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Assay Detail

CHEMBL832148

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

ADMET
Inhibitory activity against recombinant human Cytochrome P450 2D6 (CYP2D6) after incubated for 45 minutes
36
Total Activities
36
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 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series.
Vaz RJ, Nayeem A, Santone K, Chandrasena G, Gavai AV.
Bioorg Med Chem Lett (2005) 15 : 3816 -3820
PubMed 15993593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.22 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95499 1 7.52
CHEMBL179332 1 7.52
CHEMBL435551 1 7.52
CHEMBL367605 1 7.40
CHEMBL181322 1 7.40
CHEMBL178206 1 7.40
CHEMBL321582 BUCINDOLOL 2.0 1 7.30
CHEMBL179338 1 7.30
CHEMBL178100 1 7.30
CHEMBL361947 1 7.30
CHEMBL317164 1 7.30
CHEMBL180620 1 7.16
CHEMBL426596 1 7.10
CHEMBL361365 1 7.05
CHEMBL361646 1 6.96
CHEMBL180922 1 6.92
CHEMBL180975 1 6.92
CHEMBL178201 1 6.55
CHEMBL440203 1 6.51
CHEMBL182195 1 6.46
CHEMBL178963 1 6.38
CHEMBL426605 1 6.17
CHEMBL27 PROPRANOLOL 4.0 1 5.72
CHEMBL360757 1 5.68
CHEMBL178125 1 5.42
CHEMBL181620 1 5.32
CHEMBL360096 1 5.08
CHEMBL499 TIMOLOL 4.0 1 4.96
CHEMBL181895 1 4.92
CHEMBL7154 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95499 IC50 = 30.0 nM 7.52
CHEMBL435551 IC50 = 30.0 nM 7.52
CHEMBL179332 IC50 = 30.0 nM 7.52
CHEMBL367605 IC50 = 40.0 nM 7.40
CHEMBL181322 IC50 = 40.0 nM 7.40
CHEMBL178206 IC50 = 40.0 nM 7.40
CHEMBL317164 IC50 = 50.0 nM 7.30
CHEMBL361947 IC50 = 50.0 nM 7.30
CHEMBL178100 IC50 = 50.0 nM 7.30
CHEMBL179338 IC50 = 50.0 nM 7.30
CHEMBL321582 BUCINDOLOL IC50 = 50.0 nM 7.30
CHEMBL180620 IC50 = 70.0 nM 7.16
CHEMBL426596 IC50 = 80.0 nM 7.10
CHEMBL361365 IC50 = 90.0 nM 7.05
CHEMBL361646 IC50 = 110.0 nM 6.96
CHEMBL180922 IC50 = 120.0 nM 6.92
CHEMBL180975 IC50 = 120.0 nM 6.92
CHEMBL178201 IC50 = 280.0 nM 6.55
CHEMBL440203 IC50 = 310.0 nM 6.51
CHEMBL182195 IC50 = 350.0 nM 6.46
CHEMBL178963 IC50 = 420.0 nM 6.38
CHEMBL426605 IC50 = 670.0 nM 6.17
CHEMBL27 PROPRANOLOL IC50 = 1900.0 nM 5.72
CHEMBL360757 IC50 = 2100.0 nM 5.68
CHEMBL178125 IC50 = 3800.0 nM 5.42
CHEMBL181620 IC50 = 4800.0 nM 5.32
CHEMBL360096 IC50 = 8400.0 nM 5.08
CHEMBL499 TIMOLOL IC50 = 11000.0 nM 4.96
CHEMBL181895 IC50 = 12000.0 nM 4.92
CHEMBL7154 IC50 = 18000.0 nM 4.75
CHEMBL180678 IC50 = 21000.0 nM 4.68
CHEMBL178501 IC50 = 21000.0 nM 4.68
CHEMBL13 METOPROLOL IC50 = 24000.0 nM 4.62
CHEMBL180767 IC50 = 28000.0 nM 4.55
CHEMBL423 BETAXOLOL IC50 = 66000.0 nM 4.18
CHEMBL359496 IC50 = 100000.0 nM 4.00