General Information of the Protein
Protein ID
PT01304
Protein Name
C-X-C chemokine receptor type 1
Secondarily
Protein Name
CDw128a
High affinity interleukin-8 receptor A
IL-8 receptor type 1
Gene Name
CXCR1
Secondarily
Gene Name
CMKAR1
IL8RA
Sequence
MSNITDPQMWDFDDLNFTGMPPADEDYSPCMLETETLNKYVVIIAYALVFLLSLLGNSLVMLVILYSRVGRSVTDVYLLNLALADLLFALTLPIWAASKVNGWIFGTFLCKVVSLLKEVNFYSGILLLACISVDRYLAIVHATRTLTQKRHLVKFVCLGCWGLSMNLSLPFFLFRQAYHPNNSSPVCYEVLGNDTAKWRMVLRILPHTFGFIVPLFVMLFCYGFTLRTLFKAHMGQKHRAMRVIFAVVLIFLLCWLPYNLVLLADTLMRTQVIQESCERRNNIGRALDATEILGFLHSCLNPIIYAFIGQNFRHGFLKILAMHGLVSKEFLARHRVTSYTSSSVNVSSNL
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Chemokine receptor
>
CXC chemokine receptor
Function
Receptor to interleukin-8, which is a powerful neutrophils chemotactic factor (PubMed:1840701). Binding of IL-8 to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system (PubMed:8662698).
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Uniprot ID
Primary ID:
P25024

Secondarily ID:
B2R6Q3
Q2YEF8
Q2YEG4
Q2YEG5
Q2YEG7
Q2YEG8
Q53R18
Q6IN95
Q8N6T6
Q9P2T8
Q9P2T9
Q9P2U0
Q9P2U1
Q9P2U2
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Ensembl ID
ENSG00000163464
HGNC ID
HGNC:6026
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0428127
 Compound Info 
(R)-3-(2-(2,2-dimethyl-1-(5-methylfuran-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C23H27N3O5
  1
1
IC50 = 11 nM
 Bioactivity Info 
   TI
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CP0462861
 Compound Info 
(R)-3-(2-(1-(furan-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C20H21N3O5
  1
1
IC50 = 26 nM
 Bioactivity Info 
   TI
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CP0378812
 Compound Info 
(R)-2-hydroxy-N,N-dimethyl-3-(2-(2-methyl-1-(5-methylfuran-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)benzamide
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C22H25N3O5
  1
1
IC50 = 34 nM
 Bioactivity Info 
   TI
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CP0052095
 Compound Info 
(R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(5-methylfuran-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)benzamide
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C21H23N3O5
  1
1
IC50 = 36 nM
 Bioactivity Info 
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CP0424793
 Compound Info 
(R)-3-(2-(cyclopropyl(5-methylfuran-2-yl)methylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C22H23N3O5
  1
1
IC50 = 55 nM
 Bioactivity Info 
   TI
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CP0147292
 Compound Info 
(R)-3-(3,4-dioxo-2-(1-(thiophen-2-yl)propylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C20H21N3O4S
  1
1
IC50 = 81 nM
 Bioactivity Info 
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CP0442634
 Compound Info 
(R)-3-(2-(1-(benzo[d][1,3]dioxol-5-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C23H23N3O6
  1
1
IC50 = 145 nM
 Bioactivity Info 
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CP0082030
 Compound Info 
(R)-3-(2-(1-(3-fluorophenyl)propylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C22H22FN3O4
  1
1
IC50 = 197 nM
 Bioactivity Info 
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CP0500390
 Compound Info 
(R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(5-methylthiophen-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)benzamide
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C21H23N3O4S
  1
1
IC50 = 235 nM
 Bioactivity Info 
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CP0035725
 Compound Info 
(R)-3-(3,4-dioxo-2-(1-phenylpropylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C22H23N3O4
  1
1
IC50 = 254 nM
 Bioactivity Info 
   TI
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CP0462860
 Compound Info 
(R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(5-methylfuran-2-yl)ethylamino)-3,4-dioxocyclobut-1-enylamino)benzamide
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C20H21N3O5
