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Assay Detail

CHEMBL4037523

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

Binding
Antagonist activity at CXCR2 in C57 mouse whole blood assessed as inhibition of GROalpha-stimulated CD11b upregulation preincubated for 1 hr followed by GROalpha stimulation measured after 10 mins by FITC-staining based FACS analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-X-C chemokine receptor type 2 (CHEMBL4105830)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.
Lu H, Yang T, Xu Z, Lin X, Ding Q, Zhang Y, Cai X, Dong K, Gong S, Zhang W, Patel M, Copley RCB, Xiang J, Guan X, Wren P, Ren F.
J Med Chem (2018) 61 : 2518 -2532
PubMed 29406702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.16 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067429 1 8.23
CHEMBL216981 NAVARIXIN ANHYDROUS 2.0 1 8.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067429 IC50 = 5.9 nM 8.23
CHEMBL216981 NAVARIXIN ANHYDROUS IC50 = 8.1 nM 8.09