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Assay Detail

CHEMBL863428

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

Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Optimization of CCR4 antagonists: side-chain exploration.
Purandare AV, Wan H, Gao A, Somerville J, Burke C, Vaccaro W, Yang X, McIntyre KW, Poss MA.
Bioorg Med Chem Lett (2006) 16 : 204 -207
PubMed 16236499 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.31 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372399 1 7.30
CHEMBL200465 1 7.22
CHEMBL370861 1 6.52
CHEMBL199733 1 6.16
CHEMBL199913 1 6.10
CHEMBL202085 1 6.00
CHEMBL382826 1 5.92
CHEMBL200966 1 5.25
CHEMBL197654 1 -
CHEMBL200400 1 -
CHEMBL199466 1 -
CHEMBL199374 1 -
CHEMBL199780 1 -
CHEMBL199818 1 -
CHEMBL198077 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372399 IC50 = 50.0 nM 7.30
CHEMBL200465 IC50 = 60.0 nM 7.22
CHEMBL370861 IC50 = 300.0 nM 6.52
CHEMBL199733 IC50 = 700.0 nM 6.16
CHEMBL199913 IC50 = 800.0 nM 6.10
CHEMBL202085 IC50 = 1000.0 nM 6.00
CHEMBL382826 IC50 = 1200.0 nM 5.92
CHEMBL200966 IC50 = 5600.0 nM 5.25
CHEMBL197654 IC50 > 10000.0 nM -
CHEMBL200400 IC50 > 10000.0 nM -
CHEMBL199466 IC50 > 10000.0 nM -
CHEMBL199374 IC50 > 10000.0 nM -
CHEMBL199780 IC50 > 10000.0 nM -
CHEMBL199818 IC50 > 10000.0 nM -
CHEMBL198077 IC50 > 10000.0 nM -