Target Information
| Target General Information | Top | |||||
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| Target ID |
T84439
(Former ID: TTDI03232)
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| Target Name |
G-protein-coupled receptor PGR3 (GPR139)
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| Synonyms |
Probable G-protein coupled receptor 139; PGR3; GPRG1; G(q)-coupled orphan receptor GPRg1
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| Gene Name |
GPR139
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Sex development malformative disorder [ICD-11: LD2A] | |||||
| Function |
Orphan receptor. Seems to act through a G(q/11)-mediated pathway.
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| UniProt ID | ||||||
| Sequence |
MEHTHAHLAANSSLSWWSPGSACGLGFVPVVYYSLLLCLGLPANILTVIILSQLVARRQK
SSYNYLLALAAADILVLFFIVFVDFLLEDFILNMQMPQVPDKIIEVLEFSSIHTSIWITV PLTIDRYIAVCHPLKYHTVSYPARTRKVIVSVYITCFLTSIPYYWWPNIWTEDYISTSVH HVLIWIHCFTVYLVPCSIFFILNSIIVYKLRRKSNFRLRGYSTGKTTAILFTITSIFATL WAPRIIMILYHLYGAPIQNRWLVHIMSDIANMLALLNTAINFFLYCFISKRFRTMAAATL KAFFKCQKQPVQFYTNHNFSITSSPWISPANSHCIKMLVYQYDKNGKPIKVSP Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | TAK-041 | Drug Info | Phase 1 | XY disorder of sex development due to androgen resistance | [1] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Agonist | [+] 2 Agonist drugs | + | ||||
| 1 | TAK-041 | Drug Info | [1] | |||
| 2 | PMID24900311C1a | Drug Info | [2] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide | Ligand Info | |||||
| Structure Description | Cryo-EM structure of a class A orphan GPCR in complex with Gi | PDB:7VUG | ||||
| Method | Electron microscopy | Resolution | 3.20 Å | Mutation | Yes | [3] |
| PDB Sequence |
CGLGFVPVVY
32 YSLLLCLGLP42 ANILTVIILS52 QLVARRQKSV62 YNYLLALAAA72 DILVLFFIVF 82 VDFLLEDFIL92 NMQMPQVPDK102 IIEVLEFSSI112 HTSIWITVPL122 TIDRYIAVCH 132 PLKYHTVSYP142 ARTRKVIVSV152 YITCFLTSIP162 YYWWPNIWTE172 DYISTSVHHV 182 LIWIHCFTVY192 LVPCSIFFIL202 NSIIVYKLRR212 KSNFRLRGYS222 TGKTTAILFT 232 ITSIFATLWA242 PRIIMILYHL252 YGAPIQNRWL262 VHIMSDIANM272 LALLNTAINF 282 FLYCFISKRF292 RTMAAATLKA302 FF
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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| Chemical Structure based Activity Landscape of Target | Top |
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| References | Top | |||||
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| REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | Discovery and SAR of a Series of Agonists at Orphan G Protein-Coupled Receptor 139. ACS Med Chem Lett. 2011 Feb 28;2(4):303-6. | |||||
| REF 3 | Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139. Cell Res. 2022 Feb;32(2):210-213. | |||||
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