General Information of the Protein
Protein ID
PT02059
Protein Name
C-X-C chemokine receptor type 4
Secondarily
Protein Name
FB22
Fusin
HM89
LCR1
Leukocyte-derived seven transmembrane domain receptor
Lipopolysaccharide-associated protein 3
NPYRL
Stromal cell-derived factor 1 receptor
Gene Name
CXCR4
Sequence
MEGISIYTSDNYTEEMGSGDYDSMKEPCFREENANFNKIFLPTIYSIIFLTGIVGNGLVILVMGYQKKLRSMTDKYRLHLSVADLLFVITLPFWAVDAVANWYFGNFLCKAVHVIYTVNLYSSVLILAFISLDRYLAIVHATNSQRPRKLLAEKVVYVGVWIPALLLTIPDFIFANVSEADDRYICDRFYPNDLWVVVFQFQHIMVGLILPGIVILSCYCIIISKLSHSKGHQKRKALKTTVILILAFFACWLPYYIGISIDSFILLEIIKQGCEFENTVHKWISITEALAFFHCCLNPILYAFLGAKFKTSAQHALTSVSRGSSLKILSKGKRGGHSSVSTESESSSFHSS
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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 the C-X-C chemokine CXCL12/SDF-1 that transduces a signal by increasing intracellular calcium ion levels and enhancing MAPK1/MAPK3 activation (PubMed:10452968, PubMed:28978524, PubMed:18799424, PubMed:24912431). Involved in the AKT signaling cascade (PubMed:24912431). Plays a role in regulation of cell migration, e.g. during wound healing (PubMed:28978524). Acts as a receptor for extracellular ubiquitin; leading to enhanced intracellular calcium ions and reduced cellular cAMP levels (PubMed:20228059). Binds bacterial lipopolysaccharide (LPS) et mediates LPS-induced inflammatory response, including TNF secretion by monocytes (PubMed:11276205). Involved in hematopoiesis and in cardiac ventricular septum formation. Also plays an essential role in vascularization of the gastrointestinal tract, probably by regulating vascular branching and/or remodeling processes in endothelial cells. Involved in cerebellar development. In the CNS, could mediate hippocampal-neuron survival (By similarity).
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Uniprot ID
Primary ID:
P61073

Secondarily ID:
B2R5N0
O60835
P30991
P56438
Q53S69
Q9BXA0
Q9UKN2
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HGNC ID
HGNC:2561
Subcellular Location
Cell membrane
Cell junction
Early endosome
Late endosome
Lysosome
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: CL000064 , Chem-1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0489179
 Compound Info 
N-(pyridin-2-ylmethyl)-N'-[[(3R)-1,2,3,4-tetrahydroisoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C29H37N5
  1
1
IC50 = 1 nM
 Bioactivity Info 
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CP0406572
 Compound Info 
N'-[[(2S)-4-(4-chlorophenyl)sulfonylpiperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C24H34ClN5O2S
  1
1
IC50 = 2 nM
 Bioactivity Info 
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CP0416320
 Compound Info 
[(3S)-3-[[4-aminobutyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]methyl]piperazin-1-yl]-phenylmethanone
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C25H35N5O
  1
1
IC50 = 2 nM
 Bioactivity Info 
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CP0563754
 Compound Info 
N'-[[(2S)-4-(benzenesulfonyl)piperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C24H35N5O2S
  1
1
IC50 = 2 nM
 Bioactivity Info 
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CP0070322
 Compound Info 
N'-[[(3R)-1,2,3,4-tetrahydroisoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C23H32N4
  2
1
IC50 = 3 nM
 Bioactivity Info 
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2
IC50 = 120 nM
 Bioactivity Info 
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CP0484544
 Compound Info 
4-[[(3R)-1,2,3,4-tetrahydroisoquinolin-3-yl]methyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]butylurea
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C24H33N5O
  1
1
IC50 = 3 nM
 Bioactivity Info 
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CP0471105
 Compound Info 
N-[4-[[(3R)-1,2,3,4-tetrahydroisoquinolin-3-yl]methyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]butyl]acetamide
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C25H34N4O
  1
1
IC50 = 4 nM
 Bioactivity Info 
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CP0141162
