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Assay Detail

CHEMBL4187019

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

ADMET
Inhibition of CYP2C19 in human liver microsomes by LC-MS/MS analysis
2
Total Activities
2
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

Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist.
Clarke E, Jarvis CI, Goncalves MB, Kalindjian SB, Adams DR, Brown JT, Shiers JJ, Taddei DMA, Ravier E, Barlow S, Miller I, Smith V, Borthwick AD, Corcoran JPT.
Bioorg Med Chem (2018) 26 : 798 -814
PubMed 29288071 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.60 4.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107430 NRX195183 2.0 1 4.60
CHEMBL4202767 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107430 NRX195183 IC50 = 25000.0 nM 4.60
CHEMBL4202767 IC50 > 25000.0 nM -