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 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]
