osilodrostat [Ligand Id: 8310] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3099695 (Lci-699, Lci699, LCI-699-NX, LCI699-NX, Osilodrostat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CYP11B1/Cytochrome P450 11B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908] [GtoPdb: 1359] [UniProtKB: P15538] | ||||||||
| ChEMBL | Inhibition of human CYP11B1 expressed in hamster V79MZ cells using [1,2-3H]-11-deoxycorticosterone as substrate after 6 hrs by HPLC analysis | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2017) 60: 5086-5098 [PMID:28570067] |
| ChEMBL | Inhibition of human CYP11B1 expressed in hamster V79MZh cells using deoxycorticosterone as substrate | B | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (2014) 57: 5179-5189 [PMID:24899257] |
| ChEMBL | Inhibition of human CYP11B1 expressed in V79 MZ cells | B | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (2014) 57: 5011-5022 [PMID:24422519] |
| ChEMBL | Inhibition of human CYP11B1 expressed in V79 MZh cells using [14C]-deoxycorticosterone substrate incubated for 6 hrs by HPTLC method | B | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (2015) 58: 2530-2537 [PMID:25711516] |
| ChEMBL | Inhibition of CYP11B1 in human V79MZ cells using [3H]-11-deoxycorticosterone as substrate incubated for 1 hr prior to substrate addition measured after 25 mins by HPLC analysis | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Eur J Med Chem (2015) 90: 788-796 [PMID:25528333] |
| GtoPdb | - | - | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (2014) 57: 5179-89 [PMID:24899257] |
| ChEMBL | Inhibition human recombinant CYP11B1 using 11-deoxycorticosterone as substrate after 2 hrs by scintillation proximity assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2015) 58: 9382-9394 [PMID:26540564] |
| ChEMBL | Inhibition of human recombinant CYP11B1 using 11-deoxycortisol as substrate by cell-based assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1203-1207 [PMID:24900631] |
| CYP11B1/Cytochrome P450 11B1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4970] [GtoPdb: 1359] [UniProtKB: P15393] | ||||||||
| ChEMBL | Inhibition of rat recombinant CYP11B1 using 11-deoxycortisol as substrate by cell-based assay | B | 6.31 | pIC50 | 495 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1203-1207 [PMID:24900631] |
| CYP11B2/Cytochrome P450 11B2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2722] [GtoPdb: 1360] [UniProtKB: P19099] | ||||||||
| ChEMBL | Inhibition of CYP11B2 in human NCI-H295R cells assessed as inhibition of angiotensin-2-induced aldosterone production after 24 hrs by RIA | B | 8.05 | pIC50 | 9 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1203-1207 [PMID:24900631] |
| ChEMBL | Inhibition of human CYP11B2 expressed in renal leiomyoblastoma cells | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2015) 58: 8054-8065 [PMID:26403853] |
| ChEMBL | Inhibition of human CYP11B2 expressed in Chinese hamster V79 cell mitochondria assessed as reduction in aldosterone production using deoxycorticosterone as substrate after 1.5 hrs in presence of NADPH by HTRF assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2018) 61: 5594-5608 [PMID:29878770] |
| ChEMBL | Inhibition of human recombinant CYP11B2 using 11-deoxycorticosterone as substrate by cell-based assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1203-1207 [PMID:24900631] |
| ChEMBL | Inhibition of human recombinant CYP11B2 using 11-deoxycorticosterone as substrate after 2 hrs by scintillation proximity assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2015) 58: 9382-9394 [PMID:26540564] |
| ChEMBL | Inhibition of CYP11B2 in human V79MZ cells using [3H]-11-deoxycorticosterone as substrate incubated for 1 hr prior to substrate addition measured after 45 mins by HPLC analysis | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Eur J Med Chem (2015) 90: 788-796 [PMID:25528333] |
| ChEMBL | Inhibition of human CYP11B2 expressed in V79 MZh cells using [14C]-deoxycorticosterone substrate incubated for 6 hrs by HPTLC method | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2015) 58: 2530-2537 [PMID:25711516] |
| ChEMBL | Inhibition of human CYP11B2 expressed in hamster V79MZh cells using deoxycorticosterone as substrate | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2014) 57: 5179-5189 [PMID:24899257] |
| ChEMBL | Inhibition of CYP11B2 (unknown origin) | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2014) 57: 5179-5189 [PMID:24899257] |
| ChEMBL | Inhibition of human aldosterone synthase expressed in V79 MZ cells | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2014) 57: 5011-5022 [PMID:24422519] |
| GtoPdb | - | - | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2014) 57: 5179-89 [PMID:24899257] |
| CYP11B2/Cytochrome P450 11B2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3237] [GtoPdb: 1360] [UniProtKB: P30099] | ||||||||
| ChEMBL | Inhibition of rat recombinant CYP11B2 using 11-deoxycorticosterone as substrate by cell-based assay | B | 6.95 | pIC50 | 111 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1203-1207 [PMID:24900631] |
| CYP11B2 in Human [GtoPdb: 1360] [UniProtKB: P19099] | ||||||||
| GtoPdb | - | - | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2014) 57: 5179-89 [PMID:24899257] |
| CYP11B2/Cytochrome P450 11B2, mitochondrial in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621020] [GtoPdb: 1360] [UniProtKB: P15539] | ||||||||
| ChEMBL | Inhibition of mouse CYP11B2 expressed in renal leiomyoblastoma cells | B | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2015) 58: 8054-8065 [PMID:26403853] |
| CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
| ChEMBL | Inhibition of human CYP19 preincubated for 10 mins followed by protein addition measured after 90 mins by fluorimetric analysis | B | 5.22 | pIC50 | 6000 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1203-1207 [PMID:24900631] |
| ChEMBL | Inhibition of CYP19A1 (unknown origin) | B | 5.8 | pIC50 | 1584.89 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 979-984 [PMID:29254646] |
| ChEMBL | Inhibition of CYP19 (unknown origin) | B | 6.07 | pIC50 | 856 | nM | IC50 | J Med Chem (2014) 57: 5011-5022 [PMID:24422519] |
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]
