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Assay Detail

CHEMBL4050620

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

Binding
Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring compound concentration required for reduction of ADR IC50 after 48 hrs by MTT assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
Qiu Q, Shi W, Li Z, Zhang B, Pan M, Cui J, Dai Y, Huang W, Qian H.
J Med Chem (2017) 60 : 2930 -2943
PubMed 28301155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.70 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097071 1 6.92
CHEMBL4099415 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097071 EC50 = 119.6 nM 6.92
CHEMBL4099415 EC50 = 329.0 nM 6.48