General Information of the Protein
Protein ID
PT01013
Protein Name
C-X-C chemokine receptor type 2
Secondarily
Protein Name
CDw128b
GRO/MGSA receptor
High affinity interleukin-8 receptor B
IL-8 receptor type 2
Gene Name
CXCR2
Secondarily
Gene Name
IL8RB
Sequence
MEDFNMESDSFEDFWKGEDLSNYSYSSTLPPFLLDAAPCEPESLEINKYFVVIIYALVFLLSLLGNSLVMLVILYSRVGRSVTDVYLLNLALADLLFALTLPIWAASKVNGWIFGTFLCKVVSLLKEVNFYSGILLLACISVDRYLAIVHATRTLTQKRYLVKFICLSIWGLSLLLALPVLLFRRTVYSSNVSPACYEDMGNNTANWRMLLRILPQSFGFIVPLLIMLFCYGFTLRTLFKAHMGQKHRAMRVIFAVVLIFLLCWLPYNLVLLADTLMRTQVIQETCERRNHIDRALDATEILGILHSCLNPLIYAFIGQKFRHGLLKILAIHGLISKDSLPKDSRPSFVGSSSGHTSTTL
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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 for interleukin-8 which is a powerful neutrophil chemotactic factor (PubMed:1891716). 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). Binds to IL-8 with high affinity. Also binds with high affinity to CXCL3, GRO/MGSA and NAP-2.
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Uniprot ID
Primary ID:
P25025

Secondarily ID:
Q8IUZ1
Q9P2T6
Q9P2T7
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Ensembl ID
ENSG00000180871
HGNC ID
HGNC:6027
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
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 = 2.6 nM
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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 = 3.6 nM
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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 = 3.8 nM
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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 = 3.8 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 = 4.9 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 = 5 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 = 5.3 nM
 Bioactivity Info 
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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 = 5.4 nM
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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 = 6 nM
 Bioactivity Info 
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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 = 6.2 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 = 6.8 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 = 15 nM
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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 = 17 nM
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CP0428126
 Compound Info 
(S)-3-(3,4-dioxo-2-(1-phenylpropylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C22H23N3O4
  1
1
IC50 = 234 nM
 Bioactivity Info 
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CP0462859
 Compound Info 
3-(2-(benzylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C20H19N3O4
  1
1
IC50 = 236 nM
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CP0424768
 Compound Info 
(S)-3-(3,4-dioxo-2-(1-phenylethylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C21H21N3O4
  1
1
IC50 = 244 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
  2
1
IC50 = 1860 nM
 Bioactivity Info 
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2
Ki = 120 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
  2
1
IC50 = 3290 nM
 Bioactivity Info 
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2
Ki = 320 nM
 Bioactivity Info 
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CP0470432
 Compound Info 
3-(2-(2-ethylhydrazinyl)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C15H18N4O4
  1
1
IC50 = 5490 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 = 110 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 = 130 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 = 180 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 = 260 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 = 550 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 = 7200 nM
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Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000194 , RBL-1
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000102 , U-87MG ATCC
 Cell Line Info 
Cell Line ID: CL000043 , U2OS
 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
  5
1 IC50 = 0.049 nM
2 IC50 = 450 nM
3 IC50 = 680 nM
4 Ki = 4 nM
5 Ki = 5 nM
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 IC50 = 0.12 nM
CP0264141
 Compound Info 
(R)-3-(3,4-dioxo-2-(1-(pyridin-2-yl)propylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
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C21H22N4O4
  1
1 IC50 = 3.3 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 = 3.5 nM
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
  2
1 IC50 = 4.9 nM
2 Ki = 9 nM
CP0050910
 Compound Info 
(R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(5-methylisoxazol-3-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)benzamide
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C20H22N4O5
  1
1 IC50 = 6.3 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
  4
1 IC50 = 6.8 nM
2 Ki = 4 nM
3 Ki = 4.4 nM
4 Ki = 4.7 nM
CP0068783
 Compound Info 
1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea
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C13H10BrN3O4
  1
1 IC50 = 22 nM
CP0537175
 Compound Info 
methyl 2-[5-[(4-fluorophenyl)carbamoyl]pyridin-2-yl]sulfanylacetate
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C15H13FN2O3S
  1
1 IC50 = 42 nM
CP0179941
 Compound Info 
1-(4-chloro-2-hydroxy-3-sulfamoylphenyl)-3-(2,3-dichlorophenyl)urea
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C13H10Cl3N3O4S
  1
1 IC50 = 316.23 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 = 0.049 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 = 5 nM
Clinical Information about the Protein
Target 1 ( C-X-C chemokine receptor type 2 (CXCR2) )
Target Type Successful Target
Disease 8 Target-related Diseases  8
1 Fungal infection [ICD-11: 1F29-1F2F]
2 Pain [ICD-11: MG30-MG3Z]
3 Chronic obstructive pulmonary disease [ICD-11: CA22]
4 Pancreatic islet transplantation failure [ICD-11: NE84]
5 Inflammatory bowel disease [ICD-11: DD72]
6 Gout [ICD-11: FA25]
7 Asthma [ICD-11: CA23]
8 Schizophrenia [ICD-11: 6A20]
Approved Drug(s) 2 Approved Drugs  2
1 Clotrimazole
 Drug Info 
Approved
Fungal infection
2 Ibuprofen
 Drug Info 
Approved
Pain
Clinical Trial Drug(s) 5 Clinical Trial Drugs  5
1 GSK1325756
 Drug Info 
Phase 2
Chronic obstructive pulmonary disease
2 Reparixin
 Drug Info 
Phase 3
Pancreatic islet transplantation failure
3 SB-656933
 Drug Info 
Phase 2
Chronic obstructive pulmonary disease
4 SCH-527123
 Drug Info 
Phase 2
Inflammatory bowel disease
5 SB-265610
 Drug Info 
Phase 2
Asthma
Discontinued Drug(s) 2 Discontinued Drugs  2
1 INDOPROFEN
 Drug Info 
Withdrawn from market
Gout
2 SB-332235
 Drug Info 
Discontinued in Phase 1
Chronic obstructive pulmonary disease
Preclinical Drug(s) 1 Preclinical Drug  1
1 PD-157695
 Drug Info 
Preclinical
Schizophrenia