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Assay Detail

CHEMBL5104733

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

ADMET
Induction of CYP3A4 in human hepatocytes
2
Total Activities
2
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

Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.
Hao J, Beck J, Zhou X, Lackner GL, Johnston R, Reinhard M, Goldsmith P, Hollinshead S, Dehlinger V, Filla SA, Wang XS, Richardson J, Posada M, Mohutsky M, Schober D, Katner JS, Chen Q, Hu B, Remick DM, Coates DA, Mathes BM, Hawk MK, Svensson KA, Hembre E.
J Med Chem (2022) 65 : 3786 -3797
PubMed 35175768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.38 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4468760 1 5.50
CHEMBL3421729 MEVIDALEN 2.0 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4468760 EC50 = 3200.0 nM 5.50
CHEMBL3421729 MEVIDALEN EC50 = 5500.0 nM 5.26