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ChEMBL ligand: CHEMBL488 (Aminoglutethimide, Cytadren, NSC-330915, Orimeten) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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CYP11A1/Cytochrome P450 11A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2033] [GtoPdb: 1358] [UniProtKB: P05108] | ||||||||
ChEMBL | In vitro inhibition of progesterone production in hamster ovarian tissue | F | 4.1 | pIC50 | 80000 | nM | IC50 | J Med Chem (1991) 34: 725-736 [PMID:1825337] |
Cytochrome P450 11A1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4813] [UniProtKB: P00189] | ||||||||
ChEMBL | Inhibition of bovine desmolase, cytochrome P450 11A1 | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (1987) 30: 1550-1554 [PMID:3625703] |
ChEMBL | Inhibition of bovine adrenal cholesterol side chain cleavage(CSCC) cytochrome P450 11A1 | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (1988) 31: 971-976 [PMID:3361583] |
ChEMBL | Inhibition of bovine adrenal desmolase | B | 4.54 | pIC50 | 29000 | nM | IC50 | J Med Chem (1992) 35: 2210-2214 [PMID:1613747] |
CYP11A1 in Hamster [GtoPdb: 1358] | ||||||||
GtoPdb | Measuring inhibition of progesterone synthesis in hamster ovarian slices as an indicatior of CYP11A1 activity. | - | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (1991) 34: 725-36 [PMID:1825337] |
CYP11B2/Cytochrome P450 11B2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3237] [GtoPdb: 1360] [UniProtKB: P30099] | ||||||||
ChEMBL | In vitro inhibition of ACTH-stimulated aldosterone biosynthesis in rat adrenal slices | F | 4.1 | pIC50 | 80000 | nM | IC50 | J Med Chem (1995) 38: 2103-2111 [PMID:7783141] |
ChEMBL | In vitro inhibition of ACTH-stimulated aldosterone biosynthesis in rat adrenal slices | F | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (1995) 38: 2103-2111 [PMID:7783141] |
CYP17A1/Cytochrome P450 17A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3522] [GtoPdb: 1361] [UniProtKB: P05093] | ||||||||
ChEMBL | In vitro inhibition of progesterone production in hamster ovarian tissue | F | 4.22 | pIC50 | 60000 | nM | IC50 | J Med Chem (1991) 34: 1329-1334 [PMID:2016706] |
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
ChEMBL | Inhibition of human aromatase extracted from placental microsomes using [1,2-3H]androstenedione as substrate after 30 mins | B | 5.39 | pKi | 4100 | nM | Ki | Eur J Med Chem (2015) 105: 1-38 [PMID:26469743] |
ChEMBL | Inhibition of human placental cytochrome P450 19A1 with androstenedione | B | 5.74 | pKi | 1800 | nM | Ki | J Med Chem (1987) 30: 1550-1554 [PMID:3625703] |
ChEMBL | Apparent inhibition constant (Ki) for cytochrome P450 19A1 | B | 5.74 | pKi | 1800 | nM | Ki | J Med Chem (1988) 31: 971-976 [PMID:3361583] |
ChEMBL | Apparent Ki against human aromatase | B | 5.85 | pKi | 1410 | nM | Ki | J Med Chem (2004) 47: 4032-4040 [PMID:15267241] |
ChEMBL | Inhibitory constant against human placental atomatase at pH 7.0 and 37 degree C | B | 5.85 | pKi | 1410 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4063-4070 [PMID:15911319] |
ChEMBL | Inhibition of Cytochrome P450 19A1 against testosterone at 1.5 uM (Km=0.13 uM) | B | 6.17 | pKi | 680 | nM | Ki | J Med Chem (1986) 29: 520-523 [PMID:3754286] |
ChEMBL | Inhibitory constant (Ki) for Cytochrome P450 19A1 | B | 6.22 | pKi | 600 | nM | Ki | J Med Chem (1985) 28: 200-204 [PMID:3968684] |
ChEMBL | Inhibition of human placental cytochrome P450 19A1 with testosterone | B | 6.22 | pKi | 600 | nM | Ki | J Med Chem (1987) 30: 1550-1554 [PMID:3625703] |
ChEMBL | Binding affinity was measured on Cytochrome P450 19A1 | B | 6.22 | pKi | 600 | nM | Ki | J Med Chem (1990) 33: 2933-2942 [PMID:2231592] |
ChEMBL | Competitive inhibition of human placental Cytochrome P450 19A1 | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (1991) 34: 725-736 [PMID:1825337] |
ChEMBL | Inhibitory concentration against human placental aromatase as logIC50 | B | 3.45 | pIC50 | 3.45 | nM | Log IC50 | J Med Chem (2004) 47: 4032-4040 [PMID:15267241] |