 Compound Info 
[(3R)-3-[[4-aminobutyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]methyl]piperazin-1-yl]-phenylmethanone
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C25H35N5O
  1
1
IC50 = 6 nM
 Bioactivity Info 
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CP0445507
 Compound Info 
N-propan-2-yl-N'-[[(3R)-1,2,3,4-tetrahydroisoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C26H38N4
  1
1
IC50 = 7 nM
 Bioactivity Info 
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CP0069850
 Compound Info 
(6,6-dimethyl-5,6-dihydroimidazo[2,1-b][1,3]thiazol-3-yl)methyl N,N'-dicyclohexylimidothiocarbamate
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C21H34N4S2
  1
1
IC50 = 7.4 nM
 Bioactivity Info 
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CP0466954
 Compound Info 
N,N-dimethyl-N'-[[(3R)-1,2,3,4-tetrahydroisoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C25H36N4
  1
1
IC50 = 8 nM
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CP0444193
 Compound Info 
(6,6-dimethyl-5H-imidazo[2,1-b][1,3]thiazol-3-yl)methyl N'-[4-[[[2-[2-[6-[[2-[2-[[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-2-oxoethoxy]acetyl]amino]hexylamino]-2-oxoethoxy]acetyl]amino]methyl]cyclohexyl]-N-cyclohexylcarbamimidothioate
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C56H83N9O9S2
  1
1
IC50 = 17.2 nM
 Bioactivity Info 
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CP0416321
 Compound Info 
benzyl (3S)-3-[[4-aminobutyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]methyl]piperazine-1-carboxylate
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C26H37N5O2
  1
1
IC50 = 18 nM
 Bioactivity Info 
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CP0099464
 Compound Info 
N'-[[(2R)-4-(benzenesulfonyl)piperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C24H35N5O2S
  1
1
IC50 = 23 nM
 Bioactivity Info 
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CP0431549
 Compound Info 
[(3R)-3-[[4-aminobutyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]methyl]piperazin-1-yl]-(furan-2-yl)methanone
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C23H33N5O2
  1
1
IC50 = 35 nM
 Bioactivity Info 
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CP0387864
 Compound Info 
N'-[[(3R)-2-methyl-3,4-dihydro-1H-isoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C24H34N4
  1
1
IC50 = 39 nM
 Bioactivity Info 
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CP0559064
 Compound Info 
N'-[[(2S)-4-(1-benzothiophen-2-ylsulfonyl)piperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C26H35N5O2S2
  1
1
IC50 = 39 nM
 Bioactivity Info 
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CP0444196
 Compound Info 
N'-[[(3R)-2-(pyridin-2-ylmethyl)-3,4-dihydro-1H-isoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C29H37N5
  1
1
IC50 = 56 nM
 Bioactivity Info 
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CP0425036
 Compound Info 
N'-[[(2S)-4-naphthalen-2-ylsulfonylpiperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C28H37N5O2S
  1
1
IC50 = 71 nM
 Bioactivity Info 
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CP0443356
 Compound Info 
N'-[(4-phenylpiperazin-2-yl)methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C24H35N5
  1
1
IC50 = 130 nM
 Bioactivity Info 
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CP0387771
 Compound Info 
N'-[[(3R)-2-propan-2-yl-3,4-dihydro-1H-isoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C26H38N4
  1
1
IC50 = 140 nM
 Bioactivity Info 
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CP0387865
 Compound Info 
1,1-dimethyl-3-[4-[[(3R)-1,2,3,4-tetrahydroisoquinolin-3-yl]methyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]butyl]urea
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C26H37N5O
  1
1
IC50 = 180 nM
 Bioactivity Info 
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CP0125301
 Compound Info 
N'-[[(2S)-4-benzylpiperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C25H37N5
  1
1
IC50 = 190 nM
 Bioactivity Info 
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CP0450351
