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Assay Detail

CHEMBL946416

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

Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type B300-19
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of potent CCR4 antagonists: Synthesis and structure-activity relationship study of 2,4-diaminoquinazolines.
Yokoyama K, Ishikawa N, Igarashi S, Kawano N, Hattori K, Miyazaki T, Ogino S, Matsumoto Y, Takeuchi M, Ohta M.
Bioorg Med Chem (2008) 16 : 7021 -7032
PubMed 18539035 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.38 7.16
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487635 1 7.16
CHEMBL508207 1 7.14
CHEMBL510375 1 6.18
CHEMBL488640 1 6.14
CHEMBL529664 1 5.92
CHEMBL470962 1 5.72
CHEMBL509396 1 -
CHEMBL515355 1 -
CHEMBL459465 1 -
CHEMBL459464 1 -
CHEMBL516936 1 -
CHEMBL459463 1 -
CHEMBL451783 1 -
CHEMBL453594 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487635 IC50 = 70.0 nM 7.16
CHEMBL508207 IC50 = 73.0 nM 7.14
CHEMBL510375 IC50 = 660.0 nM 6.18
CHEMBL488640 IC50 = 730.0 nM 6.14
CHEMBL529664 IC50 = 1200.0 nM 5.92
CHEMBL470962 IC50 = 1900.0 nM 5.72
CHEMBL509396 IC50 - -
CHEMBL515355 Inhibition - % -
CHEMBL459465 IC50 - -
CHEMBL459464 IC50 - -
CHEMBL516936 IC50 - -
CHEMBL459463 IC50 - -
CHEMBL451783 IC50 - -
CHEMBL453594 IC50 - -