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 BRD4 (unknown origin)	B	6.66	pIC50	220	nM	IC50	Eur J Med Chem (2020) 186: 111852-111852 [PMID:31759729]
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 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	Displacement of acetylated histone H4 peptide from His-tagged recombinant human BRD4 expressed in bacteria by AlphaScreen assay	B	6.66	pIC50	220	nM	IC50	Bioorg Med Chem Lett (2022) 64: 128696-128696 [PMID:35318165]
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]
ChEMBL	Displacement of biotinylated acetylated histone H4 peptide from human recombinant N-terminal GST-tagged BRD4 BD1 (49 to 170 residues) expressed in Escherichia coli expression system incubated for 30 mins by AlphaScreen assay	B	7.39	pIC50	41	nM	IC50	Bioorg Med Chem Lett (2022) 64: 128696-128696 [PMID:35318165]
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 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]