 Compound Info 
N'-[[(2R)-4-benzylpiperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C25H37N5
  1
1
IC50 = 230 nM
 Bioactivity Info 
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CP0428477
 Compound Info 
N'-[[(2R)-piperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C18H31N5
  1
1
IC50 = 255 nM
 Bioactivity Info 
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CP0524752
 Compound Info 
N'-[[(3R)-2-(pyridin-3-ylmethyl)-3,4-dihydro-1H-isoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C29H37N5
  1
1
IC50 = 350 nM
 Bioactivity Info 
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CP0387863
 Compound Info 
N'-[[(3R)-2-(1,3-oxazol-4-ylmethyl)-3,4-dihydro-1H-isoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C27H35N5O
  1
1
IC50 = 490 nM
 Bioactivity Info 
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CP0392740
 Compound Info 
2-[(3R)-3-[[4-aminobutyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-1-morpholin-4-ylethanone
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C29H41N5O2
  1
1
IC50 = 570 nM
 Bioactivity Info 
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CP0432257
 Compound Info 
N'-[[(3R)-2-(pyridin-4-ylmethyl)-3,4-dihydro-1H-isoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C29H37N5
  1
1
IC50 = 660 nM
 Bioactivity Info 
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CP0528841
 Compound Info 
N'-[[(2S)-piperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C18H31N5
  1
1
IC50 = 1200 nM
 Bioactivity Info 
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CP0511994
 Compound Info 
(6,6-dimethyl-5H-imidazo[2,1-b][1,3]thiazol-3-yl)methyl N'-[4-[[[2-[2-[4-[[2-[2-[[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-2-oxoethoxy]acetyl]amino]butylamino]-2-oxoethoxy]acetyl]amino]methyl]cyclohexyl]carbamimidothioate
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C48H69N9O9S2
  1
1
IC50 = 3600 nM
 Bioactivity Info 
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CP0406573
 Compound Info 
(3S)-3-[[4-aminobutyl-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]amino]methyl]-N-phenylpiperazine-1-carboxamide
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C25H36N6O
  1
1
IC50 = 21000 nM
 Bioactivity Info 
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CP0564856
 Compound Info 
(6,6-dimethyl-5H-imidazo[2,1-b][1,3]thiazol-3-yl)methyl N-cyclohexyl-N'-[4-[[[2-[2-[4-[[2-[2-(methylamino)-2-oxoethoxy]acetyl]amino]butylamino]-2-oxoethoxy]acetyl]amino]methyl]cyclohexyl]carbamimidothioate
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C35H58N8O6S2
  1
1
IC50 = 69000 nM
 Bioactivity Info 
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Cell Line ID: CL000108 , CCRF-CEM
 Cell Line Info 
Cell Line ID: CL000670 , CF2.Th
 Cell Line Info 
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: CL000017 , HeLa
 Cell Line Info 
Cell Line ID: CL000501 , HeLa-MAGI-CCR5
 Cell Line Info 
Cell Line ID: CL000149 , HOS
 Cell Line Info 
Cell Line ID: CL000571 , HPB-ALL
 Cell Line Info 
Cell Line ID: CL000007 , HT-29
 Cell Line Info 
Cell Line ID: CL000001 , Jurkat
 Cell Line Info 
Cell Line ID: CL000116 , MOLT-4
 Cell Line Info 
Cell Line ID: CL000247 , MT-4
 Cell Line Info 
Cell Line ID: CL000651 , Reh
 Cell Line Info 
Cell Line ID: CL000200 , SUP-T1
 Cell Line Info 
Cell Line ID: CL000040 , THP-1
 Cell Line Info 
Cell Line ID: CL000043 , U2OS
 Cell Line Info 
Cell Line ID: CL000570 , U87.CD4.CXCR4
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0248152
 Compound Info 
2-[3-[(2S,5S,8S,14R)-5-[3-(diaminomethylideneamino)propyl]-14-[(4-hydroxyphenyl)methyl]-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propyl]guanidine
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C36H47N11O6
  1
1 IC50 = 4 nM
CP0177564
 Compound Info 
2-[3-[(2R,5S,8S,14R)-5-[3-(diaminomethylideneamino)propyl]-14-[(4-hydroxyphenyl)methyl]-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propyl]guanidine
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C36H47N11O6
  1
1 IC50 = 8 nM
CP0070322