ChEMBL | In vitro inhibitory concentration against human placental Cytochrome P450 19A was determined using [1-beta,2beta-3H]testosterone as radioligand | B | 4.43 | pIC50 | 37000 | nM | IC50 | J Med Chem (1991) 34: 2685-2691 [PMID:1895288] |
ChEMBL | Concentration inhibiting Aromatase | B | 4.43 | pIC50 | 37000 | nM | IC50 | J Med Chem (1992) 35: 2210-2214 [PMID:1613747] |
ChEMBL | Inhibition of human placental aromatase | B | 4.43 | pIC50 | 37000 | nM | IC50 | J Med Chem (1986) 29: 1362-1369 [PMID:3735304] |
ChEMBL | In vitro inhibitory concentration against human placental Cytochrome P450 19A was determined using [1-beta,2beta-3H]testosterone as radioligand | B | 4.43 | pIC50 | 37000 | nM | IC50 | J Med Chem (1991) 34: 2685-2691 [PMID:1895288] |
ChEMBL | Inhibition of Cytochrome P450 19A1 in human placenta | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (1990) 33: 2673-2679 [PMID:2391706] |
ChEMBL | In vitro inhibition of estrogen production in hamster ovarian tissue | F | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (1991) 34: 725-736 [PMID:1825337] |
ChEMBL | Inhibition of CYP19 | B | 4.53 | pIC50 | 29750 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 1134-1137 [PMID:16380254] |
ChEMBL | Inhibition of aromatase in human placental microsomes | B | 4.53 | pIC50 | 29750 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4713-4715 [PMID:18640836] |
ChEMBL | Inhibition of aromatase in Homo sapiens (human) placental microsome assessed as tritiated H2O release from [1-beta-3H] androstenedione substrate preincubated with substrate for 5 min prior to enzyme addition measured after 20 min by beta-scintillation counting analysis | B | 4.55 | pIC50 | 28500 | nM | IC50 | Med Chem Res (2013) 22: 692-698 |
ChEMBL | Inhibition of Homo sapiens (human) aromatase assessed as 3H2O formation using [1beta,2beta-3H]testosterone as substrate by liquid scintillation counting analysis | B | 4.55 | pIC50 | 28500 | nM | IC50 | Med Chem Res (2011) 20: 661-669 |
ChEMBL | Inhibition of human placental microsome cytochrome P450 19A1 aromatase | B | 4.73 | pIC50 | 18500 | nM | IC50 | J Med Chem (2001) 44: 672-680 [PMID:11262078] |
ChEMBL | Inhibition of Human placental Cytochrome P450 19A1 | B | 4.73 | pIC50 | 18500 | nM | IC50 | J Med Chem (1995) 38: 2103-2111 [PMID:7783141] |
ChEMBL | Inhibition of human placental aromatase, cytochrome P450 19A1 | B | 4.73 | pIC50 | 18500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2105-2108 [PMID:10450990] |
ChEMBL | Inhibition of cytochrome P450 19A1 of human placental microsomes with [1-beta,2beta-3H]testosterone | B | 4.73 | pIC50 | 18500 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1553-1555 [PMID:12699753] |
ChEMBL | Inhibition of human placental cytochrome P450 19A1 with androstenedione | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (1988) 31: 971-976 [PMID:3361583] |
ChEMBL | Inhibition of human placental cytochrome P450 19A1 with androstenedione | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (1987) 30: 1550-1554 [PMID:3625703] |
ChEMBL | In vitro inhibition of estrogen production in hamster ovarian tissue | F | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (1991) 34: 1329-1334 [PMID:2016706] |
ChEMBL | Inhibition of human aromatase transfected in human MCF7 cells | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 5131-5148 [PMID:26689671] |
ChEMBL | Inhibition of human placental aromatase assessed as conversion of [1-beta-3H]androstenedione to [1beta-3H]estrone after 20 mins by liquid scintillation counting | B | 5 | pIC50 | 10000 | nM | IC50 | Eur J Med Chem (2009) 44: 4121-4127 [PMID:19500885] |
ChEMBL | Inhibition of CYP19 in human placental microsome using [1beta-3H]-androstenedione as substrate after 15 mins in presence of NADPH by liquid scintillation counter method | B | 5.05 | pIC50 | 9000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2645-2649 [PMID:28512028] |
ChEMBL | Inhibition of Cytochrome P450 19A1 against Androstenedione at 0.25 uM (Km=55 nM) | B | 5.08 | pIC50 | 8300 | nM | IC50 | J Med Chem (1986) 29: 520-523 [PMID:3754286] |
