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Assay Detail

CHEMBL949060

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

Binding
Displacement of [125I]IL8 from human recombinant CXCR2 expressed in HEK293 cells by SPA assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Evaluation of a series of bicyclic CXCR2 antagonists.
Walters I, Austin C, Austin R, Bonnert R, Cage P, Christie M, Ebden M, Gardiner S, Grahames C, Hill S, Hunt F, Jewell R, Lewis S, Martin I, David Nicholls, David Robinson.
Bioorg Med Chem Lett (2008) 18 : 798 -803
PubMed 18240390 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.62 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL403225 1 9.00
CHEMBL256668 1 9.00
CHEMBL446458 1 9.00
CHEMBL272105 1 8.70
CHEMBL271012 1 8.70
CHEMBL429791 1 8.52
CHEMBL397237 1 8.40
CHEMBL272705 1 8.30
CHEMBL429682 1 8.30
CHEMBL402986 1 8.30
CHEMBL271703 1 8.15
CHEMBL257006 1 7.89
CHEMBL271013 1 7.89
CHEMBL232846 1 7.89
CHEMBL403656 1 7.80
CHEMBL233263 1 7.46
CHEMBL403877 1 7.35
CHEMBL402728 1 7.22
CHEMBL390191 1 6.92
CHEMBL403702 1 6.85
CHEMBL257025 1 6.66
CHEMBL257659 1 6.55
CHEMBL404057 1 6.55
CHEMBL257269 1 6.46
CHEMBL270446 1 6.20
CHEMBL258334 1 6.07
CHEMBL257027 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL403225 IC50 = 1.0 nM 9.00
CHEMBL256668 IC50 = 1.0 nM 9.00
CHEMBL446458 IC50 = 1.0 nM 9.00
CHEMBL272105 IC50 = 2.0 nM 8.70
CHEMBL271012 IC50 = 2.0 nM 8.70
CHEMBL429791 IC50 = 3.0 nM 8.52
CHEMBL397237 IC50 = 4.0 nM 8.40
CHEMBL272705 IC50 = 5.0 nM 8.30
CHEMBL429682 IC50 = 5.0 nM 8.30
CHEMBL402986 IC50 = 5.0 nM 8.30
CHEMBL271703 IC50 = 7.0 nM 8.15
CHEMBL257006 IC50 = 13.0 nM 7.89
CHEMBL271013 IC50 = 13.0 nM 7.89
CHEMBL232846 IC50 = 13.0 nM 7.89
CHEMBL403656 IC50 = 16.0 nM 7.80
CHEMBL233263 IC50 = 35.0 nM 7.46
CHEMBL403877 IC50 = 45.0 nM 7.35
CHEMBL402728 IC50 = 60.0 nM 7.22
CHEMBL390191 IC50 = 120.0 nM 6.92
CHEMBL403702 IC50 = 140.0 nM 6.85
CHEMBL257025 IC50 = 220.0 nM 6.66
CHEMBL257659 IC50 = 280.0 nM 6.55
CHEMBL404057 IC50 = 280.0 nM 6.55
CHEMBL257269 IC50 = 350.0 nM 6.46
CHEMBL270446 IC50 = 630.0 nM 6.20
CHEMBL258334 IC50 = 850.0 nM 6.07
CHEMBL257027 IC50 = 2500.0 nM 5.60