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Assay Detail

CHEMBL945755

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

Functional
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

C-C chemokine receptor type 3 (CHEMBL3473)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists.
Gardner DS, Santella JB, Tebben AJ, Batt DG, Ko SS, Traeger SC, Welch PK, Wadman EA, Davies P, Carter PH, Duncia JV.
Bioorg Med Chem Lett (2008) 18 : 586 -595
PubMed 18160284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 9.63 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363840 1 11.00
CHEMBL254930 1 10.89
CHEMBL399495 1 10.42
CHEMBL253210 1 9.22
CHEMBL437396 1 8.59
CHEMBL254503 1 7.66
CHEMBL254881 1 -
CHEMBL428062 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363840 IC50 = 0.01 nM 11.00
CHEMBL254930 IC50 = 0.013 nM 10.89
CHEMBL399495 IC50 = 0.038 nM 10.42
CHEMBL253210 IC50 = 0.6 nM 9.22
CHEMBL437396 IC50 = 2.6 nM 8.59
CHEMBL254503 IC50 = 22.0 nM 7.66
CHEMBL254881 IC50 = 0.005 nM -
CHEMBL428062 IC50 = 0.004 nM -