ChEMBL | Inhibitory activity against human placental cytochrome P450 19A1 | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (1987) 30: 1550-1554 [PMID:3625703] |
ChEMBL | Inhibition of human placental cytochrome P450 19A1 with testosterone | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (1988) 31: 971-976 [PMID:3361583] |
ChEMBL | Inhibition of human CYP19 using [1beta-3H]-androstenedione as substrate after 15 mins in presence of NADPH by liquid scintillation counter method | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2645-2649 [PMID:28512028] |
ChEMBL | Inhibition of aromatase from human placental microsomes | B | 5.19 | pIC50 | 6400 | nM | IC50 | J Nat Prod (2001) 64: 1286-1293 [PMID:11678652] |
ChEMBL | Inhibition of human aromatase in term placenta microsome assessed as radioactivity | B | 5.19 | pIC50 | 6400 | nM | IC50 | Eur J Med Chem (2015) 90: 379-393 [PMID:25461329] |
ChEMBL | Inhibition of Cytochrome P450 19A1 against testosterone at 1.5 uM (Km=0.13 uM) | B | 5.21 | pIC50 | 6130 | nM | IC50 | J Med Chem (1986) 29: 520-523 [PMID:3754286] |
ChEMBL | Inhibition of aromatase in human placental microsomes assessed as inhibition of aromatization of [1,2,6,7-3H] androstenedione by flow scintillation analysis | B | 5.24 | pIC50 | 5800 | nM | IC50 | Eur J Med Chem (2011) 46: 2541-2545 [PMID:21497425] |
ChEMBL | In vitro inhibition of [1,2,6,7-3H]-androstenedione binding to human placental microsome cytochrome P450 19A1 | B | 5.28 | pIC50 | 5200 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1059-1061 [PMID:11909717] |
ChEMBL | Inhibition of aromatase activity in human placental microsomes | B | 5.28 | pIC50 | 5200 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 2859-2861 [PMID:12270163] |
ChEMBL | Inhibitory concentration against human placental aromatase by deutirium oxide release | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4063-4070 [PMID:15911319] |
ChEMBL | Inhibitory concentration against human placental aromatase | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2004) 47: 4032-4040 [PMID:15267241] |
ChEMBL | In vitro inhibition of human placental Cytochrome P450 19A1 | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1993) 36: 1393-1400 [PMID:8496907] |
ChEMBL | In vitro inhibition of cytochrome P450 19A1 Aromatase | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1991) 34: 1329-1334 [PMID:2016706] |
ChEMBL | Inhibition of human placental microsome cytochrome P450 19A1 | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (1991) 34: 725-736 [PMID:1825337] |
ChEMBL | Inhibition of aromatase after 30 mins by fluorescence assay | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2009) 52: 1873-1884 [PMID:19265439] |
ChEMBL | Inhibition of human aromatase | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2007) 50: 2799-2806 [PMID:17511439] |
ChEMBL | Inhibition of human placental microsome CYP19 | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3050-3064 [PMID:20413308] |
CYP19A1/Cytochrome P450 19A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3859] [GtoPdb: 1362] [UniProtKB: P22443] | ||||||||
ChEMBL | Inhibition of rat ovarian Cytochrome P450 19A | B | 4.47 | pIC50 | 34000 | nM | IC50 | J Med Chem (1991) 34: 2685-2691 [PMID:1895288] |
ChEMBL | In vitro inhibition of rat ovarian microsomal Cytochrome P450 19A1 | B | 5.21 | pIC50 | 6200 | nM | IC50 | J Med Chem (1995) 38: 2103-2111 [PMID:7783141] |
ChEMBL | In vitro inhibition of cytochrome P450 19A1 by rat ovarian microsomes incubated with [3H]androstenedione and NADPH-generating system. | B | 6.59 | pEC50 | 260 | nM | EC50 | J Med Chem (1987) 30: 1359-1365 [PMID:3612685] |
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] | ||||||||
ChEMBL | Inhibition of Thromboxane-A synthase | B | 4.73 | pIC50 | 18500 | nM | IC50 | J Med Chem (2000) 43: 1841-1851 [PMID:10794700] |
ChEMBL data shown on this page come from version 32:
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]