AZD8329 [Ligand Id: 7715] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2177609 (AZD-8329) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4235] [GtoPdb: 2763] [UniProtKB: P28845] | ||||||||
| ChEMBL | Inhibition of N-terminal 6-His tagged full length human 11betaHSD1 incubated for 25 mins by HTRF assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| GtoPdb | - | - | 8.05 | pIC50 | 9 | nM | IC50 | AZD8329.. astrazeneca.com |
| ChEMBL | Inhibition of 11betaHSD1 in human adipocytes assessed as cortisone to cortisol conversion by scintillation counting method | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3910] [GtoPdb: 2763] [UniProtKB: P50172] | ||||||||
| ChEMBL | Inhibition of N-terminal 6-His tagged full length mouse 11betaHSD1 incubated for 25 mins by HTRF assay | B | 5.21 | pIC50 | 6100 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2391] [GtoPdb: 2763] [UniProtKB: P16232] | ||||||||
| ChEMBL | Inhibition of N-terminal 6-His tagged full length rat 11betaHSD1 incubated for 25 mins by HTRF assay | B | 7.07 | pIC50 | 86 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| hydroxysteroid 11-beta dehydrogenase 2/11-beta-hydroxysteroid dehydrogenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3746] [GtoPdb: 3143] [UniProtKB: P80365] | ||||||||
| ChEMBL | Inhibition of 11beta-HSD2 assessed as conversion of cortisol to cortisone by fluorescence based assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| Estradiol 17-beta-dehydrogenase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3181] [UniProtKB: P14061] | ||||||||
| ChEMBL | Inhibition of 17beta-HSD1 assessed as conversion of estrone to estradiol by scintillation counting method | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
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]
