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Assay Detail

CHEMBL5366003

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

Functional
Inhibition of CXCR2 (unknown origin) expressed in HEK293 coexpressing snap-CXCR2-LGBit and beta-arrestin2-SMBit using furimazine as substrate preincubated for 1 hr followed by substrate addition and measured after 5 mins by bioluminescence based NanoBiT assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-X-C chemokine receptor type 2 (CHEMBL2434)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2.
Casella BM, Farmer JP, Nesheva DN, Williams HEL, Charlton SJ, Holliday ND, Laughton CA, Mistry SN.
J Med Chem (2023) 66 : 12911 -12930
PubMed 37523859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.33 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216981 NAVARIXIN ANHYDROUS 2.0 1 8.54
CHEMBL5421394 1 7.93
CHEMBL5404638 1 7.54
CHEMBL5423846 1 6.67
CHEMBL5398802 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216981 NAVARIXIN ANHYDROUS IC50 = 2.884 nM 8.54
CHEMBL5421394 IC50 = 11.75 nM 7.93
CHEMBL5404638 IC50 = 28.84 nM 7.54
CHEMBL5423846 IC50 = 213.8 nM 6.67
CHEMBL5398802 IC50 = 1122.02 nM 5.95