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Assay Detail

CHEMBL4713554

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Binding
Inhibition of ABCG2 (unknown origin) expressed in MDCK-II cells assessed as reduction in pheophorbide A efflux measured after 2 hrs by flow cytometry
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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 18 6.51 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4792783 1 7.02
CHEMBL4761715 1 6.88
CHEMBL4747679 1 6.85
CHEMBL4752426 1 6.83
CHEMBL4762956 1 6.77
CHEMBL4069428 1 6.72
CHEMBL4750965 1 6.68
CHEMBL4798521 1 6.65
CHEMBL4797455 1 6.56
CHEMBL4800631 1 6.55
CHEMBL4799327 1 6.53
CHEMBL4741738 1 6.43
CHEMBL4744165 1 6.41
CHEMBL4794767 1 6.36
CHEMBL4783240 1 6.30
CHEMBL4754067 1 6.22
CHEMBL4782268 1 6.12
CHEMBL4764020 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4792783 IC50 = 96.0 nM 7.02
CHEMBL4761715 IC50 = 133.0 nM 6.88
CHEMBL4747679 IC50 = 141.0 nM 6.85
CHEMBL4752426 IC50 = 147.0 nM 6.83
CHEMBL4762956 IC50 = 169.0 nM 6.77
CHEMBL4069428 IC50 = 189.0 nM 6.72
CHEMBL4750965 IC50 = 210.0 nM 6.68
CHEMBL4798521 IC50 = 223.0 nM 6.65
CHEMBL4797455 IC50 = 274.0 nM 6.56
CHEMBL4800631 IC50 = 283.0 nM 6.55
CHEMBL4799327 IC50 = 293.0 nM 6.53
CHEMBL4741738 IC50 = 373.0 nM 6.43
CHEMBL4744165 IC50 = 387.0 nM 6.41
CHEMBL4794767 IC50 = 435.0 nM 6.36
CHEMBL4783240 IC50 = 500.0 nM 6.30
CHEMBL4754067 IC50 = 608.0 nM 6.22
CHEMBL4782268 IC50 = 763.0 nM 6.12
CHEMBL4764020 IC50 = 4410.0 nM 5.36