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Assay Detail

CHEMBL885077

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

Binding
50% in vitro inhibitory concentration against Cytochrome P450 19A1 from human placental microsomes by thiobarbituric acid assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Microsome
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
Jacobs C, Frotscher M, Dannhardt G, Hartmann RW.
J Med Chem (2000) 43 : 1841 -1851
PubMed 10794700 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.05 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300109 1 6.80
CHEMBL53068 1 6.77
CHEMBL53290 1 6.66
CHEMBL54803 1 6.46
CHEMBL301106 1 6.46
CHEMBL292899 1 6.42
CHEMBL291700 1 6.36
CHEMBL293122 1 6.30
CHEMBL57513 1 6.17
CHEMBL53644 1 6.16
CHEMBL55144 1 6.04
CHEMBL298720 1 5.86
CHEMBL55083 1 5.62
CHEMBL299066 1 5.51
CHEMBL460382 1 5.45
CHEMBL55558 1 5.41
CHEMBL56059 1 5.22
CHEMBL52509 1 5.19
CHEMBL301608 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300109 IC50 = 160.0 nM 6.80
CHEMBL53068 IC50 = 170.0 nM 6.77
CHEMBL53290 IC50 = 220.0 nM 6.66
CHEMBL54803 IC50 = 350.0 nM 6.46
CHEMBL301106 IC50 = 350.0 nM 6.46
CHEMBL292899 IC50 = 380.0 nM 6.42
CHEMBL291700 IC50 = 440.0 nM 6.36
CHEMBL293122 IC50 = 500.0 nM 6.30
CHEMBL57513 IC50 = 680.0 nM 6.17
CHEMBL53644 IC50 = 700.0 nM 6.16
CHEMBL55144 IC50 = 920.0 nM 6.04
CHEMBL298720 IC50 = 1380.0 nM 5.86
CHEMBL55083 IC50 = 2400.0 nM 5.62
CHEMBL299066 IC50 = 3060.0 nM 5.51
CHEMBL460382 IC50 = 3560.0 nM 5.45
CHEMBL55558 IC50 = 3900.0 nM 5.41
CHEMBL56059 IC50 = 6000.0 nM 5.22
CHEMBL52509 IC50 = 6400.0 nM 5.19
CHEMBL301608 IC50 = 111000.0 nM -