Target Information
| Target General Information | Top | |||||
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| Target ID |
T98494
(Former ID: TTDI01803)
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| Target Name |
Galanin receptor (GAL-R)
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| Synonyms |
GALR; GALNR; GAL-R
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| Gene Name |
GALR1; GALR2; GALR3
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Mild neurocognitive disorder [ICD-11: 6D71] | |||||
| Function |
Receptor for the hormone galanin. Receptor for the hormone spexin-1.
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MELAVGNLSEGNASWPEPPAPEPGPLFGIGVENFVTLVVFGLIFALGVLGNSLVITVLAR
SKPGKPRSTTNLFILNLSIADLAYLLFCIPFQATVYALPTWVLGAFICKFIHYFFTVSML VSIFTLAAMSVDRYVAIVHSRRSSSLRVSRNALLGVGCIWALSIAMASPVAYHQGLFHPR ASNQTFCWEQWPDPRHKKAYVVCTFVFGYLLPLLLICFCYAKVLNHLHKKLKNMSKKSEA SKKKTAQTVLVVVVVFGISWLPHHIIHLWAEFGVFPLTPASFLFRITAHCLAYSNSSVNP IIYAFLSENFRKAYKQVFKCHIRKDSHLSDTKESKSRIDTPPSTNCTHV Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | HT-2157 | Drug Info | Phase 1/2 | Cognitive impairment | [2], [3] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Antagonist | [+] 6 Antagonist drugs | + | ||||
| 1 | HT-2157 | Drug Info | [1] | |||
| 2 | 2,3-dihydro-1,4-dithiin-1,1,4,4-tetroxide | Drug Info | [5] | |||
| 3 | dithiipin-1,1,4,4-tetroxide analogue 7 | Drug Info | [5] | |||
| 4 | GalR3ant | Drug Info | [8] | |||
| 5 | Sch 202596 | Drug Info | [9] | |||
| 6 | SNAP 398299 | Drug Info | [1] | |||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | (E)-3-(2,3-dichlorophenylimino)indolin-2-one | Drug Info | [4] | |||
| 2 | (E)-3-(4-chlorophenylimino)indolin-2-one | Drug Info | [4] | |||
| Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
| 1 | CYM2503 | Drug Info | [6] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | galmic | Drug Info | [7] | |||
| 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 | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | Neuroactive ligand-receptor interaction | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Peptide ligand-binding receptors | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | GPCRs, Class A Rhodopsin-like | |||||
| 2 | Peptide GPCRs | |||||
| 3 | GPCR ligand binding | |||||
| 4 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489-94. | |||||
| REF 2 | 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. (Ligand id: 6126). | |||||
| REF 3 | ClinicalTrials.gov (NCT01413932) Pharmacokinetics - Pharmacodynamic Study of HT-2157 in Healthy Subjects and in Patients With Major Depressive Disorder. U.S. National Institutes of Health. | |||||
| REF 4 | 3-arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonists. J Med Chem. 2006 Jun 29;49(13):3757-8. | |||||
| REF 5 | 2,3-Dihydro-dithiin and -dithiepine-1,1,4,4-tetroxides: small molecule non-peptide antagonists of the human galanin hGAL-1 receptor. Bioorg Med Chem. 2000 Jun;8(6):1383-91. | |||||
| REF 6 | GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34. | |||||
| REF 7 | Galmic, a nonpeptide galanin receptor agonist, affects behaviors in seizure, pain, and forced-swim tests. Proc Natl Acad Sci U S A. 2004 Jul 13;101(28):10470-5. | |||||
| REF 8 | Galanin (2-11) binds to GalR3 in transfected cell lines: limitations for pharmacological definition of receptor subtypes. Neuropeptides. 2005 Jun;39(3):165-7. | |||||
| REF 9 | 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: 245). | |||||
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