Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL729205

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

ADMET
Inhibition of 1'-hydroxybufuralol formation by human liver microsomes
6
Total Activities
5
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 Expert

Target

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a pharmacophore for inhibition of human liver cytochrome P-450 2D6: molecular modeling and inhibition studies.
Strobl GR, von Kruedener S, Stöckigt J, Guengerich FP, Wolff T.
J Med Chem (1993) 36 : 1136 -1145
PubMed 8487254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.80 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3559672 RAUWOLFIA SERPENTINA 4.0 1 7.89
CHEMBL15245 YOHIMBINE 3.0 1 6.72
CHEMBL428695 1 5.50
CHEMBL2079612 2 5.27
CHEMBL2079610 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3559672 RAUWOLFIA SERPENTINA Ki = 13.0 nM 7.89
CHEMBL15245 YOHIMBINE Ki = 190.0 nM 6.72
CHEMBL428695 Ki = 3200.0 nM 5.50
CHEMBL2079612 Ki = 5400.0 nM 5.27
CHEMBL2079612 Ki = 16000.0 nM 4.80
CHEMBL2079610 Ki = 24000.0 nM 4.62