  1
1
IC50 = 775 nM
 Bioactivity Info 
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CP0554313
 Compound Info 
3-(3,4-dioxo-2-(pentan-3-ylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C18H23N3O4
  1
1
IC50 = 910 nM
 Bioactivity Info 
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CP0871005
 Compound Info 
(R)-3-(3,4-dioxo-2-(1-phenylethylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C21H21N3O4
  1
1
IC50 = 3058 nM
 Bioactivity Info 
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CP0492268
 Compound Info 
3-(2-(2-ethyl-2-phenylhydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C21H22N4O4
  1
1
Ki = 4100 nM
 Bioactivity Info 
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CP0374039
 Compound Info 
3-(2-(2-ethyl-2-(pyridin-2-yl)hydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C20H21N5O4
  1
1
Ki = 5200 nM
 Bioactivity Info 
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CP0501544
 Compound Info 
3-(2-(2-ethyl-2-(4-methoxyphenyl)hydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C22H24N4O5
  1
1
Ki = 6500 nM
 Bioactivity Info 
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CP0096177
 Compound Info 
3-(2-(2,2-diethylhydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C17H22N4O4
  1
1
Ki = 9700 nM
 Bioactivity Info 
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CP0384488
 Compound Info 
3-(2-(2-ethyl-2-(4-fluorobenzyl)hydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C22H23FN4O4
  1
1
Ki > 12000 nM
 Bioactivity Info 
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CP0459197
 Compound Info 
3-(2-(2-ethyl-2-(4-fluorobenzoyl)hydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C22H21FN4O5
  1
1
Ki > 12000 nM
 Bioactivity Info 
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CP0470434
 Compound Info 
3-(2-(2-acetyl-2-ethylhydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C17H20N4O5
  1
1
Ki > 12000 nM
 Bioactivity Info 
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CP0501543
 Compound Info 
3-(2-(2-ethyl-2-(4-fluorophenyl)hydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C21H21FN4O4
  1
1
Ki > 12000 nM
 Bioactivity Info 
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Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000194 , RBL-1
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0052095
 Compound Info 
(R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(5-methylfuran-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)benzamide
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C21H23N3O5
  2
1 IC50 = 3.9 nM
2 Ki = 20 nM
CP0035725
 Compound Info 
(R)-3-(3,4-dioxo-2-(1-phenylpropylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C22H23N3O4
  2
1 IC50 = 6.8 nM
2 Ki = 40 nM
CP0554313
 Compound Info 
3-(3,4-dioxo-2-(pentan-3-ylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C18H23N3O4
  1
1 IC50 = 15 nM
CP0155901
 Compound Info 
(R)-3-(2-(1-(4-bromofuran-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C20H20BrN3O5
  1
1 IC50 = 55 nM
CP0462861
 Compound Info 
(R)-3-(2-(1-(furan-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C20H21N3O5
  1
1 Kd = 3.9 nM
CP0147292
 Compound Info 
(R)-3-(3,4-dioxo-2-(1-(thiophen-2-yl)propylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C20H21N3O4S
  1
1 Ki = 210 nM
Clinical Information about the Protein
Target 1 ( C-X-C chemokine receptor type 1 (CXCR1) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Pain [ICD-11: MG30-MG3Z]
2 Pancreatic islet transplantation failure [ICD-11: NE84]
3 Inflammatory bowel disease [ICD-11: DD72]
4 Gout [ICD-11: FA25]
Approved Drug(s) 1 Approved Drug  1
1 Ibuprofen
 Drug Info 
Approved
Pain
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Reparixin
 Drug Info 
Phase 3
Pancreatic islet transplantation failure
2 SCH-527123
 Drug Info 
Phase 2
Inflammatory bowel disease
Discontinued Drug(s) 1 Discontinued Drug  1
1 INDOPROFEN
 Drug Info 
Withdrawn from market
Gout