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Assay Detail

CHEMBL880272

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory concentration against human placental cytochrome P450 19A1 using [1-beta-3H]-androstenedione as substrate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
Voets M, Antes I, Scherer C, Müller-Vieira U, Biemel K, Barassin C, Marchais-Oberwinkler S, Hartmann RW.
J Med Chem (2005) 48 : 6632 -6642
PubMed 16220979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.93 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9298 FADROZOLE 2.0 1 7.52
CHEMBL194472 1 6.89
CHEMBL362968 1 6.23
CHEMBL381014 1 6.01
CHEMBL438802 1 5.90
CHEMBL197576 1 5.74
CHEMBL195996 1 5.55
CHEMBL365735 1 5.24
CHEMBL193343 1 5.18
CHEMBL196328 1 5.04
CHEMBL195571 1 -
CHEMBL193534 1 -
CHEMBL196796 1 -
CHEMBL371430 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9298 FADROZOLE IC50 = 30.0 nM 7.52
CHEMBL194472 IC50 = 129.0 nM 6.89
CHEMBL362968 IC50 = 586.0 nM 6.23
CHEMBL381014 IC50 = 970.0 nM 6.01
CHEMBL438802 IC50 = 1252.0 nM 5.90
CHEMBL197576 IC50 = 1805.0 nM 5.74
CHEMBL195996 IC50 = 2821.0 nM 5.55
CHEMBL365735 IC50 = 5727.0 nM 5.24
CHEMBL193343 IC50 = 6638.0 nM 5.18
CHEMBL196328 IC50 = 9107.0 nM 5.04
CHEMBL195571 IC50 > 36000.0 nM -
CHEMBL193534 IC50 > 36000.0 nM -
CHEMBL196796 IC50 > 36000.0 nM -
CHEMBL371430 IC50 > 36000.0 nM -