ChEMBL ligand: CHEMBL4541479
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!
mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] 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	Inhibition of BRD4 (unknown origin)	B	5.44	pKd	3600	nM	Kd	Eur J Med Chem (2019) 178: 530-543 [PMID:31212132]
ChEMBL	Binding affinity to human BRD4 BD1 (44 to 168 residues) expressed in bacterial expression system by bromoscan assay	B	5.44	pKd	3600	nM	Kd	J Med Chem (2022) 65: 6513-6540 [PMID:35468293]
ChEMBL	Binding affinity to BRD4 (unknown origin)	B	5.44	pKd	3600	nM	Kd	J Med Chem (2023) 66: 4491-4502 [PMID:37002872]
mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164]
ChEMBL	Inhibition of ERK5 in human SN12C cells transduced with MEF2-responsive transcription element assessed as reduction in MEF2 transcription by measuring luciferase signal after 16 hrs by luciferase reporter gene assay	B	7.07	pIC50	86	nM	IC50	J Med Chem (2019) 62: 928-940 [PMID:30563338]
ChEMBL	Inhibition of ERK5 in human HeLa cells assessed as reduction in EGF-induced ERK5 autophosphorylation	B	7.07	pIC50	86	nM	IC50	J Med Chem (2023) 66: 4491-4502 [PMID:37002872]
ChEMBL	Inhibition of His-tagged MAP2K5 activated N-terminal GST-tagged recombinant human ERK5 (1 to 398 residues) expressed in Escherichia coli using biotin-Ahx-PPGDYSTTPGGTLFSTTPGGTRI peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by TR-FRET assay	B	7.7	pIC50	20	nM	IC50	J Med Chem (2019) 62: 928-940 [PMID:30563338]
ChEMBL	Inhibition of ERK5 in human HeLa cells by KiNativ profiling method	B	8.1	pIC50	8	nM	IC50	Eur J Med Chem (2019) 178: 530-543 [PMID:31212132]
ChEMBL	Inhibition of ERK5 (unknown origin) incubated for 1 hr by KiNativ profiling analysis	B	8.1	pIC50	8	nM	IC50	J Med Chem (2022) 65: 6513-6540 [PMID:35468293]
ChEMBL	Inhibition of ERK5 (unknown origin)	B	8.1	pIC50	8	nM	IC50	J Med Chem (2023) 66: 4491-4502 [PMID:37002872]
GtoPdb	-	-	8.1	pIC50	8	nM	IC50	Proc Natl Acad Sci U S A (2016) 113: 11865-11870 [PMID:27679845]

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]