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Assay Detail

CHEMBL662153

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

Binding
Evaluated using an SPA assay with recombinant human [125I]IL-8 and membranes prepared from Sf9 cells expressing human CXCR2
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Nicotinamide N-oxides as CXCR2 antagonists.
Cutshall NS, Ursino R, Kucera KA, Latham J, Ihle NC.
Bioorg Med Chem Lett (2001) 11 : 1951 -1954
PubMed 11459668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.70 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57680 1 7.50
CHEMBL301424 1 7.05
CHEMBL294095 1 6.89
CHEMBL61835 1 6.89
CHEMBL58619 1 6.55
CHEMBL61655 1 6.40
CHEMBL62108 1 6.34
CHEMBL60066 1 6.00
CHEMBL293139 1 -
CHEMBL59734 1 -
CHEMBL292767 1 -
CHEMBL291368 1 -
CHEMBL60115 1 -
CHEMBL60578 1 -
CHEMBL58561 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57680 IC50 = 32.0 nM 7.50
CHEMBL301424 IC50 = 90.0 nM 7.05
CHEMBL294095 IC50 = 130.0 nM 6.89
CHEMBL61835 IC50 = 130.0 nM 6.89
CHEMBL58619 IC50 = 280.0 nM 6.55
CHEMBL61655 IC50 = 400.0 nM 6.40
CHEMBL62108 IC50 = 460.0 nM 6.34
CHEMBL60066 IC50 = 1000.0 nM 6.00
CHEMBL293139 IC50 > 20000.0 nM -
CHEMBL59734 IC50 > 20000.0 nM -
CHEMBL292767 IC50 > 20000.0 nM -
CHEMBL291368 IC50 > 20000.0 nM -
CHEMBL60115 IC50 > 20000.0 nM -
CHEMBL60578 IC50 > 20000.0 nM -
CHEMBL58561 IC50 > 20000.0 nM -