Target
Sodium- and chloride-dependent GABA transporter 1
Ligand
BDBM50563999
Substrate
n/a
Meas. Tech.
ChEMBL_2086323 (CHEMBL4767586)
Ki
5.1±n/a nM
Citation
 Zar?ba, PGryz?o, BMalawska, KSa?at, KHöfner, GCNowaczyk, AFija?kowski, ?Rapacz, APodkowa, AFurga?a, A?mudzki, PWanner, KTMalawska, BKulig, K Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice. Eur J Med Chem 188:0 (2020) [PubMed]  Article 
Target
Name:
Sodium- and chloride-dependent GABA transporter 1
Synonyms:
GABA transporter | Gabt1 | Gat-1 | Gat1 | SC6A1_RAT | Slc6a1 | Solute carrier family 6 member 1
Type:
PROTEIN
Mol. Mass.:
67006.26
Organism:
Rattus norvegicus
Description:
ChEMBL_1472611
Residue:
599
Sequence:
MATDNSKVADGQISTEVSEAPVASDKPKTLVVKVQKKAGDLPDRDTWKGRFDFLMSCVGYAIGLGNVWRFPYLCGKNGGGAFLIPYFLTLIFAGVPLFLLECSLGQYTSIGGLGVWKLAPMFKGVGLAAAVLSFWLNIYYIVIISWAIYYLYNSFTTTLPWKQCDNPWNTDRCFSNYSLVNTTNMTSAVVEFWERNMHQMTDGLDKPGQIRWPLAITLAIAWVLVYFCIWKGVGWTGKVVYFSATYPYIMLIILFFRGVTLPGAKEGILFYITPNFRKLSDSEVWLDAATQIFFSYGLGLGSLIALGSYNSFHNNVYRDSIIVCCINSCTSMFAGFVIFSIVGFMAHVTKRSIADVAASGPGLAFLAYPEAVTQLPISPLWAILFFSMLLMLGIDSQFCTVEGFITALVDEYPRLLRNRRELFIAAVCIVSYLIGLSNITQGGIYVFKLFDYYSASGMSLLFLVFFECVSISWFYGVNRFYDNIQEMVGSRPCIWWKLCWSFFTPIIVAGVFLFSAVQMTPLTMGSYVFPKWGQGVGWLMALSSMVLIPGYMAYMFLTLKGSLKQRLQVMIQPSEDIVRPENGPEQPQAGSSASKEAYI
  
Inhibitor
Name:
BDBM50563999
Synonyms:
CHEMBL4595698
Type:
Small organic molecule
Emp. Form.:
C21H20Cl2N2O3
Mol. Mass.:
419.301
SMILES:
OC(=O)C1=CCCN(CCO\N=C\c2ccccc2-c2ccc(Cl)cc2Cl)C1 |t:3|
Structure:
Search PDB for entries with ligand similarity: