taladegib [Ligand Id: 10333] 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: CHEMBL2142592 (LY-2940680, LY2940680, Taladegib) |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| SMO/Smoothened homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5971] [GtoPdb: 239] [UniProtKB: Q99835] | ||||||||
| ChEMBL | Antagonist activity at resistant Smo D473H mutant (unknown origin) in presence of GDC0449 | F | 6.4 | pIC50 | 400 | nM | IC50 | Eur J Med Chem (2021) 215: 113268-113268 [PMID:33636537] |
| 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 | Inhibition of SMO in mouse 3T3/HH FlashII-7 cells incubated for 36 hrs in presence of SHH by Gli-luciferase reporter assay | B | 8.93 | pIC50 | 1.18 | nM | IC50 | Bioorg Med Chem (2022) 74: 117051-117051 [PMID:36270113] |
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]
