Assay Detail

CHEMBL912819

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Functional

Inhibition of CXCL8-induced human neutrophil chemotaxis

ChEMBL ↗

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Target

Interleukin-8 receptors, CXCR1/CXCR2 (CHEMBL2096909) ↗

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Interleukin-8 receptors, CXCR1/CXCR2 (CHEMBL2096909) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Interleukin-8 receptors, CXCR1/CXCR2

CHEMBL2096909

Anchored from Assay target.

Protein identity Interleukin-8 receptors, CXCR1/CXCR2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.

Dwyer MP, Yu Y, Chao J, Aki C, Chao J, Biju P, Girijavallabhan V, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, Rokosz LL, Kaiser B, Li G, Wang W, Stauffer T, Ozgur L, Baldwin J, Taveras AG.
J Med Chem (2006) 49 : 7603 -7606
PubMed 17181143 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	6.93	7.80

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL216981	NAVARIXIN ANHYDROUS	2.0	1	7.80
CHEMBL216602	—	—	1	6.60
CHEMBL254370	—	—	1	6.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL216981	NAVARIXIN ANHYDROUS	IC50	=	16.0	nM	7.80
CHEMBL216602	—	IC50	=	251.0	nM	6.60
CHEMBL254370	—	IC50	=	398.0	nM	6.40