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Assay Detail

CHEMBL1020786

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

Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type B300-19
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 4 (CHEMBL5410)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines.
Yokoyama K, Ishikawa N, Igarashi S, Kawano N, Masuda N, Hamaguchi W, Yamasaki S, Koganemaru Y, Hattori K, Miyazaki T, Ogino S, Matsumoto Y, Takeuchi M, Ohta M.
Bioorg Med Chem (2009) 17 : 64 -73
PubMed 19081254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.88 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521737 1 7.72
CHEMBL508207 1 7.41
CHEMBL496356 1 7.24
CHEMBL487635 1 6.89
CHEMBL486840 1 6.89
CHEMBL495736 1 6.85
CHEMBL526474 1 6.64
CHEMBL495737 1 6.41
CHEMBL496152 1 6.38
CHEMBL496151 1 6.37
CHEMBL496791 1 -
CHEMBL522233 1 -
CHEMBL526495 1 -
CHEMBL499852 1 -
CHEMBL495948 1 -
CHEMBL496147 1 -
CHEMBL463522 1 -
CHEMBL463722 1 -
CHEMBL518386 1 -
CHEMBL499592 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521737 IC50 = 19.0 nM 7.72
CHEMBL508207 IC50 = 39.0 nM 7.41
CHEMBL496356 IC50 = 58.0 nM 7.24
CHEMBL487635 IC50 = 130.0 nM 6.89
CHEMBL486840 IC50 = 130.0 nM 6.89
CHEMBL495736 IC50 = 140.0 nM 6.85
CHEMBL526474 IC50 = 230.0 nM 6.64
CHEMBL495737 IC50 = 390.0 nM 6.41
CHEMBL496152 IC50 = 420.0 nM 6.38
CHEMBL496151 IC50 = 430.0 nM 6.37
CHEMBL496791 IC50 - -
CHEMBL522233 IC50 - -
CHEMBL526495 IC50 - -
CHEMBL499852 IC50 - -
CHEMBL495948 IC50 - -
CHEMBL496147 IC50 - -
CHEMBL463522 IC50 - -
CHEMBL463722 IC50 - -
CHEMBL518386 IC50 - -
CHEMBL499592 IC50 - -