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Assay Detail

CHEMBL695682

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

Functional
In vitro for its inhibitory activity against MRP1-transfected HeLa-T5 cell line in the presence of doxorubicin
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa-T5
Confidence 9 — Direct single protein target
Curated By Expert

Target

ATP-dependent translocase ABCB1 (CHEMBL4302)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1).
Norman BH, Gruber JM, Hollinshead SP, Wilson JW, Starling JJ, Law KL, Self TD, Tabas LB, Williams DC, Paul DC, Wagner MM, Dantzig AH.
Bioorg Med Chem Lett (2002) 12 : 883 -886
PubMed 11958985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.62 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL168831 1 6.19
CHEMBL172119 1 6.05
CHEMBL554924 1 5.95
CHEMBL354935 1 5.89
CHEMBL434490 1 5.83
CHEMBL171614 1 5.75
CHEMBL170624 1 5.75
CHEMBL170699 1 5.68
CHEMBL355346 1 5.64
CHEMBL169765 1 5.50
CHEMBL169857 1 5.43
CHEMBL354544 1 5.40
CHEMBL434871 1 5.39
CHEMBL172059 1 5.31
CHEMBL170545 1 5.10
CHEMBL169803 1 5.00
CHEMBL171087 1 -
CHEMBL171665 1 -
CHEMBL171726 1 -
CHEMBL352527 1 -
CHEMBL354369 1 -
CHEMBL354582 1 -
CHEMBL355843 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL168831 EC50 = 640.0 nM 6.19
CHEMBL172119 EC50 = 900.0 nM 6.05
CHEMBL554924 EC50 = 1130.0 nM 5.95
CHEMBL354935 EC50 = 1300.0 nM 5.89
CHEMBL434490 EC50 = 1470.0 nM 5.83
CHEMBL171614 EC50 = 1800.0 nM 5.75
CHEMBL170624 EC50 = 1770.0 nM 5.75
CHEMBL170699 EC50 = 2100.0 nM 5.68
CHEMBL355346 EC50 = 2300.0 nM 5.64
CHEMBL169765 EC50 = 3200.0 nM 5.50
CHEMBL169857 EC50 = 3700.0 nM 5.43
CHEMBL354544 EC50 = 4000.0 nM 5.40
CHEMBL434871 EC50 = 4100.0 nM 5.39
CHEMBL172059 EC50 = 4900.0 nM 5.31
CHEMBL170545 EC50 = 7900.0 nM 5.10
CHEMBL169803 EC50 = 10000.0 nM 5.00
CHEMBL171087 EC50 > 10000.0 nM -
CHEMBL171665 EC50 >> 10000.0 nM -
CHEMBL171726 EC50 >> 10000.0 nM -
CHEMBL352527 EC50 > 10000.0 nM -
CHEMBL354369 EC50 > 10000.0 nM -
CHEMBL354582 EC50 > 10000.0 nM -
CHEMBL355843 EC50 > 10000.0 nM -