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Assay Detail

CHEMBL758056

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

ADMET
Inhibition of partially purified cytochrome P450 2D6 1'-hydroxybufuralol formation
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
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 5 5.73 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1294 QUINIDINE 4.0 1 7.37
CHEMBL15245 YOHIMBINE 3.0 1 6.28
CHEMBL2079612 2 5.58
CHEMBL170 QUININE 4.0 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1294 QUINIDINE Ki = 43.0 nM 7.37
CHEMBL15245 YOHIMBINE Ki = 520.0 nM 6.28
CHEMBL2079612 Ki = 2600.0 nM 5.58
CHEMBL170 QUININE Ki = 15000.0 nM 4.82
CHEMBL2079612 Ki = 25000.0 nM 4.60