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Assay Detail

CHEMBL970953

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ADMET
Inhibition of human liver microsome CYP3A4 in assessed as [14C]formaldehyde formation
21
Total Activities
21
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

Potent CYP3A4 inhibitory constituents of Piper cubeba.
Usia T, Watabe T, Kadota S, Tezuka Y.
J Nat Prod (2005) 68 : 64 -68
PubMed 15679319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.17 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480295 ETHOXYCLUSIN 1 6.36
CHEMBL157101 KETOCONAZOLE 4.0 1 6.14
CHEMBL469916 1 6.10
CHEMBL482233 1 6.08
CHEMBL479701 1 6.08
CHEMBL471067 1 6.00
CHEMBL469917 1 5.96
CHEMBL482034 1 5.13
CHEMBL520915 1 5.11
CHEMBL242011 HINOKININ 1 5.10
CHEMBL501260 1 5.06
CHEMBL399831 1 5.04
CHEMBL486597 DIHYDROCUBEBIN 1 5.02
CHEMBL513023 MEDIORESINOL 1 4.86
CHEMBL479314 1 4.83
CHEMBL480296 1 4.82
CHEMBL481233 1 4.54
CHEMBL450829 1 4.13
CHEMBL156339 MAGNOSALIN 1 4.07
CHEMBL333306 TRANS-ASARONE 1 4.04
CHEMBL501119 1 4.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480295 ETHOXYCLUSIN IC50 = 440.0 nM 6.36
CHEMBL157101 KETOCONAZOLE IC50 = 720.0 nM 6.14
CHEMBL469916 IC50 = 800.0 nM 6.10
CHEMBL482233 IC50 = 830.0 nM 6.08
CHEMBL479701 IC50 = 830.0 nM 6.08
CHEMBL471067 IC50 = 1000.0 nM 6.00
CHEMBL469917 IC50 = 1100.0 nM 5.96
CHEMBL482034 IC50 = 7400.0 nM 5.13
CHEMBL520915 IC50 = 7700.0 nM 5.11
CHEMBL242011 HINOKININ IC50 = 8000.0 nM 5.10
CHEMBL501260 IC50 = 8800.0 nM 5.06
CHEMBL399831 IC50 = 9100.0 nM 5.04
CHEMBL486597 DIHYDROCUBEBIN IC50 = 9500.0 nM 5.02
CHEMBL513023 MEDIORESINOL IC50 = 13700.0 nM 4.86
CHEMBL479314 IC50 = 14900.0 nM 4.83
CHEMBL480296 IC50 = 15000.0 nM 4.82
CHEMBL481233 IC50 = 28700.0 nM 4.54
CHEMBL450829 IC50 = 74000.0 nM 4.13
CHEMBL156339 MAGNOSALIN IC50 = 85400.0 nM 4.07
CHEMBL333306 TRANS-ASARONE IC50 = 92300.0 nM 4.04
CHEMBL501119 IC50 = 98200.0 nM 4.01