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Assay Detail

CHEMBL5546192

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

ADMET
Inhibition of CYP3A4 in human liver microsomes using midazolam substrate incubated for 5 mins in presence of NADPH by UPLC-MS/MS analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
Thomson CG, Aicher TD, Cheng W, Du H, Dudgeon C, Li AH, Li B, Lightcap E, Luo D, Mulvihill M, Pan P, Rahemtulla BF, Rigby AC, Sherborne B, Sood S, Surguladze D, Talbot EPA, Tameire F, Taylor S, Wang Y, Wojnarowicz P, Xiao F, Ramurthy S.
J Med Chem (2024) 67 : 5259 -5271
PubMed 38530741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.94 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571568 1 5.60
CHEMBL5571377 1 5.60
CHEMBL5579682 1 5.29
CHEMBL5574976 1 4.92
CHEMBL5591595 1 4.60
CHEMBL5593998 1 4.57
CHEMBL5593039 1 4.48
CHEMBL5569981 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571568 IC50 = 2500.0 nM 5.60
CHEMBL5571377 IC50 = 2500.0 nM 5.60
CHEMBL5579682 IC50 = 5100.0 nM 5.29
CHEMBL5574976 IC50 = 12000.0 nM 4.92
CHEMBL5591595 IC50 = 25000.0 nM 4.60
CHEMBL5593998 IC50 = 27000.0 nM 4.57
CHEMBL5593039 IC50 = 33000.0 nM 4.48
CHEMBL5569981 IC50 = 33000.0 nM 4.48