Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3107752

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

ADMET
Inhibition of CYP3A4 in human liver microsomes assessed as 6beta-hydroxylation of testosterone
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Tissue Liver
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.
Keenan M, Chaplin JH, Alexander PW, Abbott MJ, Best WM, Khong A, Botero A, Perez C, Cornwall S, Thompson RA, White KL, Shackleford DM, Koltun M, Chiu FC, Morizzi J, Ryan E, Campbell M, von Geldern TW, Scandale I, Chatelain E, Charman SA.
J Med Chem (2013) 56 : 10158 -10170
PubMed 24304150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.99 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3104490 1 5.40
CHEMBL3104537 1 5.28
CHEMBL3104479 1 5.20
CHEMBL3104488 1 5.16
CHEMBL3104478 1 4.92
CHEMBL3104526 1 4.82
CHEMBL3104376 1 4.80
CHEMBL3104473 1 4.80
CHEMBL3104525 1 4.77
CHEMBL3104534 1 4.75
CHEMBL3104375 1 -
CHEMBL3104374 1 -
CHEMBL3104472 1 -
CHEMBL3104476 1 -
CHEMBL3104485 1 -
CHEMBL3104486 1 -
CHEMBL3104487 1 -
CHEMBL3104489 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3104490 IC50 = 4000.0 nM 5.40
CHEMBL3104537 IC50 = 5200.0 nM 5.28
CHEMBL3104479 IC50 = 6300.0 nM 5.20
CHEMBL3104488 IC50 = 7000.0 nM 5.16
CHEMBL3104478 IC50 = 12000.0 nM 4.92
CHEMBL3104526 IC50 = 15000.0 nM 4.82
CHEMBL3104376 IC50 = 16000.0 nM 4.80
CHEMBL3104473 IC50 = 16000.0 nM 4.80
CHEMBL3104525 IC50 = 17000.0 nM 4.77
CHEMBL3104534 IC50 = 18000.0 nM 4.75
CHEMBL3104375 IC50 > 20000.0 nM -
CHEMBL3104374 IC50 > 20000.0 nM -
CHEMBL3104472 IC50 > 20000.0 nM -
CHEMBL3104476 IC50 > 20000.0 nM -
CHEMBL3104485 IC50 > 20000.0 nM -
CHEMBL3104486 IC50 > 20000.0 nM -
CHEMBL3104487 IC50 > 20000.0 nM -
CHEMBL3104489 IC50 > 20000.0 nM -