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Assay Detail

CHEMBL3532205

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

ADMET
Binding affinity to CYP2A6 (unknown origin) assessed as type 1 interaction as increase in absorbance 379 to 387 nm and decrease in 414 to 420 nm
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 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
Kd 6 5.17 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3188333 1 6.17
CHEMBL3526658 1 5.35
CHEMBL151649 PHENETHYLISOTHIOCYANATE 1 5.21
CHEMBL416 METHOXSALEN 4.0 1 4.96
CHEMBL1522291 NICOTYRINE 1 4.15
CHEMBL3 NICOTINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3188333 Kd = 680.0 nM 6.17
CHEMBL3526658 Kd = 4500.0 nM 5.35
CHEMBL151649 PHENETHYLISOTHIOCYANATE Kd = 6200.0 nM 5.21
CHEMBL416 METHOXSALEN Kd = 11000.0 nM 4.96
CHEMBL1522291 NICOTYRINE Kd = 71000.0 nM 4.15
CHEMBL3 NICOTINE Kd = 470000.0 nM -