ETC-1922159 [Ligand Id: 11168] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3633802 (Etc-159, Etc-1922159)
  • porcupine O-acyltransferase/Probable protein-cysteine N-palmitoyltransferase porcupine in Human [ChEMBL: CHEMBL1255163] [GtoPdb: 3145] [UniProtKB: Q9H237]
  • porcupine O-acyltransferase/Probable protein-cysteine N-palmitoyltransferase porcupine in Mouse [ChEMBL: CHEMBL1255164] [GtoPdb: 3145] [UniProtKB: Q9JJJ7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
porcupine O-acyltransferase/Probable protein-cysteine N-palmitoyltransferase porcupine in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255163] [GtoPdb: 3145] [UniProtKB: Q9H237]
ChEMBL Inhibition of porcupine in human HEK293 cells assessed as reduction in Wnt secretion by measuring suppression of beta-catenin reporter activity after 24 hrs by STF reporter assay B 8.54 pIC50 2.9 nM IC50 Bioorg Med Chem Lett (2015) 25: 5472-5476 [PMID:26522946]
ChEMBL Inhibition of porcupine (unknown origin) B 8.54 pIC50 2.9 nM IC50 J Med Chem (2017) 60: 6678-6692 [PMID:28671458]
GtoPdb - - 8.54 pIC50 2.9 nM IC50 Bioorg Med Chem Lett (2015) 25: 5472-6 [PMID:26522946]
porcupine O-acyltransferase/Probable protein-cysteine N-palmitoyltransferase porcupine in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255164] [GtoPdb: 3145] [UniProtKB: Q9JJJ7]
ChEMBL Inhibition of mouse porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay B 7.74 pIC50 18.1 nM IC50 Bioorg Med Chem Lett (2015) 25: 5472-5476 [PMID:26522946]

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]