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Assay Detail

CHEMBL832851

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

Binding
Potency towards cytochrome P 450 26 enzyme activity
31
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cytochrome P450 26A1 (CHEMBL5141)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs).
Mulvihill MJ, Kan JL, Beck P, Bittner M, Cesario C, Cooke A, Keane DM, Nigro AI, Nillson C, Smith V, Srebernak M, Sun FL, Vrkljan M, Winski SL, Castelhano AL, Emerson D, Gibson N.
Bioorg Med Chem Lett (2005) 15 : 1669 -1673
PubMed 15745819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.47 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL368448 2 8.48
CHEMBL426789 2 8.46
CHEMBL359627 2 8.22
CHEMBL181309 2 8.15
CHEMBL179550 1 8.10
CHEMBL360072 1 7.84
CHEMBL178474 2 7.80
CHEMBL362412 2 7.72
CHEMBL360771 2 7.70
CHEMBL180805 2 7.67
CHEMBL180348 1 7.60
CHEMBL181385 2 7.47
CHEMBL367357 1 7.46
CHEMBL182438 1 7.43
CHEMBL362489 1 7.33
CHEMBL360148 1 7.32
CHEMBL180856 1 7.30
CHEMBL180829 1 7.27
CHEMBL180592 1 7.11
CHEMBL179825 1 7.00
CHEMBL178873 1 6.47
CHEMBL389433 LIAROZOLE 2.0 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL368448 IC50 = 3.3 nM 8.48
CHEMBL426789 IC50 = 3.5 nM 8.46
CHEMBL359627 IC50 = 6.0 nM 8.22
CHEMBL426789 IC50 = 6.3 nM 8.20
CHEMBL181309 IC50 = 7.0 nM 8.15
CHEMBL179550 IC50 = 8.0 nM 8.10
CHEMBL368448 IC50 = 12.0 nM 7.92
CHEMBL360072 IC50 = 14.4 nM 7.84
CHEMBL178474 IC50 = 16.0 nM 7.80
CHEMBL181309 IC50 = 18.0 nM 7.75
CHEMBL362412 IC50 = 19.0 nM 7.72
CHEMBL360771 IC50 = 20.0 nM 7.70
CHEMBL180805 IC50 = 21.4 nM 7.67
CHEMBL180348 IC50 = 25.0 nM 7.60
CHEMBL181385 IC50 = 34.0 nM 7.47
CHEMBL367357 IC50 = 35.0 nM 7.46
CHEMBL182438 IC50 = 37.0 nM 7.43
CHEMBL360771 IC50 = 46.0 nM 7.34
CHEMBL362489 IC50 = 47.0 nM 7.33
CHEMBL360148 IC50 = 48.0 nM 7.32
CHEMBL180856 IC50 = 50.0 nM 7.30
CHEMBL180829 IC50 = 54.0 nM 7.27
CHEMBL359627 IC50 = 71.0 nM 7.15
CHEMBL180805 IC50 = 73.0 nM 7.14
CHEMBL180592 IC50 = 77.0 nM 7.11
CHEMBL178474 IC50 = 85.0 nM 7.07
CHEMBL181385 IC50 = 86.0 nM 7.07
CHEMBL179825 IC50 = 100.0 nM 7.00
CHEMBL362412 IC50 = 153.0 nM 6.82
CHEMBL178873 IC50 = 335.0 nM 6.47
CHEMBL389433 LIAROZOLE IC50 = 6000.0 nM 5.22