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Assay Detail

CHEMBL833397

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Functional
Inhibition of CXCL8-induced chemotaxis in human polymorphonuclear cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Interleukin-8 receptors, CXCR1/CXCR2 (CHEMBL2096909)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
Allegretti M, Bertini R, Cesta MC, Bizzarri C, Di Bitondo R, Di Cioccio V, Galliera E, Berdini V, Topai A, Zampella G, Russo V, Di Bello N, Nano G, Nicolini L, Locati M, Fantucci P, Florio S, Colotta F.
J Med Chem (2005) 48 : 4312 -4331
PubMed 15974585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.55 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190899 1 8.74
CHEMBL191413 REPARIXIN 3.0 1 8.28
CHEMBL372052 R-KETOPROFEN 1 7.47
CHEMBL75435 DEXKETOPROFEN 4.0 1 7.30
CHEMBL192943 1 7.10
CHEMBL175 DEXIBUPROFEN 4.0 1 7.00
CHEMBL427526 (R)-IBUPROPHEN 1.0 1 6.96
CHEMBL365276 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190899 IC50 = 1.8 nM 8.74
CHEMBL191413 REPARIXIN IC50 = 5.3 nM 8.28
CHEMBL372052 R-KETOPROFEN IC50 = 34.0 nM 7.47
CHEMBL75435 DEXKETOPROFEN IC50 = 50.0 nM 7.30
CHEMBL192943 IC50 = 80.0 nM 7.10
CHEMBL175 DEXIBUPROFEN IC50 = 100.0 nM 7.00
CHEMBL427526 (R)-IBUPROPHEN IC50 = 110.0 nM 6.96
CHEMBL365276 IC50 - nM -