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Assay Detail

CHEMBL4833550

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

ADMET
Induction of CYP3A4 in human hepatocytes assessed as mRNA expression incubated for 3 days by RT-RTPCR analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy.
Chuang C, Collibee S, Ashcraft L, Wang W, Vander Wal M, Wang X, Hwee DT, Wu Y, Wang J, Chin ER, Cremin P, Zamora J, Hartman J, Schaletzky J, Wehri E, Robertson LA, Malik FI, Morgan BP.
J Med Chem (2021) 64 : 14142 -14152
PubMed 34606259 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 5.66 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297517 MAVACAMTEN 4.0 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297517 MAVACAMTEN EC50 = 2200.0 nM 5.66