Wnt-C59 [Ligand Id: 12020] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2139947
  • porcupine O-acyltransferase/Probable protein-cysteine N-palmitoyltransferase porcupine in Human [ChEMBL: CHEMBL1255163] [GtoPdb: 3145] [UniProtKB: Q9H237]
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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 HEK293T cells transfected with Wnt3A-expressing vector assessed as suppression of Wnt/beta-catenin signaling after 22 hrs by Super-top flash reporter gene assay B 9 pIC50 <1 nM IC50 J Med Chem (2018) 61: 4087-4102 [PMID:29630366]
GtoPdb Measuring inhibition of PORCN activity expressed in human HT1080 cells in a Wnt3A-driven luciferase production assay - 10.13 pIC50 0.07 nM IC50 Bioorg Med Chem Lett (2015) 25: 5472-6 [PMID:26522946]
ChEMBL Inhibition of porcupine activity (unknown origin) expressed in human HT1080 cells assessed as suppression of Wnt3A-mediated super top flash activity by STF luciferase assay B 10.13 pIC50 0.07 nM IC50 Bioorg Med Chem Lett (2015) 25: 5472-5476 [PMID:26522946]

ChEMBL data shown on this page come from version 35:

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]