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Assay Detail

CHEMBL675690

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

Functional
Inhibitory activity against P-glycoprotein (Pgp) using accumulation assay for Pgp expressing EMT6/AR1.0 cells.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

ATP-dependent translocase ABCB1 (CHEMBL3467)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug resistance.
Wang S, Ryder H, Pretswell I, Depledge P, Milton J, Hancox TC, Dale I, Dangerfield W, Charlton P, Faint R, Dodd R, Hassan S.
Bioorg Med Chem Lett (2002) 12 : 571 -574
PubMed 11844674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.71 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL152651 1 7.30
CHEMBL156894 1 6.80
CHEMBL154490 1 6.41
CHEMBL356478 1 6.22
CHEMBL154596 1 6.20
CHEMBL152590 1 6.10
CHEMBL435437 1 6.07
CHEMBL156947 1 6.00
CHEMBL154003 1 5.99
CHEMBL152157 1 5.97
CHEMBL421980 1 5.97
CHEMBL264490 1 5.96
CHEMBL345316 1 5.89
CHEMBL423413 1 5.87
CHEMBL433715 1 5.80
CHEMBL346486 1 5.77
CHEMBL157162 1 5.72
CHEMBL152447 1 5.70
CHEMBL357996 1 5.68
CHEMBL157318 1 5.43
CHEMBL356477 1 5.38
CHEMBL350775 BIRICODAR 2.0 1 5.30
CHEMBL347672 1 5.30
CHEMBL154430 1 5.14
CHEMBL357064 1 5.10
CHEMBL154004 1 5.00
CHEMBL348567 1 4.85
CHEMBL152046 1 4.40
CHEMBL153452 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL152651 IC50 = 50.0 nM 7.30
CHEMBL156894 IC50 = 160.0 nM 6.80
CHEMBL154490 IC50 = 390.0 nM 6.41
CHEMBL356478 IC50 = 600.0 nM 6.22
CHEMBL154596 IC50 = 630.0 nM 6.20
CHEMBL152590 IC50 = 800.0 nM 6.10
CHEMBL435437 IC50 = 850.0 nM 6.07
CHEMBL156947 IC50 = 1000.0 nM 6.00
CHEMBL154003 IC50 = 1030.0 nM 5.99
CHEMBL152157 IC50 = 1060.0 nM 5.97
CHEMBL421980 IC50 = 1070.0 nM 5.97
CHEMBL264490 IC50 = 1100.0 nM 5.96
CHEMBL345316 IC50 = 1300.0 nM 5.89
CHEMBL423413 IC50 = 1350.0 nM 5.87
CHEMBL433715 IC50 = 1600.0 nM 5.80
CHEMBL346486 IC50 = 1700.0 nM 5.77
CHEMBL157162 IC50 = 1900.0 nM 5.72
CHEMBL152447 IC50 = 2000.0 nM 5.70
CHEMBL357996 IC50 = 2100.0 nM 5.68
CHEMBL157318 IC50 = 3700.0 nM 5.43
CHEMBL356477 IC50 = 4200.0 nM 5.38
CHEMBL350775 BIRICODAR IC50 = 5000.0 nM 5.30
CHEMBL347672 IC50 = 5000.0 nM 5.30
CHEMBL154430 IC50 = 7200.0 nM 5.14
CHEMBL357064 IC50 = 8000.0 nM 5.10
CHEMBL154004 IC50 = 10000.0 nM 5.00
CHEMBL348567 IC50 = 14000.0 nM 4.85
CHEMBL152046 IC50 = 40000.0 nM 4.40
CHEMBL153452 IC50 = 41000.0 nM 4.39