Reaction Details Report a problem with these data
Target
Urotensin-2 receptor
Ligand
BDBM50249878
Substrate
n/a
Meas. Tech.
ChEMBL_954177 (CHEMBL2351692)
IC50
6.0±n/a nM
Citation
Taylor, SJ; Soleymanzadeh, F; Muegge, I; Akiba, I; Taki, N; Ueda, S; Mainolfi, E; Eldrup, AB Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists. Bioorg Med Chem Lett 23:2177-80 (2013) [PubMed] Article
More Info.:
Target
Name:
Urotensin-2 receptor
Synonyms:
G-protein coupled receptor 14 | GPR14 | UR-II-R | UR2R_HUMAN | UTS2R | Urotensin II receptor | Urotensin-II
Type:
Enzyme Catalytic Domain
Mol. Mass.:
42159.71
Organism:
Homo sapiens (Human)
Description:
Urotensin-II UTS2R HUMAN::Q9UKP6
Residue:
389
Sequence:
MALTPESPSSFPGLAATGSSVPEPPGGPNATLNSSWASPTEPSSLEDLVATGTIGTLLSAMGVVGVVGNAYTLVVTCRSLRAVASMYVYVVNLALADLLYLLSIPFIVATYVTKEWHFGDVGCRVLFGLDFLTMHASIFTLTVMSSERYAAVLRPLDTVQRPKGYRKLLALGTWLLALLLTLPVMLAMRLVRRGPKSLCLPAWGPRAHRAYLTLLFATSIAGPGLLIGLLYARLARAYRRSQRASFKRARRPGARALRLVLGIVLLFWACFLPFWLWQLLAQYHQAPLAPRTARIVNYLTTCLTYGNSCANPFLYTLLTRNYRDHLRGRVRGPGSGGGRGPVPSLQPRARFQRCSGRSLSSCSPQPTDSLVLAPAAPARPAPEGPRAPA
Inhibitor
Name:
BDBM50249878
Synonyms:
(R)-2-bromo-4,5-dimethoxy-N-(3-(1-methylpyrrolidin-3-yloxy)-4-(trifluoromethyl)phenyl)benzenesulfonamide | CHEMBL522770 | SB-706375
Type:
Small organic molecule
Emp. Form.:
C20H22BrF3N2O5S
Mol. Mass.:
539.363
SMILES:
COc1cc(Br)c(cc1OC)S(=O)(=O)Nc1ccc(c(O[C@@H]2CCN(C)C2)c1)C(F)(F)F |r|