General Information of the Protein
Protein ID
PT04582
Protein Name
CX3C chemokine receptor 1
Secondarily
Protein Name
Beta chemokine receptor-like 1
Fractalkine receptor
G-protein coupled receptor 13
V28
Gene Name
CX3CR1
Secondarily
Gene Name
CMKBRL1
GPR13
Sequence
MDQFPESVTENFEYDDLAEACYIGDIVVFGTVFLSIFYSVIFAIGLVGNLLVVFALTNSKKPKSVTDIYLLNLALSDLLFVATLPFWTHYLINEKGLHNAMCKFTTAFFFIGFFGSIFFITVISIDRYLAIVLAANSMNNRTVQHGVTISLGVWAAAILVAAPQFMFTKQKENECLGDYPEVLQEIWPVLRNVETNFLGFLLPLLIMSYCYFRIIQTLFSCKNHKKAKAIKLILLVVIVFFLFWTPYNVMIFLETLKLYDFFPSCDMRKDLRLALSVTETVAFSHCCLNPLIYAFAGEKFRRYLYHLYGKCLAVLCGRSVHVDFSSSESQRSRHGSVLSSNFTYHTSDGDALLLL
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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
>
CX3C chemokine receptor
Function
Receptor for the C-X3-C chemokine fractalkine (CX3CL1) present on many early leukocyte cells; CX3CR1-CX3CL1 signaling exerts distinct functions in different tissue compartments, such as immune response, inflammation, cell adhesion and chemotaxis (PubMed:9390561, PubMed:9782118, PubMed:12055230, PubMed:23125415). CX3CR1-CX3CL1 signaling mediates cell migratory functions (By similarity). Responsible for the recruitment of natural killer (NK) cells to inflamed tissues (By similarity). Acts as a regulator of inflammation process leading to atherogenesis by mediating macrophage and monocyte recruitment to inflamed atherosclerotic plaques, promoting cell survival (By similarity). Involved in airway inflammation by promoting interleukin 2-producing T helper (Th2) cell survival in inflamed lung (By similarity). Involved in the migration of circulating monocytes to non-inflamed tissues, where they differentiate into macrophages and dendritic cells (By similarity). Acts as a negative regulator of angiogenesis, probably by promoting macrophage chemotaxis (PubMed:14581400, PubMed:18971423). Plays a key role in brain microglia by regulating inflammatory response in the central nervous system (CNS) and regulating synapse maturation (By similarity). Required to restrain the microglial inflammatory response in the CNS and the resulting parenchymal damage in response to pathological stimuli (By similarity). Involved in brain development by participating in synaptic pruning, a natural process during which brain microglia eliminates extra synapses during postnatal development (By similarity). Synaptic pruning by microglia is required to promote the maturation of circuit connectivity during brain development (By similarity). Acts as an important regulator of the gut microbiota by controlling immunity to intestinal bacteria and fungi (By similarity). Expressed in lamina propria dendritic cells in the small intestine, which form transepithelial dendrites capable of taking up bacteria in order to provide defense against pathogenic bacteria (By similarity). Required to initiate innate and adaptive immune responses against dissemination of commensal fungi (mycobiota) component of the gut: expressed in mononuclear phagocytes (MNPs) and acts by promoting induction of antifungal IgG antibodies response to confer protection against disseminated C.albicans or C.auris infection (PubMed:29326275). Also acts as a receptor for C-C motif chemokine CCL26, inducing cell chemotaxis (PubMed:20974991).
