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Assay Detail

CHEMBL3390819

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

Binding
Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H69
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators.
Krauze A, Grinberga S, Krasnova L, Adlere I, Sokolova E, Domracheva I, Shestakova I, Andzans Z, Duburs G.
Bioorg Med Chem (2014) 22 : 5860 -5870
PubMed 25311564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 5.08 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342124 1 5.96
CHEMBL3342123 1 5.41
CHEMBL3342117 1 5.28
CHEMBL3342116 1 5.28
CHEMBL3344541 1 5.18
CHEMBL3342125 1 5.16
CHEMBL1506885 1 5.01
CHEMBL3344543 1 4.92
CHEMBL15177 MK-571 1 4.91
CHEMBL3342118 1 4.91
CHEMBL6966 VERAPAMIL 4.0 1 4.56
CHEMBL3342110 1 4.38
CHEMBL3344542 1 -
CHEMBL3342111 1 -
CHEMBL3342112 1 -
CHEMBL3342113 1 -
CHEMBL3342115 1 -
CHEMBL3342119 1 -
CHEMBL3342120 1 -
CHEMBL3342121 1 -
CHEMBL3342122 1 -
CHEMBL3342135 1 -
CHEMBL3342126 1 -
CHEMBL3342127 1 -
CHEMBL3342128 1 -
CHEMBL3342129 1 -
CHEMBL3342134 1 -
CHEMBL3342133 1 -
CHEMBL3342131 1 -
CHEMBL3342130 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342124 EC50 = 1100.0 nM 5.96
CHEMBL3342123 EC50 = 3900.0 nM 5.41
CHEMBL3342117 EC50 = 5200.0 nM 5.28
CHEMBL3342116 EC50 = 5200.0 nM 5.28
CHEMBL3344541 EC50 = 6600.0 nM 5.18
CHEMBL3342125 EC50 = 7000.0 nM 5.16
CHEMBL1506885 EC50 = 9800.0 nM 5.01
CHEMBL3344543 EC50 = 11900.0 nM 4.92
CHEMBL15177 MK-571 EC50 = 12400.0 nM 4.91
CHEMBL3342118 EC50 = 12400.0 nM 4.91
CHEMBL6966 VERAPAMIL EC50 = 27800.0 nM 4.56
CHEMBL3342110 EC50 = 41400.0 nM 4.38
CHEMBL3344542 EC50 - -
CHEMBL3342111 EC50 - -
CHEMBL3342112 EC50 - -
CHEMBL3342113 EC50 - -
CHEMBL3342115 EC50 - -
CHEMBL3342119 EC50 - -
CHEMBL3342120 EC50 - -
CHEMBL3342121 EC50 - -
CHEMBL3342122 EC50 - -
CHEMBL3342135 EC50 - -
CHEMBL3342126 EC50 - -
CHEMBL3342127 EC50 - -
CHEMBL3342128 EC50 - -
CHEMBL3342129 EC50 - -
CHEMBL3342134 EC50 - -
CHEMBL3342133 EC50 - -
CHEMBL3342131 EC50 - -
CHEMBL3342130 EC50 - -