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Target
Glycine receptor subunit alpha-3
Ligand
BDBM50229715
Substrate
n/a
Meas. Tech.
ChEMBL_1644301 (CHEMBL3993230)
EC50
50±n/a nM
Citation
 Bregman, H; Simard, JR; Andrews, KL; Ayube, S; Chen, H; Gunaydin, H; Guzman-Perez, A; Hu, J; Huang, L; Huang, X; Krolikowski, PH; Lehto, SG; Lewis, RT; Michelsen, K; Pegman, P; Plant, MH; Shaffer, PL; Teffera, Y; Yi, S; Zhang, M; Gingras, J; DiMauro, EF The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors. J Med Chem 60:1105-1125 (2017) [PubMed]  Article 
Target
Name:
Glycine receptor subunit alpha-3
Synonyms:
GLRA3 | GLRA3_HUMAN | Glycine receptor alpha-3/beta
Type:
PROTEIN
Mol. Mass.:
53809.29
Organism:
Homo sapiens (Human)
Description:
ChEMBL_967474
Residue:
464
Sequence:
MAHVRHFRTLVSGFYFWEAALLLSLVATKETDSARSRSAPMSPSDFLDKLMGRTSGYDARIRPNFKGPPVNVTCNIFINSFGSIAETTMDYRVNIFLRQKWNDPRLAYSEYPDDSLDLDPSMLDSIWKPDLFFANEKGANFHEVTTDNKLLRIFKNGNVLYSIRLTLTLSCPMDLKNFPMDVQTCIMQLESFGYTMNDLIFEWQDEAPVQVAEGLTLPQFLLKEEKDLRYCTKHYNTGKFTCIEVRFHLERQMGYYLIQMYIPSLLIVILSWVSFWINMDAAPARVALGITTVLTMTTQSSGSRASLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRKNKTEAFALEKFYRFSDMDDEVRESRFSFTAYGMGPCLQAKDGMTPKGPNHPVQVMPKSPDEMRKVFIDRAKKIDTISRACFPLAFLIFNIFYWVIYKILRHEDIHQQQD
  
Inhibitor
Name:
BDBM50229715
Synonyms:
CHEMBL4070615
Type:
Small organic molecule
Emp. Form.:
C19H19N3O5S
Mol. Mass.:
401.436
SMILES:
[H][C@]12CN([C@@H](C)[C@@]1([H])C(=O)N(C)c1ccncc21)S(=O)(=O)c1ccc2OCOc2c1 |r|
Structure:
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