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Assay Detail

CHEMBL1219905

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

Binding
Inhibition of MDR1 expressed in MDCK cells assessed as calcein AM accumulation by fluorescence assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type MDCK
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Phenylsulfonylfuroxans as modulators of multidrug-resistance-associated protein-1 and P-glycoprotein.
Fruttero R, Crosetti M, Chegaev K, Guglielmo S, Gasco A, Berardi F, Niso M, Perrone R, Panaro MA, Colabufo NA.
J Med Chem (2010) 53 : 5467 -5475
PubMed 20684594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 35 4.96 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308033 1 5.82
CHEMBL1215647 1 5.67
CHEMBL1097450 1 5.65
CHEMBL1097451 1 5.65
CHEMBL299112 1 5.52
CHEMBL1215646 1 5.48
CHEMBL1215644 1 5.47
CHEMBL1215645 1 5.34
CHEMBL1215576 1 5.13
CHEMBL507014 1 5.00
CHEMBL363325 1 4.92
CHEMBL1215713 1 4.69
CHEMBL113641 1 4.55
CHEMBL1215715 1 4.49
CHEMBL486633 1 4.34
CHEMBL1215714 1 4.30
CHEMBL1215574 1 4.30
CHEMBL1215575 1 4.28
CHEMBL1215507 1 4.28
CHEMBL1215577 1 4.26
CHEMBL1215506 1 -
CHEMBL1215437 1 -
CHEMBL574360 1 -
CHEMBL459673 1 -
CHEMBL507873 1 -
CHEMBL456685 1 -
CHEMBL1215438 1 -
CHEMBL459640 1 -
CHEMBL500868 1 -
CHEMBL1215508 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308033 EC50 = 1500.0 nM 5.82
CHEMBL1215647 EC50 = 2150.0 nM 5.67
CHEMBL1097450 EC50 = 2230.0 nM 5.65
CHEMBL1097451 EC50 = 2260.0 nM 5.65
CHEMBL299112 EC50 = 3000.0 nM 5.52
CHEMBL1215646 EC50 = 3310.0 nM 5.48
CHEMBL1215644 EC50 = 3350.0 nM 5.47
CHEMBL1215645 EC50 = 4600.0 nM 5.34
CHEMBL1215576 EC50 = 7400.0 nM 5.13
CHEMBL507014 EC50 = 10000.0 nM 5.00
CHEMBL363325 EC50 = 12000.0 nM 4.92
CHEMBL1215713 EC50 = 20500.0 nM 4.69
CHEMBL113641 EC50 = 28300.0 nM 4.55
CHEMBL1215715 EC50 = 32200.0 nM 4.49
CHEMBL486633 EC50 = 46000.0 nM 4.34
CHEMBL1215714 EC50 = 49700.0 nM 4.30
CHEMBL1215574 EC50 = 50000.0 nM 4.30
CHEMBL1215575 EC50 = 52600.0 nM 4.28
CHEMBL1215507 EC50 = 53000.0 nM 4.28
CHEMBL1215577 EC50 = 55400.0 nM 4.26
CHEMBL1215509 EC50 > 100000.0 nM -
CHEMBL336467 FUROXAN EC50 > 100000.0 nM -
CHEMBL1212966 EC50 > 100000.0 nM -
CHEMBL320995 EC50 > 100000.0 nM -
CHEMBL500095 EC50 > 100000.0 nM -
CHEMBL1215508 EC50 > 100000.0 nM -
CHEMBL500868 EC50 > 100000.0 nM -
CHEMBL459640 EC50 > 100000.0 nM -
CHEMBL1215438 EC50 > 100000.0 nM -
CHEMBL456685 EC50 > 100000.0 nM -
CHEMBL507873 EC50 > 100000.0 nM -
CHEMBL459673 EC50 > 100000.0 nM -
CHEMBL574360 EC50 > 100000.0 nM -
CHEMBL1215437 EC50 > 100000.0 nM -
CHEMBL1215506 EC50 > 100000.0 nM -