compound 3 [PMID: 17942791] [Ligand Id: 8556] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1979298
  • Ras converting CAAX endopeptidase 1/Prenyl protein specific protease in Human [ChEMBL: CHEMBL3411] [GtoPdb: 2412] [UniProtKB: Q9Y256]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Ras converting CAAX endopeptidase 1/Prenyl protein specific protease in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3411] [GtoPdb: 2412] [UniProtKB: Q9Y256]
GtoPdb - - 5.05 pIC50 9000 nM IC50 J Biomol Screen (2007) 12: 983-93 [PMID:17942791]
ChEMBL Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins B 5.16 pIC50 6900 nM IC50 Bioorg Med Chem (2016) 24: 160-178 [PMID:26706114]
Protein disulfide-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5422] [UniProtKB: P07237]
ChEMBL Inhibition of recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) using bovine insulin as substrate preincubated for 1 hr followed by substrate addition B 6.52 pIC50 300 nM IC50 J Med Chem (2020) 63: 10263-10286 [PMID:32830969]

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]