GNF-1331 [Ligand Id: 12019] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4540197
  • 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 Displacement of [3H]-GNF-1331 from human PORCN after 3 hrs by scintillation counting analysis B 8.1 pIC50 8 nM IC50 ACS Med Chem Lett (2016) 7: 676-680 [PMID:27437076]
GtoPdb Measuring displacement of radio-labelled GNF-1331 from hPORCN - 8.1 pIC50 8 nM IC50 ACS Med Chem Lett (2016) 7: 676-80 [PMID:27437076]
porcupine O-acyltransferase/Probable protein-cysteine N-palmitoyltransferase porcupine in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255164] [GtoPdb: 3145] [UniProtKB: Q9JJJ7]
ChEMBL Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by luminescence assay B 7.92 pIC50 12 nM IC50 ACS Med Chem Lett (2016) 7: 676-680 [PMID:27437076]

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]