Target
Probable G-protein coupled receptor 139
Ligand
BDBM263504
Substrate
n/a
Meas. Tech.
ChEMBL_2101648 (CHEMBL4810044)
Ki
33±n/a nM
Citation
 Reichard, HASchiffer, HHMonenschein, HAtienza, JMCorbett, GSkaggs, AWCollia, DRRay, WJSerrats, JBliesath, JKaushal, NLam, BPAmador-Arjona, ARahbaek, LMcConn, DJMulligan, VJBrice, NGaskin, PLRCilia, JHitchcock, 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:
BDBM263504
Synonyms:
(s)?n-(1-(2-fluoro-4-(trifluoromethoxy)phenyl)ethyl)-2-(5-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4h)-yl)acetamide | US10561662, Example 72 | US11173161, EX 72 | US9556130, test 72
Type:
Small organic molecule
Emp. Form.:
C19H16F4N4O4
Mol. Mass.:
440.3484
SMILES:
COc1cccc2nnn(CC(=O)N[C@@H](C)c3ccc(OC(F)(F)F)cc3F)c(=O)c12 |r|
Structure:
Search PDB for entries with ligand similarity: