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Assay Detail

CHEMBL4151595

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Binding
Activation of ATPase activity of ABCG2 (unknown origin) expressed in High Five insect cell membranes by ascorbic acid ammonia molybdate reaction based colorimetry
8
Total Activities
8
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

Publication

2,4,6-Substituted Quinazolines with Extraordinary Inhibitory Potency toward ABCG2.
Krapf MK, Gallus J, Namasivayam V, Wiese M.
J Med Chem (2018) 61 : 7952 -7976
PubMed 30075623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.95 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4163310 1 8.00
CHEMBL4174458 1 7.54
CHEMBL4167604 1 7.32
CHEMBL4171017 1 7.20
CHEMBL4164155 1 6.95
CHEMBL4163784 1 6.49
CHEMBL4174412 1 6.16
CHEMBL4167361 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4163310 EC50 = 10.0 nM 8.00
CHEMBL4174458 EC50 = 29.0 nM 7.54
CHEMBL4167604 EC50 = 48.0 nM 7.32
CHEMBL4171017 EC50 = 63.0 nM 7.20
CHEMBL4164155 EC50 = 112.0 nM 6.95
CHEMBL4163784 EC50 = 326.0 nM 6.49
CHEMBL4174412 EC50 = 690.0 nM 6.16
CHEMBL4167361 EC50 = 1230.0 nM 5.91