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Assay Detail

CHEMBL4048749

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

Binding
Activation of recombinant human ABCG2 ATPase activity expressed in baculovirus infected High five insect cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction-based colorimetric method
35
Total Activities
35
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

New Inhibitors of Breast Cancer Resistance Protein (ABCG2) Containing a 2,4-Disubstituted Pyridopyrimidine Scaffold.
Krapf MK, Gallus J, Vahdati S, Wiese M.
J Med Chem (2018) 61 : 3389 -3408
PubMed 29547272 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 35 7.53 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101737 1 8.70
CHEMBL4073213 1 8.52
CHEMBL4091528 1 8.40
CHEMBL4072298 1 8.40
CHEMBL4094899 1 8.40
CHEMBL4074563 1 8.30
CHEMBL4081623 1 8.10
CHEMBL4064296 1 8.10
CHEMBL1195084 1 7.96
CHEMBL4082782 1 7.96
CHEMBL4099250 1 7.92
CHEMBL4073354 1 7.89
CHEMBL547193 1 7.89
CHEMBL2158558 1 7.85
CHEMBL4075963 1 7.85
CHEMBL4076800 1 7.80
CHEMBL4060914 1 7.80
CHEMBL4077346 1 7.80
CHEMBL4069582 1 7.70
CHEMBL50 QUERCETIN 3.0 1 7.52
CHEMBL4083745 1 7.50
CHEMBL4072305 1 7.33
CHEMBL4063711 1 7.14
CHEMBL1194993 1 7.14
CHEMBL1410991 1 7.14
CHEMBL4094904 1 7.07
CHEMBL4066611 1 6.94
CHEMBL4070627 1 6.85
CHEMBL4075334 1 6.85
CHEMBL4104361 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101737 EC50 = 2.0 nM 8.70
CHEMBL4073213 EC50 = 3.0 nM 8.52
CHEMBL4091528 EC50 = 4.0 nM 8.40
CHEMBL4072298 EC50 = 4.0 nM 8.40
CHEMBL4094899 EC50 = 4.0 nM 8.40
CHEMBL4074563 EC50 = 5.0 nM 8.30
CHEMBL4081623 EC50 = 8.0 nM 8.10
CHEMBL4064296 EC50 = 8.0 nM 8.10
CHEMBL1195084 EC50 = 11.0 nM 7.96
CHEMBL4082782 EC50 = 11.0 nM 7.96
CHEMBL4099250 EC50 = 12.0 nM 7.92
CHEMBL4073354 EC50 = 13.0 nM 7.89
CHEMBL547193 EC50 = 13.0 nM 7.89
CHEMBL2158558 EC50 = 14.0 nM 7.85
CHEMBL4075963 EC50 = 14.0 nM 7.85
CHEMBL4060914 EC50 = 16.0 nM 7.80
CHEMBL4076800 EC50 = 16.0 nM 7.80
CHEMBL4077346 EC50 = 16.0 nM 7.80
CHEMBL4069582 EC50 = 20.0 nM 7.70
CHEMBL50 QUERCETIN EC50 = 30.0 nM 7.52
CHEMBL4083745 EC50 = 32.0 nM 7.50
CHEMBL4072305 EC50 = 47.0 nM 7.33
CHEMBL4063711 EC50 = 72.0 nM 7.14
CHEMBL1194993 EC50 = 72.0 nM 7.14
CHEMBL1410991 EC50 = 72.0 nM 7.14
CHEMBL4094904 EC50 = 85.0 nM 7.07
CHEMBL4066611 EC50 = 116.0 nM 6.94
CHEMBL4070627 EC50 = 141.0 nM 6.85
CHEMBL4075334 EC50 = 140.0 nM 6.85
CHEMBL4104361 EC50 = 145.0 nM 6.84
CHEMBL4069654 EC50 = 210.0 nM 6.68
CHEMBL4094267 EC50 = 1190.0 nM 5.92
CHEMBL4072482 EC50 = 1230.0 nM 5.91
CHEMBL4077318 EC50 = 1440.0 nM 5.84
CHEMBL4088022 EC50 - -