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ChEMBL ligand: CHEMBL4541479 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
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 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] |
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 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]