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Assay Detail

CHEMBL3404716

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

Binding
Displacement of [125I]IL-8 from human recombinant CXCR2 receptor expressed in HEK293 cells by scintillation counting analysis
30
Total Activities
30
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

Discovery and evaluation of a novel monocyclic series of CXCR2 antagonists.
Austin RP, Bennion C, Bonnert RV, Cheema L, Cook AR, Cox RJ, Ebden MR, Gaw A, Grime K, Meghani P, Nicholls D, Phillips C, Smith N, Steele J, Stonehouse JP.
Bioorg Med Chem Lett (2015) 25 : 1616 -1620
PubMed 25708618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.43 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446458 1 9.00
CHEMBL3403851 1 8.60
CHEMBL397237 1 8.40
CHEMBL3403854 1 8.40
CHEMBL3403850 1 8.40
CHEMBL3403855 1 8.30
CHEMBL3403848 1 8.30
CHEMBL3403849 1 8.10
CHEMBL3403852 1 8.10
CHEMBL3403853 1 8.10
CHEMBL3403840 1 8.00
CHEMBL3403835 1 7.90
CHEMBL3403847 1 7.90
CHEMBL3403843 1 7.60
CHEMBL3403846 1 7.50
CHEMBL3403842 1 7.50
CHEMBL3403834 1 7.50
CHEMBL3403839 1 7.30
CHEMBL3403845 1 7.20
CHEMBL3403841 1 7.10
CHEMBL3403830 1 7.10
CHEMBL3403838 1 6.80
CHEMBL3403836 1 6.80
CHEMBL3403833 1 6.40
CHEMBL3403828 1 6.40
CHEMBL3403837 1 6.20
CHEMBL3403829 1 6.10
CHEMBL3403832 1 5.50
CHEMBL3403831 1 5.10
CHEMBL3403844 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446458 IC50 = 1.0 nM 9.00
CHEMBL3403851 IC50 = 2.512 nM 8.60
CHEMBL397237 IC50 = 3.981 nM 8.40
CHEMBL3403854 IC50 = 3.981 nM 8.40
CHEMBL3403850 IC50 = 3.981 nM 8.40
CHEMBL3403855 IC50 = 5.012 nM 8.30
CHEMBL3403848 IC50 = 5.012 nM 8.30
CHEMBL3403849 IC50 = 7.943 nM 8.10
CHEMBL3403852 IC50 = 7.943 nM 8.10
CHEMBL3403853 IC50 = 7.943 nM 8.10
CHEMBL3403840 IC50 = 10.0 nM 8.00
CHEMBL3403835 IC50 = 12.59 nM 7.90
CHEMBL3403847 IC50 = 12.59 nM 7.90
CHEMBL3403843 IC50 = 25.12 nM 7.60
CHEMBL3403846 IC50 = 31.62 nM 7.50
CHEMBL3403842 IC50 = 31.62 nM 7.50
CHEMBL3403834 IC50 = 31.62 nM 7.50
CHEMBL3403839 IC50 = 50.12 nM 7.30
CHEMBL3403845 IC50 = 63.1 nM 7.20
CHEMBL3403841 IC50 = 79.43 nM 7.10
CHEMBL3403830 IC50 = 79.43 nM 7.10
CHEMBL3403838 IC50 = 158.49 nM 6.80
CHEMBL3403836 IC50 = 158.49 nM 6.80
CHEMBL3403833 IC50 = 398.11 nM 6.40
CHEMBL3403828 IC50 = 398.11 nM 6.40
CHEMBL3403837 IC50 = 630.96 nM 6.20
CHEMBL3403829 IC50 = 794.33 nM 6.10
CHEMBL3403832 IC50 = 3162.28 nM 5.50
CHEMBL3403831 IC50 = 7943.28 nM 5.10
CHEMBL3403844 IC50 > 10000.0 nM -