMBL	Inhibition of BRD4 (unknown origin)	B	6.66	pIC50	220	nM	IC50	Bioorg Med Chem (2018) 26: 3399-3405 [PMID:29764756]
ChEMBL	Inhibition of BRD4 isoform 1 by AlphaScreen assay	B	6.66	pIC50	220	nM	IC50	J Med Chem (2012) 55: 9831-9837 [PMID:23095041]
GtoPdb	Assayed using recombinant BRD4-BD1.	-	6.66	pIC50	220	nM	IC50	J Med Chem (2012) 55: 9831-7 [PMID:23095041]
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	7.06	pIC50	88	nM	IC50	Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
ChEMBL	Binding affinity to CREBBP by SPR method	B	4.31	pKd	49000	nM	Kd	J Med Chem (2012) 55: 9831-9837 [PMID:23095041]

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]