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Assay Detail

CHEMBL980949

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Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 4 (CHEMBL2414)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent CCR4 antagonists: synthesis, evaluation, and docking study of 2,4-diaminoquinazolines.
Yokoyama K, Ishikawa N, Igarashi S, Kawano N, Masuda N, Hattori K, Miyazaki T, Ogino S, Orita M, Matsumoto Y, Takeuchi M, Ohta M.
Bioorg Med Chem (2008) 16 : 7968 -7974
PubMed 18694645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.14 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487635 1 7.72
CHEMBL486840 1 7.62
CHEMBL488018 1 7.60
CHEMBL487835 1 7.51
CHEMBL488857 1 7.37
CHEMBL486656 1 7.21
CHEMBL488690 1 7.04
CHEMBL487836 1 7.01
CHEMBL488855 1 6.89
CHEMBL488691 1 6.82
CHEMBL488704 1 6.66
CHEMBL487665 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487635 IC50 = 19.0 nM 7.72
CHEMBL486840 IC50 = 24.0 nM 7.62
CHEMBL488018 IC50 = 25.0 nM 7.60
CHEMBL487835 IC50 = 31.0 nM 7.51
CHEMBL488857 IC50 = 43.0 nM 7.37
CHEMBL486656 IC50 = 61.0 nM 7.21
CHEMBL488690 IC50 = 92.0 nM 7.04
CHEMBL487836 IC50 = 98.0 nM 7.01
CHEMBL488855 IC50 = 130.0 nM 6.89
CHEMBL488691 IC50 = 150.0 nM 6.82
CHEMBL488704 IC50 = 220.0 nM 6.66
CHEMBL487665 IC50 = 550.0 nM 6.26