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Assay Detail

CHEMBL4015708

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

Binding
Activation of ABCG2 (unknown origin) ATPase activity expressed in baculovirus infected high five cell membranes by ascorbic acid/ammonia molybdate reaction-based colorimetric analysis
27
Total Activities
27
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

4-Anilino-2-pyridylquinazolines and -pyrimidines as Highly Potent and Nontoxic Inhibitors of Breast Cancer Resistance Protein (ABCG2).
Krapf MK, Gallus J, Wiese M.
J Med Chem (2017) 60 : 4474 -4495
PubMed 28471656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 7.11 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081708 1 8.40
CHEMBL4082228 1 8.40
CHEMBL4083491 1 8.15
CHEMBL4075328 1 8.05
CHEMBL4082355 1 8.00
CHEMBL2158558 1 7.82
CHEMBL4059784 1 7.80
CHEMBL4069582 1 7.70
CHEMBL4098723 1 7.68
CHEMBL4083108 1 7.66
CHEMBL4090505 1 7.38
CHEMBL4071162 1 7.30
CHEMBL4097911 1 7.24
CHEMBL1499954 1 7.16
CHEMBL4082677 1 7.10
CHEMBL4077632 1 7.09
CHEMBL4062126 1 7.07
CHEMBL4085567 1 6.88
CHEMBL50 QUERCETIN 3.0 1 6.56
CHEMBL4089579 1 6.46
CHEMBL4071711 1 6.17
CHEMBL4068441 1 5.82
CHEMBL4099533 1 5.81
CHEMBL4088963 1 5.75
CHEMBL4096657 1 5.68
CHEMBL4069428 1 5.61
CHEMBL4060750 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081708 EC50 = 4.0 nM 8.40
CHEMBL4082228 EC50 = 4.0 nM 8.40
CHEMBL4083491 EC50 = 7.0 nM 8.15
CHEMBL4075328 EC50 = 9.0 nM 8.05
CHEMBL4082355 EC50 = 10.0 nM 8.00
CHEMBL2158558 EC50 = 15.0 nM 7.82
CHEMBL4059784 EC50 = 16.0 nM 7.80
CHEMBL4069582 EC50 = 20.0 nM 7.70
CHEMBL4098723 EC50 = 21.0 nM 7.68
CHEMBL4083108 EC50 = 22.0 nM 7.66
CHEMBL4090505 EC50 = 42.0 nM 7.38
CHEMBL4071162 EC50 = 50.0 nM 7.30
CHEMBL4097911 EC50 = 58.0 nM 7.24
CHEMBL1499954 EC50 = 70.0 nM 7.16
CHEMBL4082677 EC50 = 79.0 nM 7.10
CHEMBL4077632 EC50 = 82.0 nM 7.09
CHEMBL4062126 EC50 = 85.0 nM 7.07
CHEMBL4085567 EC50 = 131.0 nM 6.88
CHEMBL50 QUERCETIN EC50 = 278.0 nM 6.56
CHEMBL4089579 EC50 = 350.0 nM 6.46
CHEMBL4071711 EC50 = 676.0 nM 6.17
CHEMBL4068441 EC50 = 1530.0 nM 5.82
CHEMBL4099533 EC50 = 1540.0 nM 5.81
CHEMBL4088963 EC50 = 1800.0 nM 5.75
CHEMBL4096657 EC50 = 2080.0 nM 5.68
CHEMBL4069428 EC50 = 2460.0 nM 5.61
CHEMBL4060750 EC50 - -