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Assay Detail

CHEMBL3532211

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ADMET
Mixed inhibition of CYP2A6 (unknown origin)
7
Total Activities
7
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 2A6 (CHEMBL5282)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Evaluation of inhibition selectivity for human cytochrome P450 2A enzymes.
Stephens ES, Walsh AA, Scott EE.
Drug Metab Dispos (2012) 40 : 1797 -1802
PubMed 22696418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.86 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3989843 TRANYLCYPROMINE 4.0 1 6.89
CHEMBL416 METHOXSALEN 4.0 1 6.60
CHEMBL151649 PHENETHYLISOTHIOCYANATE 1 5.77
CHEMBL3526658 1 5.70
CHEMBL550 PILOCARPINE 4.0 1 5.52
CHEMBL3188333 1 5.44
CHEMBL1522291 NICOTYRINE 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3989843 TRANYLCYPROMINE Ki = 130.0 nM 6.89
CHEMBL416 METHOXSALEN Ki = 250.0 nM 6.60
CHEMBL151649 PHENETHYLISOTHIOCYANATE Ki = 1700.0 nM 5.77
CHEMBL3526658 Ki = 2000.0 nM 5.70
CHEMBL550 PILOCARPINE Ki = 3000.0 nM 5.52
CHEMBL3188333 Ki = 3600.0 nM 5.44
CHEMBL1522291 NICOTYRINE Ki = 7500.0 nM 5.12