AZD4017 [Ligand Id: 7695] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2153191 (Azd 4017, Azd-4017, AZD-4017, AZD4017) |
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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 | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| ChEMBL | Inhibition of N-terminal His6-tagged full length human 11betaHSD1 expressed in baculovirus infected cells using cortisone as substrate after 25 mins by HTRF assay | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
| ChEMBL | Inhibition of N-terminal 6-His-tagged human full length 11beta-HSD1 assessed as conversion of cortisone to cortisol after 25 mins by HTRF assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Medchemcomm (2012) 3: 1264-1269 |
| ChEMBL | Time Resolved Fluorescence Assay: The conversion of cortisone to the active steroid cortisol by 11βHSD1 oxo-reductase activity, can be measured using a competitive homogeneous time resolved fluorescence assay (HTRF) (CisBio International, R&D, Administration and Europe Office, In Vitro Technologies HTRF/Bioassays BP 84175, 30204 Bagnols/Cèze Cedex, France. Cortisol bulk HTRF kit: Cat No. 62CORPEC). | B | 8.15 | pIC50 | 7 | nM | IC50 | US-8673938-B2. Chemical compounds (2014) |
| ChEMBL | Inhibition of 11betaHSD1 in human isolated adipocytes using [3H]cortisone as substrate after 6 hrs by flow scintillation analysis | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
| 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] |
| ChEMBL | Inhibition of 11beta-HSD1 in human adipocytes assessed as conversion of [3H]-cortisone to [3H]-cortisol by scintillation counting analysis | B | 8.7 | pIC50 | 2 | nM | IC50 | Medchemcomm (2012) 3: 1264-1269 |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2012) 55: 5951-64 [PMID:22691057] |
| 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 His6-tagged full length mouse 11betaHSD1 expressed in baculovirus infected cells using cortisone as substrate after 25 mins by HTRF assay | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
| ChEMBL | Inhibition of N-terminal 6-His tagged full length mouse 11betaHSD1 incubated for 25 mins by HTRF assay | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| ChEMBL | Inhibition of N-terminal 6-His-tagged mouse full length 11beta-HSD1 assessed as conversion of cortisone to cortisol after 25 mins by HTRF assay | B | 6.12 | pIC50 | 750 | nM | IC50 | Medchemcomm (2012) 3: 1264-1269 |
| 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 His6-tagged full length rat 11betaHSD1 expressed in baculovirus infected cells using cortisone as substrate after 25 mins by HTRF assay | B | 5.39 | pIC50 | 4060 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
| ChEMBL | Inhibition of N-terminal 6-His tagged full length rat 11betaHSD1 incubated for 25 mins by HTRF assay | B | 5.39 | pIC50 | 4060 | nM | IC50 | J Med Chem (2012) 55: 10136-10147 [PMID:23088558] |
| ChEMBL | Inhibition of N-terminal 6-His-tagged rat full length 11beta-HSD1 assessed as conversion of cortisone to cortisol after 25 mins by HTRF assay | B | 5.39 | pIC50 | 4060 | nM | IC50 | Medchemcomm (2012) 3: 1264-1269 |
| 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 recombinant 11betaHSD2 using cortisol as substrate after 40 mins by fluorescence spectrophotometry | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
| 11-beta-hydroxysteroid dehydrogenase type 1 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5342] [UniProtKB: Q5XX84] | ||||||||
| ChEMBL | Inhibition of N-terminal His6-tagged full length dog 11betaHSD1 expressed in baculovirus infected cells using cortisone as substrate after 25 mins by HTRF assay | B | 5.42 | pIC50 | 3770 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
| Estradiol 17-beta-dehydrogenase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3181] [UniProtKB: P14061] | ||||||||
| ChEMBL | Inhibition of recombinant 17betaHSD1 using [3H]estrone as substrate after 20 mins by flow scintillation analysis | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
| Estradiol 17-beta-dehydrogenase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4234] [UniProtKB: P37058] | ||||||||
| ChEMBL | Inhibition of recombinant 17betaHSD3 using [3H]androstenedione as substrate after 90 mins by flow scintillation analysis | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by IonWorks assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 5951-5964 [PMID:22691057] |
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]
