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Assay Detail

CHEMBL754768

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ADMET
Inhibitory constant for cytochrome P450 2D6
6
Total Activities
6
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 6 7.15 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3559672 RAUWOLFIA SERPENTINA 4.0 1 8.48
CHEMBL277382 PRODIPINE 2.0 1 8.32
CHEMBL1294 QUINIDINE 4.0 1 7.22
CHEMBL122270 LOBELINE 2.0 1 6.92
CHEMBL15023 TRIFLUPERIDOL 2.0 1 6.77
CHEMBL71 CHLORPROMAZINE 4.0 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3559672 RAUWOLFIA SERPENTINA Ki = 3.3 nM 8.48
CHEMBL277382 PRODIPINE Ki = 4.8 nM 8.32
CHEMBL1294 QUINIDINE Ki = 60.0 nM 7.22
CHEMBL122270 LOBELINE Ki = 120.0 nM 6.92
CHEMBL15023 TRIFLUPERIDOL Ki = 170.0 nM 6.77
CHEMBL71 CHLORPROMAZINE Ki = 7000.0 nM 5.16