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Assay Detail

CHEMBL980950

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

Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
9
Total Activities
9
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 9 6.72 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL488018 1 7.16
CHEMBL486840 1 6.96
CHEMBL487635 1 6.70
CHEMBL488857 1 6.55
CHEMBL487835 1 6.50
CHEMBL486656 1 6.44
CHEMBL488855 1 -
CHEMBL488691 1 -
CHEMBL487665 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL488018 IC50 = 69.0 nM 7.16
CHEMBL486840 IC50 = 110.0 nM 6.96
CHEMBL487635 IC50 = 200.0 nM 6.70
CHEMBL488857 IC50 = 280.0 nM 6.55
CHEMBL487835 IC50 = 320.0 nM 6.50
CHEMBL486656 IC50 = 360.0 nM 6.44
CHEMBL488855 IC50 - -
CHEMBL488691 IC50 - -
CHEMBL487665 IC50 - -