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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL2139947
  • porcupine O-acyltransferase/Probable protein-cysteine N-palmitoyltransferase porcupine in Human [ChEMBL: CHEMBL1255163] [GtoPdb: 3145] [UniProtKB: Q9H237]
There should be some charts here, you may need to enable JavaScript!
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 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]