LGK974 [Ligand Id: 11167] 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: CHEMBL3188386 (Lgk974, LGK-974, LGK974, Wnt-974, Wnt974, WNT-974, WNT974) |
|---|
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] | ||||||||
| 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 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]
