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Assay Detail

CHEMBL829411

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

ADMET
Inhibitory concentration value against human cytochrome P-450 2A6
25
Total Activities
25
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 2A6 (CHEMBL5282)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6.
Denton TT, Zhang X, Cashman JR.
J Med Chem (2005) 48 : 224 -239
PubMed 15634016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.62 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL359657 1 6.77
CHEMBL178090 1 6.57
CHEMBL179669 1 6.21
CHEMBL360999 1 6.12
CHEMBL179399 1 6.12
CHEMBL178781 1 6.00
CHEMBL425519 1 5.89
CHEMBL361153 1 5.85
CHEMBL178534 1 5.85
CHEMBL178780 1 5.85
CHEMBL368883 1 5.82
CHEMBL178516 1 5.82
CHEMBL179704 1 5.82
CHEMBL361364 1 5.51
CHEMBL179529 1 5.46
CHEMBL178681 1 5.43
CHEMBL178330 1 5.38
CHEMBL179398 1 5.32
CHEMBL179005 1 5.24
CHEMBL179763 1 5.18
CHEMBL178711 1 5.13
CHEMBL179618 1 5.11
CHEMBL362702 1 5.07
CHEMBL1795039 1 5.01
CHEMBL178547 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL359657 IC50 = 170.0 nM 6.77
CHEMBL178090 IC50 = 270.0 nM 6.57
CHEMBL179669 IC50 = 620.0 nM 6.21
CHEMBL360999 IC50 = 750.0 nM 6.12
CHEMBL179399 IC50 = 750.0 nM 6.12
CHEMBL178781 IC50 = 1000.0 nM 6.00
CHEMBL425519 IC50 = 1300.0 nM 5.89
CHEMBL361153 IC50 = 1400.0 nM 5.85
CHEMBL178534 IC50 = 1400.0 nM 5.85
CHEMBL178780 IC50 = 1400.0 nM 5.85
CHEMBL368883 IC50 = 1500.0 nM 5.82
CHEMBL178516 IC50 = 1500.0 nM 5.82
CHEMBL179704 IC50 = 1500.0 nM 5.82
CHEMBL361364 IC50 = 3100.0 nM 5.51
CHEMBL179529 IC50 = 3500.0 nM 5.46
CHEMBL178681 IC50 = 3700.0 nM 5.43
CHEMBL178330 IC50 = 4200.0 nM 5.38
CHEMBL179398 IC50 = 4800.0 nM 5.32
CHEMBL179005 IC50 = 5800.0 nM 5.24
CHEMBL179763 IC50 = 6600.0 nM 5.18
CHEMBL178711 IC50 = 7400.0 nM 5.13
CHEMBL179618 IC50 = 7800.0 nM 5.11
CHEMBL362702 IC50 = 8600.0 nM 5.07
CHEMBL1795039 IC50 = 9800.0 nM 5.01
CHEMBL178547 IC50 = 82300.0 nM 4.08