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Assay Detail

CHEMBL1029448

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

ADMET
Inhibition of human CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline
15
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective cytochrome P450 3A4 inhibitory activity of Amaryllidaceae alkaloids.
McNulty J, Nair JJ, Singh M, Crankshaw DJ, Holloway AC, Bastida J.
Bioorg Med Chem Lett (2009) 19 : 3233 -3237
PubMed 19428250 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.21 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157101 KETOCONAZOLE 4.0 2 7.62
CHEMBL564408 2 6.80
CHEMBL558873 2 6.60
CHEMBL98745 NARCICLASINE 2 6.20
CHEMBL251077 2 5.12
CHEMBL465295 2 5.00
CHEMBL659 GALANTAMINE 4.0 1 -
CHEMBL400092 LYCORINE 1 -
CHEMBL419335 PANCRATISTATIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157101 KETOCONAZOLE Ki = 24.0 nM 7.62
CHEMBL157101 KETOCONAZOLE Ki = 25.12 nM 7.60
CHEMBL564408 Ki = 158.49 nM 6.80
CHEMBL564408 Ki = 210.0 nM 6.68
CHEMBL558873 Ki = 251.19 nM 6.60
CHEMBL558873 Ki = 260.0 nM 6.58
CHEMBL98745 NARCICLASINE Ki = 630.0 nM 6.20
CHEMBL98745 NARCICLASINE Ki = 630.96 nM 6.20
CHEMBL251077 Ki = 7600.0 nM 5.12
CHEMBL251077 Ki = 7943.28 nM 5.10
CHEMBL465295 Ki = 10000.0 nM 5.00
CHEMBL465295 Ki = 11000.0 nM 4.96
CHEMBL659 GALANTAMINE Ki - -
CHEMBL400092 LYCORINE Ki - -
CHEMBL419335 PANCRATISTATIN Ki - -