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Assay Detail

CHEMBL890042

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

Binding
Displacement of [125I]MDC from human CCR4 expressed 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

Core exploration in optimization of chemokine receptor CCR4 antagonists.
Purandare AV, Wan H, Somerville JE, Burke C, Vaccaro W, Yang X, McIntyre KW, Poss MA.
Bioorg Med Chem Lett (2007) 17 : 679 -682
PubMed 17098428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.28 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL233046 1 7.70
CHEMBL372399 1 7.30
CHEMBL394859 1 7.10
CHEMBL397028 1 6.85
CHEMBL233047 1 6.55
CHEMBL396787 1 6.55
CHEMBL233045 1 6.30
CHEMBL232839 1 6.09
CHEMBL232840 1 6.08
CHEMBL396786 1 5.96
CHEMBL232841 1 5.72
CHEMBL232639 1 5.68
CHEMBL232641 1 5.58
CHEMBL233261 1 5.44
CHEMBL232640 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL233046 IC50 = 20.0 nM 7.70
CHEMBL372399 IC50 = 50.0 nM 7.30
CHEMBL394859 IC50 = 80.0 nM 7.10
CHEMBL397028 IC50 = 140.0 nM 6.85
CHEMBL233047 IC50 = 280.0 nM 6.55
CHEMBL396787 IC50 = 280.0 nM 6.55
CHEMBL233045 IC50 = 500.0 nM 6.30
CHEMBL232839 IC50 = 820.0 nM 6.09
CHEMBL232840 IC50 = 830.0 nM 6.08
CHEMBL396786 IC50 = 1100.0 nM 5.96
CHEMBL232841 IC50 = 1910.0 nM 5.72
CHEMBL232639 IC50 = 2100.0 nM 5.68
CHEMBL232641 IC50 = 2600.0 nM 5.58
CHEMBL233261 IC50 = 3600.0 nM 5.44
CHEMBL232640 IC50 = 4900.0 nM 5.31