 Compound Info 
N'-[[(3R)-1,2,3,4-tetrahydroisoquinolin-3-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C23H32N4
  3
1 IC50 = 15 nM
2 IC50 = 35 nM
3 IC50 = 112 nM
CP0067401
 Compound Info 
(S)-N-((1H-benzo[d]imidazol-2-yl)methyl)-N-(4-aminobutyl)-5,6,7,8-tetrahydroquinolin-8-amine
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C21H27N5
  1
1 IC50 = 30 nM
CP0733906
 Compound Info 
1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene octahydrochloride
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C28H62Cl8N8
  1
1 IC50 = 30 nM
CP0145769
 Compound Info 
1,1''-{1,4-phenylenebis(methylene)}-bis{1,4,8,11-tetraaza-cyclotetradecane}
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C28H54N8
  1
1 IC50 = 74 nM
CP0125301
 Compound Info 
N'-[[(2S)-4-benzylpiperazin-2-yl]methyl]-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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C25H37N5
  1
1 IC50 = 2920 nM
CP0071651
 Compound Info 
4-[[4-(4-benzyl-1H-pyrazol-5-yl)piperidin-1-yl]methyl]pyridine
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C21H24N4
  1
1 IC50 = 10000 nM
CP0649585
 Compound Info 
1-butyl-3-(2-methylpropyl)-9-(6-phenylhexyl)-1,4,9-triazaspiro-[5.5]undeca-2,5-dione hydrochloride
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C28H46ClN3O2
  1
1 IC50 > 10000 nM
CP0651200
 Compound Info 
9-(1,4-benzodioxane-6-yl)-1-butyl-3-(2-methylpropyl)-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C25H38ClN3O4
  1
1 IC50 > 10000 nM
CP0651215
 Compound Info 
9-benzyl-1-butyl-3-(2-methylpropyl)-1,4,9-triazaspiro[5.5]-undeca-2,5-dione hydrochloride
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C23H36ClN3O2
  1
1 IC50 > 10000 nM
CP0657856
 Compound Info 
(+/-)-1-butyl-3-(cyclohexylmethyl)-9-(4-phenoxybenzyl)-1,4,9-triazaspiro[5.5]undecane-2,5-dione hydrochloride
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C32H44ClN3O3
  1
1 IC50 > 10000 nM
CP0662025
 Compound Info 
(3R)-3-cyclohexylmethyl-9-(6-phenylhexyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C30H48ClN3O2
  1
1 IC50 > 10000 nM
CP0662064
 Compound Info 
9-(1,4-benzodioxane-6-yl)-1-butyl-3-cyclohexyl-1,4,9-triazaspiro-[5.5]undeca-2,5-dione hydrochloride
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C28H42ClN3O4
  1
1 IC50 > 10000 nM
CP0662079
 Compound Info 
(3S)-3-cyclohexylmethyl-9-(6-phenylhexyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C30H48ClN3O2
  1
1 IC50 > 10000 nM
CP0720738
 Compound Info 
(+/-)-1-butyl-3-isobutyl-9-(4-phenoxybenzyl)-1,4,9-triazaspiro[5.5]undecane-2,5-dione hydrochloride
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C29H40ClN3O3
  1
1 IC50 > 10000 nM
CP0837909
 Compound Info 
9-(4-allyloxyphenylmethyl)-1-butyl-3-cyclohexyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C29H44ClN3O3
  1
1 IC50 > 10000 nM
CP0651202
 Compound Info 
1-butyl-3-cyclohexylmethyl-9-(4-methoxyphenylmethyl)-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C27H42ClN3O3
  1
1 IC50 > 30000 nM
CP0699196
 Compound Info 
3-(2-methylpropyl)-9-(4-phenoxyphenylmethyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C28H38ClN3O3
  1
1 IC50 > 30000 nM
Clinical Information about the Protein
Target 1 ( C-X-C chemokine receptor type 4 (CXCR4) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Non-hodgkin lymphoma [ICD-11: 2B33.5]
2 Whim syndrome [ICD-11: 4A00.Y]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
4 Human immunodeficiency virus-1 infection [ICD-11: 1C62]
5 Acute lymphoblastic leukaemia [ICD-11: 2A85]
Approved Drug(s) 1 Approved Drug  1
1 Plerixafor
 Drug Info 
Approved
Non-hodgkin lymphoma
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 AMD-070
 Drug Info 
Phase 3
Whim syndrome
2 MSX-122
 Drug Info 
Phase 1
Solid tumour/cancer
Investigative Drug(s) 2 Investigative Drugs  2
1 GSK-812397
 Drug Info 
Investigative
Human immunodeficiency virus-1 infection
2 TN-14003
 Drug Info 
Investigative
Acute lymphoblastic leukaemia
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06053 C-X-C chemokine receptor type 4 Rattus norvegicus, Rat
 Protein Info