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Assay Detail

CHEMBL4725979

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

ADMET
Inhibition of recombinant human CYP3A4
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of BMS-986235/LAR-1219: A Potent Formyl Peptide Receptor 2 (FPR2) Selective Agonist for the Prevention of Heart Failure.
Asahina Y,Wurtz NR,Arakawa K,Carson N,Fujii K,Fukuchi K,Garcia R,Hsu MY,Ishiyama J,Ito B,Kick E,Lupisella J,Matsushima S,Ohata K,Ostrowski J,Saito Y,Tsuda K,Villarreal F,Yamada H,Yamaoka T,Wexler R,Gordon D,Kohno Y
J Med Chem (2020) 63 : 9003 -9019
PubMed 32407089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.25 5.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4760897 1 5.25
CHEMBL4781596 1 -
CHEMBL4784510 BMS-986235 1.0 1 -
CHEMBL4762030 1 -
CHEMBL4790836 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4760897 IC50 = 5600.0 nM 5.25
CHEMBL4781596 IC50 > 20000.0 nM -
CHEMBL4784510 BMS-986235 IC50 > 20000.0 nM -
CHEMBL4762030 IC50 > 20000.0 nM -
CHEMBL4790836 IC50 > 20000.0 nM -