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Uniprot ID
Primary ID:
P49238

Secondarily ID:
A0N0N6
B2R5Z4
J3KP17
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Ensembl ID
ENSG00000168329
HGNC ID
HGNC:2558
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0059888
(2R)-2-[[2-amino-5-[(1S)-1-phenylethyl]sulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C19H25N5OS2
 1
1
Ki = 3.9 nM
   TI
   LI
   LO
   TS
CP0382874
(2R)-2-[[2-amino-5-[(2-bromophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C18H22BrN5OS2
 1
1
Ki = 4 nM
   TI
   LI
   LO
   TS
CP0382416
(2R)-2-[[2-amino-5-[(1S)-1-(2-fluorophenyl)ethyl]sulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C19H24FN5OS2
 1
1
Ki = 4.7 nM
   TI
   LI
   LO
   TS
CP0382414
5-[(1S)-1-(4-chloropyridin-2-yl)ethyl]sulfanyl-7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C18H22ClN5O2S2
 1
1
Ki = 5.8 nM
   TI
   LI
   LO
   TS
CP0462410
(2R)-2-[[2-amino-5-[(1S)-1-(4-chloropyridin-2-yl)ethyl]sulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C18H23ClN6OS2
 1
1
Ki = 6.2 nM
   TI
   LI
   LO
   TS
CP0423472
7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-5-[(1S)-1-phenylethyl]sulfanyl-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C19H24N4O2S2
 1
1
Ki = 7.8 nM
   TI
   LI
   LO
   TS
CP0382421
7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-5-[(1R)-1-phenylethyl]sulfanyl-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C19H24N4O2S2
 1
1
Ki = 8 nM
   TI
   LI
   LO
   TS
CP0488530
(2R)-2-[[2-amino-5-[(4-bromo-2-fluorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C18H21BrFN5OS2
 1
1
Ki = 8.1 nM
   TI
   LI
   LO
   TS
CP0382418
methyl (2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentanoate
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C19H23N5O2S2
 1
1
Ki = 8.3 nM
   TI
   LI
   LO
   TS
CP0443172
5-[(2,3-difluorophenyl)methylsulfanyl]-7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C18H20F2N4O2S2
 1
1
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0423471
(2R)-2-[[2-amino-5-[(1S)-1-(2-bromophenyl)ethyl]sulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C19H24BrN5OS2
 1
1
Ki = 13 nM
   TI
   LI
   LO
   TS
CP0462411
3-[(1S)-1-[[7-[[(2R)-1-hydroxypentan-2-yl]amino]-2-oxo-3H-[1,3]thiazolo[4,5-d]pyrimidin-5-yl]sulfanyl]ethyl]benzonitrile
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C19H21N5O2S2
 1
1
Ki = 14 nM
   TI
   LI
   LO
   TS
CP0423462
(2R)-2-[[2-amino-5-(2-phenylethylsulfanyl)-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C19H25N5OS2
 1
1
Ki = 18 nM
   TI
   LI
   LO
   TS
CP0507104
(2R)-2-[[2-amino-5-[(1R)-1-phenylethyl]sulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C19H25N5OS2
 1
1
Ki = 18 nM
   TI
   LI
   LO
   TS
CP0382419
5-[(1S)-1-(4-chloropyridin-3-yl)ethyl]sulfanyl-7-[[(2R)-1-hydroxypentan-2-yl]amino]-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C17H20ClN5O2S2
 1
1
Ki = 21 nM
   TI
   LI
   LO
   TS
CP0382873
(2R)-2-[[2-amino-5-[(2-fluorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C18H22FN5OS2
 1
1
Ki = 23 nM
   TI
   LI
   LO
   TS
CP0382415
(2R)-2-[[2-amino-5-[(1S)-1-(3-methylsulfonylphenyl)ethyl]sulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C20H27N5O3S3
 1
1
Ki = 28 nM
   TI
   LI
   LO
   TS
CP0435855
5-benzylsulfanyl-7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C18H22N4O2S2
 1
1
Ki = 30 nM
   TI
   LI
   LO
   TS
CP0462406
(2R)-2-[[2-amino-5-[(3-bromophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C18H22BrN5OS2
 1
1
Ki = 32 nM
   TI
   LI
   LO
   TS
CP0507102
3-[(1S)-1-[[2-amino-7-[[(2R)-1-hydroxypentan-2-yl]amino]-[1,3]thiazolo[4,5-d]pyrimidin-5-yl]sulfanyl]ethyl]benzonitrile
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C19H22N6OS2
 1
1
Ki = 42 nM
   TI
   LI
   LO
   TS
CP0435531
methyl (2R)-2-[[2-amino-5-[(2-chlorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentanoate
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C19H22ClN5O2S2
 1
1
Ki = 43 nM
   TI
   LI
   LO
   TS
CP0423469
7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-5-phenylmethoxy-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C18H22N4O3S
 1
1
Ki = 44 nM
   TI
   LI
   LO
   TS
CP0423467
(2R)-2-[[2-amino-5-[(4-bromophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C18H22BrN5OS2
 1
1
Ki = 47 nM
   TI
   LI
   LO
   TS
CP0423057
(2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentan-1-ol
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C18H23N5OS2
 1
1
Ki = 48 nM
   TI
   LI
   LO
   TS
CP0449542
(2R)-2-[[2-amino-5-[(2-chlorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C18H22ClN5OS2
 1
1
Ki = 51 nM
   TI
   LI
   LO
   TS
CP0473399
(2R)-2-[[2-amino-5-[(2-methylphenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C19H25N5OS2
 1
1
Ki = 70 nM
