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Assay Detail

CHEMBL1000805

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ADMET
Inhibition of human CYP3A4 by radiometric assay
19
Total Activities
19
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

Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities.
Usia T, Iwata H, Hiratsuka A, Watabe T, Kadota S, Tezuka Y.
J Nat Prod (2004) 67 : 1079 -1083
PubMed 15270556 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 4.52 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157101 KETOCONAZOLE 4.0 1 6.61
CHEMBL519761 1 4.84
CHEMBL240954 1 4.69
CHEMBL245412 ZERUMBONE 1 4.66
CHEMBL309061 ERMANIN 1 4.66
CHEMBL471074 1 4.50
CHEMBL469850 1 4.45
CHEMBL165064 ISOKAEMPFERIDE 1 4.44
CHEMBL471072 1 4.44
CHEMBL513372 1 4.37
CHEMBL512339 ZERUMBONE EPOXIDE 1 4.32
CHEMBL469851 1 4.25
CHEMBL469431 1 4.23
CHEMBL503727 1 4.20
CHEMBL25948 SHOGAOL 1 4.11
CHEMBL470049 1 4.05
CHEMBL470048 1 4.01
CHEMBL240528 AFZELIN 1 -
CHEMBL221542 BETA-SITOSTEROL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157101 KETOCONAZOLE IC50 = 245.0 nM 6.61
CHEMBL519761 IC50 = 14400.0 nM 4.84
CHEMBL240954 IC50 = 20600.0 nM 4.69
CHEMBL245412 ZERUMBONE IC50 = 21800.0 nM 4.66
CHEMBL309061 ERMANIN IC50 = 21800.0 nM 4.66
CHEMBL471074 IC50 = 31600.0 nM 4.50
CHEMBL469850 IC50 = 35500.0 nM 4.45
CHEMBL165064 ISOKAEMPFERIDE IC50 = 36200.0 nM 4.44
CHEMBL471072 IC50 = 36400.0 nM 4.44
CHEMBL513372 IC50 = 42600.0 nM 4.37
CHEMBL512339 ZERUMBONE EPOXIDE IC50 = 48400.0 nM 4.32
CHEMBL469851 IC50 = 55800.0 nM 4.25
CHEMBL469431 IC50 = 59000.0 nM 4.23
CHEMBL503727 IC50 = 62500.0 nM 4.20
CHEMBL25948 SHOGAOL IC50 = 77700.0 nM 4.11
CHEMBL470049 IC50 = 90000.0 nM 4.05
CHEMBL470048 IC50 = 98300.0 nM 4.01
CHEMBL240528 AFZELIN IC50 > 100000.0 nM -
CHEMBL221542 BETA-SITOSTEROL IC50 > 100000.0 nM -