aminoglutethimide [Ligand Id: 7054] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL488 (Aminoglutethimide, Cytadren, NSC-330915, Orimeten)
  • CYP11A1/Cytochrome P450 11A1 in Human [ChEMBL: CHEMBL2033] [GtoPdb: 1358] [UniProtKB: P05108]
  • Cytochrome P450 11A1 in Bovine [ChEMBL: CHEMBL4813] [UniProtKB: P00189]
  • CYP11A1 in Hamster [GtoPdb: 1358]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]