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Target
Probable G-protein coupled receptor 139
Ligand
BDBM263490
Substrate
n/a
Meas. Tech.
ChEMBL_2101648 (CHEMBL4810044)
Ki
76±n/a nM
Citation
 Reichard, HA; Schiffer, HH; Monenschein, H; Atienza, JM; Corbett, G; Skaggs, AW; Collia, DR; Ray, WJ; Serrats, J; Bliesath, J; Kaushal, N; Lam, BP; Amador-Arjona, A; Rahbaek, L; McConn, DJ; Mulligan, VJ; Brice, N; Gaskin, PLR; Cilia, J; Hitchcock, S Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia. J Med Chem 64:11527-11542 (2021) [PubMed]  Article 
Target
Name:
Probable G-protein coupled receptor 139
Synonyms:
G(q)-coupled orphan receptor GPRg1 | G-protein coupled receptor 139 | G-protein-coupled receptor PGR3 | GP139_HUMAN | GPR139 | GPRG1 | GPRG1 | PGR3 | Probable G-protein coupled receptor 139
Type:
PROTEIN
Mol. Mass.:
40700.34
Organism:
Homo sapiens (Human)
Description:
ChEMBL_109920
Residue:
353
Sequence:
MEHTHAHLAANSSLSWWSPGSACGLGFVPVVYYSLLLCLGLPANILTVIILSQLVARRQKSSYNYLLALAAADILVLFFIVFVDFLLEDFILNMQMPQVPDKIIEVLEFSSIHTSIWITVPLTIDRYIAVCHPLKYHTVSYPARTRKVIVSVYITCFLTSIPYYWWPNIWTEDYISTSVHHVLIWIHCFTVYLVPCSIFFILNSIIVYKLRRKSNFRLRGYSTGKTTAILFTITSIFATLWAPRIIMILYHLYGAPIQNRWLVHIMSDIANMLALLNTAINFFLYCFISKRFRTMAAATLKAFFKCQKQPVQFYTNHNFSITSSPWISPANSHCIKMLVYQYDKNGKPIKVSP
  
Inhibitor
Name:
BDBM263490
Synonyms:
(s)-2-(5-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4h)-yl)-n-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide | US10561662, Example 58 | US11173161, EX 58 | US9556130, test 58
Type:
Small organic molecule
Emp. Form.:
C19H17F3N4O4
Mol. Mass.:
422.3579
SMILES:
COc1cccc2nnn(CC(=O)N[C@@H](C)c3ccc(OC(F)(F)F)cc3)c(=O)c12 |r|
Structure:
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