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

CHEMBL3541097

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

ADMET
Inhibition of CYP2C19 in human liver microsomes using omeprazole substrate by LC-MS/MS method
20
Total Activities
20
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 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
Ren S, Zeng J, Mei Y, Zhang JZ, Yan SF, Fei J, Chen L.
Drug Metab Dispos (2013) 41 : 60 -71
PubMed 23033255 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.97 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1484 NICARDIPINE 4.0 1 6.25
CHEMBL45816 MIBEFRADIL 4.0 1 5.88
CHEMBL1428 NIMODIPINE 4.0 1 5.66
CHEMBL193 NIFEDIPINE 4.0 1 5.27
CHEMBL388590 BENZBROMARONE 4.0 1 4.74
CHEMBL567 PERPHENAZINE 4.0 1 4.73
CHEMBL6966 VERAPAMIL 4.0 1 4.66
CHEMBL809 SERTRALINE 4.0 1 4.65
CHEMBL833 TICLOPIDINE 4.0 1 4.55
CHEMBL1008 BEPRIDIL 4.0 1 4.49
CHEMBL71 CHLORPROMAZINE 4.0 1 4.47
CHEMBL42 CLOZAPINE 4.0 1 4.34
CHEMBL1017 TELMISARTAN 4.0 1 -
CHEMBL161 CEFTRIAXONE 4.0 1 -
CHEMBL30008 FLUNARIZINE 2.0 1 -
CHEMBL682 AMODIAQUINE 4.0 1 -
CHEMBL9 NORFLOXACIN 4.0 1 -
CHEMBL54 HALOPERIDOL 4.0 1 -
CHEMBL13 METOPROLOL 4.0 1 -
CHEMBL1451 TRIAMCINOLONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1484 NICARDIPINE IC50 = 560.0 nM 6.25
CHEMBL45816 MIBEFRADIL IC50 = 1320.0 nM 5.88
CHEMBL1428 NIMODIPINE IC50 = 2170.0 nM 5.66
CHEMBL193 NIFEDIPINE IC50 = 5420.0 nM 5.27
CHEMBL388590 BENZBROMARONE IC50 = 18200.0 nM 4.74
CHEMBL567 PERPHENAZINE IC50 = 18500.0 nM 4.73
CHEMBL6966 VERAPAMIL IC50 = 21800.0 nM 4.66
CHEMBL809 SERTRALINE IC50 = 22500.0 nM 4.65
CHEMBL833 TICLOPIDINE IC50 = 28400.0 nM 4.55
CHEMBL1008 BEPRIDIL IC50 = 32200.0 nM 4.49
CHEMBL71 CHLORPROMAZINE IC50 = 34100.0 nM 4.47
CHEMBL42 CLOZAPINE IC50 = 45300.0 nM 4.34
CHEMBL1017 TELMISARTAN IC50 > 50000.0 nM -
CHEMBL161 CEFTRIAXONE IC50 > 50000.0 nM -
CHEMBL30008 FLUNARIZINE IC50 > 50000.0 nM -
CHEMBL682 AMODIAQUINE IC50 > 50000.0 nM -
CHEMBL9 NORFLOXACIN IC50 > 50000.0 nM -
CHEMBL54 HALOPERIDOL IC50 > 50000.0 nM -
CHEMBL13 METOPROLOL IC50 > 50000.0 nM -
CHEMBL1451 TRIAMCINOLONE IC50 > 50000.0 nM -