Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4713557

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

Binding
Inhibition of ABCC1 (unknown origin) expressed in human NCI-H69AR cells assessed as reduction in calcein AM efflux preincubated for 30 mins followed by calcein AM addition and measured at 60 secs interval for 1 hr by fluorescence assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H69AR
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site.
Silbermann K,Li J,Namasivayam V,Stefan SM,Wiese M
Eur J Med Chem (2021) 212 : 113045 -113045
PubMed 33454462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.18 5.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 5.53
CHEMBL4744165 1 5.39
CHEMBL4754067 1 5.39
CHEMBL4782268 1 5.04
CHEMBL4799327 1 5.02
CHEMBL4741738 1 4.68
CHEMBL4747679 1 -
CHEMBL4761715 1 -
CHEMBL4783240 1 -
CHEMBL4798521 1 -
CHEMBL4794767 1 -
CHEMBL4750965 1 -
CHEMBL4752426 1 -
CHEMBL4792783 1 -
CHEMBL4800631 1 -
CHEMBL4762956 1 -
CHEMBL4764020 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE IC50 = 2950.0 nM 5.53
CHEMBL4744165 IC50 = 4040.0 nM 5.39
CHEMBL4754067 IC50 = 4080.0 nM 5.39
CHEMBL4782268 IC50 = 9050.0 nM 5.04
CHEMBL4799327 IC50 = 9580.0 nM 5.02
CHEMBL4741738 IC50 = 20700.0 nM 4.68
CHEMBL4747679 IC50 - -
CHEMBL4761715 IC50 - -
CHEMBL4783240 IC50 - -
CHEMBL4798521 IC50 - -
CHEMBL4794767 IC50 - -
CHEMBL4750965 IC50 - -
CHEMBL4752426 IC50 - -
CHEMBL4792783 IC50 - -
CHEMBL4800631 IC50 - -
CHEMBL4762956 IC50 - -
CHEMBL4764020 IC50 - -