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

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ChEMBL ligand: CHEMBL488 (Cytadren, Orimeten, Aminoglutethimide)
  • 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]
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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 26:

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]