osilodrostat [Ligand Id: 8310] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3099695 (Osilodrostat, LCI-699-NX, LCI699-NX)
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  • CYP11B2 in Human [GtoPdb: 1360] [UniProtKB: P19099]
  • CYP11B2/Cytochrome P450 11B2, mitochondrial in Mouse [ChEMBL: CHEMBL3621020] [GtoPdb: 1360] [UniProtKB: P15539]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]