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Assay Detail

CHEMBL656826

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Functional
Inhibition of multidrug resistance associated protein type 1 (MRP1) assayed by an accumulation assay in COR.L23/R cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Multidrug resistance-associated protein 1 (CHEMBL3004)
Type SINGLE PROTEIN
Organism Homo sapiens

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 30 5.38 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL356478 1 6.40
CHEMBL156947 1 6.30
CHEMBL435437 1 6.05
CHEMBL152590 1 6.00
CHEMBL154003 1 6.00
CHEMBL421980 1 5.98
CHEMBL423413 1 5.88
CHEMBL157318 1 5.82
CHEMBL346486 1 5.81
CHEMBL264490 1 5.70
CHEMBL357064 1 5.55
CHEMBL152157 1 5.54
CHEMBL347672 1 5.50
CHEMBL154004 1 5.48
CHEMBL156894 1 5.42
CHEMBL433715 1 5.35
CHEMBL350775 BIRICODAR 2.0 1 5.29
CHEMBL154596 1 5.20
CHEMBL356477 1 5.14
CHEMBL152447 1 5.12
CHEMBL348567 1 5.00
CHEMBL152651 1 4.82
CHEMBL154430 1 4.73
CHEMBL154490 1 4.44
CHEMBL157162 1 4.43
CHEMBL357996 1 4.41
CHEMBL347213 1 4.02
CHEMBL153452 1 -
CHEMBL345316 1 -
CHEMBL152046 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL356478 IC50 = 400.0 nM 6.40
CHEMBL156947 IC50 = 500.0 nM 6.30
CHEMBL435437 IC50 = 900.0 nM 6.05
CHEMBL152590 IC50 = 1000.0 nM 6.00
CHEMBL154003 IC50 = 1000.0 nM 6.00
CHEMBL421980 IC50 = 1050.0 nM 5.98
CHEMBL423413 IC50 = 1330.0 nM 5.88
CHEMBL157318 IC50 = 1500.0 nM 5.82
CHEMBL346486 IC50 = 1560.0 nM 5.81
CHEMBL264490 IC50 = 2020.0 nM 5.70
CHEMBL357064 IC50 = 2800.0 nM 5.55
CHEMBL152157 IC50 = 2910.0 nM 5.54
CHEMBL347672 IC50 = 3200.0 nM 5.50
CHEMBL154004 IC50 = 3330.0 nM 5.48
CHEMBL156894 IC50 = 3840.0 nM 5.42
CHEMBL433715 IC50 = 4500.0 nM 5.35
CHEMBL350775 BIRICODAR IC50 = 5180.0 nM 5.29
CHEMBL154596 IC50 = 6350.0 nM 5.20
CHEMBL356477 IC50 = 7200.0 nM 5.14
CHEMBL152447 IC50 = 7600.0 nM 5.12
CHEMBL348567 IC50 = 10000.0 nM 5.00
CHEMBL152651 IC50 = 15100.0 nM 4.82
CHEMBL154430 IC50 = 18570.0 nM 4.73
CHEMBL154490 IC50 = 36000.0 nM 4.44
CHEMBL157162 IC50 = 37000.0 nM 4.43
CHEMBL357996 IC50 = 39000.0 nM 4.41
CHEMBL347213 IC50 = 95000.0 nM 4.02
CHEMBL153452 IC50 > 100000.0 nM -
CHEMBL345316 IC50 > 10000.0 nM -
CHEMBL152046 IC50 > 100000.0 nM -