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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 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 CYP19 | B | 4.53 | pIC50 | 29750 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 1134-1137 [PMID:16380254] |
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 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 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 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 aromatase in human breast tumor | B | 5 | pIC50 | 10000 | nM | IC50 | Eur J Med Chem (2022) 241: 114658-114658 [PMID:35964426] |
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 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 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 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 aromatase from human placental microsomes | B | 5.19 | pIC50 | 6400 | nM | IC50 | J Nat Prod (2001) 64: 1286-1293 [PMID:11678652] |
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 | 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 | 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 | Inhibitory concentration against human placental aromatase | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2004) 47: 4032-4040 [PMID:15267241] |
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 | 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 | 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 | 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 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]