MK-7622 [Ligand Id: 10712] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4078588 (Mk-7622, MK7622)
  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL Inhibition of recombinant human 5-LOX using arachidonic acid as substrate measured after 5 mins by fluorescence assay B 5.36 pIC50 4400 nM IC50 ACS Med Chem Lett (2018) 9: 652-656 [PMID:30034595]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.22 pIC50 60000 nM IC50 ACS Med Chem Lett (2018) 9: 652-656 [PMID:30034595]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO-NFAT cells assessed as potentiation of acetylcholine-induced calcium mobilization after 4 hrs by CCF4-AM dye-based assay F 7 pEC50 <100 nM EC50 Bioorg Med Chem Lett (2018) 28: 2175-2179 [PMID:29754948]

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]