taladegib [Ligand Id: 10333] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2142592 (LY-2940680, LY2940680, Taladegib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| SMO/Smoothened homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5971] [GtoPdb: 239] [UniProtKB: Q99835] | ||||||||
| GtoPdb | Gli-luc reporter assay. | - | 8.2 | pIC50 | 6.3 | nM | IC50 | Eur J Med Chem (2017) 138: 384-395 [PMID:28688278] |
| ChEMBL | Inhibition of SMO D473H mutant receptor (unknown origin) assessed as inhibition of SAG-induced Hh signaling pathway by Gli luciferase reporter cell-based assay | B | 8.38 | pIC50 | 4.17 | nM | IC50 | Bioorg Med Chem (2020) 28: 115354-115354 [PMID:32063403] |
| SMO/Smoothened homolog in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6080] [GtoPdb: 239] [UniProtKB: P56726] | ||||||||
| ChEMBL | Antagonist activity at Smo receptor in mouse NIH/3T3 cells harboring GRE-Luc assessed as inhibition of SAG-induced Hh signaling pathway preincubated for 1 to 2 hrs followed by SAG addition and measured after 24 hrs by Bright-Glo luciferase reporter gene assay | F | 8.62 | pIC50 | 2.4 | nM | IC50 | Medchemcomm (2017) 8: 1332-1336 [PMID:30108845] |
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]
