LGK974 [Ligand Id: 11167] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3188386 (Lgk974, LGK-974, LGK974, Wnt-974, Wnt974, WNT-974, WNT974) |
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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] | ||||||||
| GtoPdb | Displacement of [3H]-GNF-1331 in a hPORCN radioligand binding assay. | - | 9 | pIC50 | 1 | nM | IC50 | Proc Natl Acad Sci USA (2013) 110: 20224-9 [PMID:24277854] |
| 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 | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5472-5476 [PMID:26522946] |
| ChEMBL | Inhibition of porcupine (unknown origin) | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2017) 60: 6678-6692 [PMID:28671458] |
| porcupine O-acyltransferase/Probable protein-cysteine N-palmitoyltransferase porcupine in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255164] [GtoPdb: 3145] [UniProtKB: Q9JJJ7] | ||||||||
| ChEMBL | Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells after 48 hrs by Super-top flash reporter gene assay | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Bioorg Med Chem (2016) 24: 5861-5872 [PMID:27692509] |
| ChEMBL | Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells assessed as suppression of Wnt signaling after 48 hrs by Super-top flash reporter gene assay | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Eur J Med Chem (2018) 149: 110-121 [PMID:29499483] |
| 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 | 9.4 | pIC50 | 0.4 | nM | IC50 | ACS Med Chem Lett (2016) 7: 676-680 [PMID:27437076] |
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]
