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Assay Detail

CHEMBL5520754

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

ADMET
Inhibition of human CYP3A4 incubated for 60 mins by red fluorescent-probe-based microsomal assay
2
Total Activities
2
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

Hit-to-Lead Identification and Validation of a Triaromatic Pleuromutilin Antibiotic Candidate.
Heidtmann CV, Fejer AR, Stærk K, Pedersen M, Asmussen MG, Hertz FB, Prabhala BK, Frimodt-Møller N, Klitgaard JK, Andersen TE, Nielsen CU, Nielsen P.
J Med Chem (2024) 67 : 3692 -3710
PubMed 38385364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.26 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5561773 1 6.39
CHEMBL3291398 LEFAMULIN 4.0 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5561773 IC50 = 410.0 nM 6.39
CHEMBL3291398 LEFAMULIN IC50 = 750.0 nM 6.12