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Assay Detail

CHEMBL947075

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

Assay Information

Assay Type Functional
Organism Macaca fascicularis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 3 (CHEMBL1075262)
Type SINGLE PROTEIN
Organism Macaca fascicularis

Publication

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.
Santella JB, Gardner DS, Yao W, Shi C, Reddy P, Tebben AJ, DeLucca GV, Wacker DA, Watson PS, Welch PK, Wadman EA, Davies P, Solomon KA, Graden DM, Yeleswaram S, Mandlekar S, Kariv I, Decicco CP, Ko SS, Carter PH, Duncia JV.
Bioorg Med Chem Lett (2008) 18 : 576 -585
PubMed 18096386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.82 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399495 1 9.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399495 IC50 = 0.15 nM 9.82