   TI
   LI
   LO
   TS
CP0423474
(2R)-2-[[2-amino-5-[(2,3-difluorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C18H21F2N5OS2
 1
1
Ki = 71 nM
   TI
   LI
   LO
   TS
CP0462405
3-[[2-amino-7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-[1,3]thiazolo[4,5-d]pyrimidin-5-yl]sulfanylmethyl]benzonitrile
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C19H22N6OS2
 1
1
Ki = 91 nM
   TI
   LI
   LO
   TS
CP0480139
(3R)-3-[[2-amino-5-[(2-chlorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-5-methylhexan-1-ol
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C19H24ClN5OS2
 1
1
Ki = 91 nM
   TI
   LI
   LO
   TS
CP0462408
(2R)-2-[[2-amino-5-[(2-methoxyphenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C19H25N5O2S2
 1
1
Ki = 99 nM
   TI
   LI
   LO
   TS
CP0455313
(2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]pentan-1-ol
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C17H21N5OS2
 1
1
Ki = 100 nM
   TI
   LI
   LO
   TS
CP0382420
(2R)-2-[[2-amino-5-[(1R)-1-(2-bromophenyl)ethyl]sulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C19H24BrN5OS2
 1
1
Ki = 102 nM
   TI
   LI
   LO
   TS
CP0449546
(2R)-2-[[2-amino-5-(3-phenylpropylsulfanyl)-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
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C20H27N5OS2
 1
1
Ki = 110 nM
   TI
   LI
   LO
   TS
CP0507101
5-benzylsulfonyl-7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C18H22N4O4S2
 1
1
Ki = 110 nM
   TI
   LI
   LO
   TS
CP0382417
2-[[2-amino-7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-[1,3]thiazolo[4,5-d]pyrimidin-5-yl]sulfanylmethyl]benzonitrile
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C19H22N6OS2
 1
1
Ki = 120 nM
   TI
   LI
   LO
   TS
CP0382876
(2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-3,3-dimethylbutan-1-ol
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C18H23N5OS2
 1
1
Ki = 190 nM
   TI
   LI
   LO
   TS
CP0443171
(2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentanamide
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C18H22N6OS2
 1
1
Ki = 220 nM
   TI
   LI
   LO
   TS
CP0454405
(2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-2-phenylethanol
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C20H19N5OS2
 1
1
Ki = 220 nM
   TI
   LI
   LO
   TS
CP0473397
5-benzylsulfinyl-7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C18H22N4O3S2
 1
1
Ki = 280 nM
   TI
   LI
   LO
   TS
CP0435577
(2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentanoic acid
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C18H21N5O2S2
 1
1
Ki = 320 nM
   TI
   LI
   LO
   TS
CP0423464
(2R)-2-[[2-amino-5-(pyridin-2-ylmethylsulfanyl)-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
   Show/Hide
C17H22N6OS2
 1
1
Ki = 360 nM
   TI
   LI
   LO
   TS
CP0465327
5-benzylsulfanyl-7-[[(2R)-1-hydroxybutan-2-yl]amino]-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
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C16H18N4O2S2
 1
1
Ki = 560 nM
   TI
   LI
   LO
   TS
CP0514129
(2S)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentan-1-ol
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C18H23N5OS2
 1
1
Ki = 600 nM
   TI
   LI
   LO
   TS
CP0507103
(2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-3-methylbutan-1-ol
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C17H21N5OS2
 1
1
Ki = 640 nM
   TI
   LI
   LO
   TS
CP0382422
(2R)-2-[[2-amino-5-(pyridin-3-ylmethylsulfanyl)-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
   Show/Hide
C17H22N6OS2
 1
1
Ki = 670 nM
   TI
   LI
   LO
   TS
CP0462822
(R)-2-(2-amino-5-(benzylthio)thiazolo[4,5-d]pyrimidin-7-ylamino)butan-1-ol
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C16H19N5OS2
 1
1
Ki = 770 nM
   TI
   LI
   LO
   TS
CP0423473
(2R)-2-[[2-amino-5-(pyridin-4-ylmethylsulfanyl)-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol
   Show/Hide
C17H22N6OS2
 1
1
Ki = 900 nM
   TI
   LI
   LO
   TS
CP0525678
(2R)-2-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]propan-1-ol
   Show/Hide
C15H17N5OS2
 1
1
Ki = 1100 nM
   TI
   LI
   LO
   TS
CP0435578
(3R)-3-[(2-amino-5-benzylsulfanyl-[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-2,5-dimethylhexan-2-ol
   Show/Hide
C20H27N5OS2
 1
1
Ki = 1200 nM
   TI
   LI
   LO
   TS
CP0462404
4-[[2-amino-7-[[(2R)-1-hydroxy-4-methylpentan-2-yl]amino]-[1,3]thiazolo[4,5-d]pyrimidin-5-yl]sulfanylmethyl]benzonitrile
   Show/Hide
C19H22N6OS2
 1
1
Ki = 1200 nM
   TI
   LI
   LO
   TS
CP0462409
5-benzylsulfanyl-7-[[(2R)-1-hydroxypropan-2-yl]amino]-3H-[1,3]thiazolo[4,5-d]pyrimidin-2-one
   Show/Hide
C15H16N4O2S2
 1
1
Ki = 29000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( C-X3-C chemokine receptor 1 (CX3CR1) )
Target Type Literature-reported Target