Target Information
| Target General Information | Top | |||||
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| Target ID |
T25315
(Former ID: TTDC00125)
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| Target Name |
C-X-C chemokine receptor type 3 (CXCR3)
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| Synonyms |
Interferon-inducible protein 10 receptor; IP-10 receptor; GPR9; G protein-coupled receptor 9; Chemokine receptor CXCR3/interferon-inducible protein-10; Chemokine receptor CXCR3; CXCR3/IP-10; CXCR-3; CXC-R3; CKR-L2; CD183 antigen; CD183
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| Gene Name |
CXCR3
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| Target Type |
Preclinical target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Psoriasis [ICD-11: EA90] | |||||
| 2 | Hepatic fibrosis/cirrhosis [ICD-11: DB93] | |||||
| 3 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| 4 | Postoperative inflammation [ICD-11: 1A00-CA43] | |||||
| Function |
Binds to CCL21. Probably promotes cell chemotaxis response. Isoform 1: Receptor for the C-X-C chemokine CXCL9, CXCL10 and CXCL11 and mediates the proliferation, survival and angiogenic activity of human mesangial cells (HMC) through a heterotrimeric G-protein signaling pathway.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MVLEVSDHQVLNDAEVAALLENFSSSYDYGENESDSCCTSPPCPQDFSLNFDRAFLPALY
SLLFLLGLLGNGAVAAVLLSRRTALSSTDTFLLHLAVADTLLVLTLPLWAVDAAVQWVFG SGLCKVAGALFNINFYAGALLLACISFDRYLNIVHATQLYRRGPPARVTLTCLAVWGLCL LFALPDFIFLSAHHDERLNATHCQYNFPQVGRTALRVLQLVAGFLLPLLVMAYCYAHILA VLLVSRGQRRLRAMRLVVVVVVAFALCWTPYHLVVLVDILMDLGALARNCGRESRVDVAK SVTSGLGYMHCCLNPLLYAFVGVKFRERMWMLLLRLGCPNQRGLQRQPSSSRRDSSWSET SEASYSGL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A06414 ; BADD_A08478 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | T487 | Drug Info | Discontinued in Phase 2 | Psoriatic disorder | [2] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | dioscin | Drug Info | Preclinical | Hepatic fibrosis | [3] | |
| 2 | JT07 | Drug Info | Preclinical | Solid tumour/cancer | [4] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Antagonist | [+] 6 Antagonist drugs | + | ||||
| 1 | T487 | Drug Info | [1], [5] | |||
| 2 | dioscin | Drug Info | [6] | |||
| 3 | hypoglaucin A | Drug Info | [6] | |||
| 4 | kallstroemin D | Drug Info | [6] | |||
| 5 | NBI-74330 | Drug Info | [1] | |||
| 6 | Sch-900875 | Drug Info | [7] | |||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | JT07 | Drug Info | [4] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Cytokine-cytokine receptor interaction | |||||
| 2 | Chemokine signaling pathway | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | IL2 Signaling Pathway | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Inflammation mediated by chemokine and cytokine signaling pathway | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | CXCR3-mediated signaling events | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Chemokine receptors bind chemokines | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | GPCRs, Class A Rhodopsin-like | |||||
| 2 | Peptide GPCRs | |||||
| 3 | GPCR ligand binding | |||||
| 4 | GPCR downstream signaling | |||||
| 5 | GPCRs, Other | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
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| REF 1 | Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J Pharmacol Exp Ther. 2005 Jun;313(3):1263-71. | |||||
| REF 2 | Clinical pipeline report, company report or official report of ChemoCentryx. | |||||
| REF 3 | Drugs and Targets in Fibrosis. Front Pharmacol. 2017 Nov 23;8:855. | |||||
| REF 4 | Clinical pipeline report, company report or official report of Jyant Technologies. | |||||
| REF 5 | FANCG is phosphorylated at serines 383 and 387 during mitosis. Mol Cell Biol. 2004 Oct;24(19):8576-85. | |||||
| REF 6 | Discovery of structurally diverse natural product antagonists of chemokine receptor CXCR3. Mol Divers. 2005;9(1-3):123-9. | |||||
| REF 7 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 70). | |||||
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