Reaction Details Report a problem with these data
Target
Gamma-aminobutyric acid type B receptor subunit 1
Ligand
BDBM24182
Substrate
n/a
Meas. Tech.
ChEMBL_321555 (CHEMBL881969)
IC50
50±n/a nM
Citation
 Minetti, P; Tinti, MO; Carminati, P; Castorina, M; Di Cesare, MA; Di Serio, S; Gallo, G; Ghirardi, O; Giorgi, F; Giorgi, L; Piersanti, G; Bartoccini, F; Tarzia, G 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. J Med Chem 48:6887-96 (2005) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid type B receptor subunit 1
Synonyms:
GABA B | GABA B receptor | GABA uptake | GABA-B receptor 1 | GABA-B-R1 | GABA-BR1 | GABABR1 | GABR1_RAT | Gabbr1 | Gb1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
111548.69
Organism:
Rattus norvegicus (Rat)
Description:
Q9Z0U4
Residue:
991
Sequence:
MLLLLLVPLFLRPLGAGGAQTPNATSEGCQIIHPPWEGGIRYRGLTRDQVKAINFLPVDYEIEYVCRGEREVVGPKVRKCLANGSWTDMDTPSRCVRICSKSYLTLENGKVFLTGGDLPALDGARVEFRCDPDFHLVGSSRSVCSQGQWSTPKPHCQVNRTPHSERRAVYIGALFPMSGGWPGGQACQPAVEMALEDVNSRRDILPDYELKLIHHDSKCDPGQATKYLYELLYNDPIKIILMPGCSSVSTLVAEAARMWNLIVLSYGSSSPALSNRQRFPTFFRTHPSATLHNPTRVKLFEKWGWKKIATIQQTTEVFTSTLDDLEERVKEAGIEITFRQSFFSDPAVPVKNLKRQDARIIVGLFYETEARKVFCEVYKERLFGKKYVWFLIGWYADNWFKTYDPSINCTVEEMTEAVEGHITTEIVMLNPANTRSISNMTSQEFVEKLTKRLKRHPEETGGFQEAPLAYDAIWALALALNKTSGGGGRSGVRLEDFNYNNQTITDQIYRAMNSSSFEGVSGHVVFDASGSRMAWTLIEQLQGGSYKKIGYYDSTKDDLSWSKTDKWIGGSPPADQTLVIKTFRFLSQKLFISVSVLSSLGIVLAVVCLSFNIYNSHVRYIQNSQPNLNNLTAVGCSLALAAVFPLGLDGYHIGRSQFPFVCQARLWLLGLGFSLGYGSMFTKIWWVHTVFTKKEEKKEWRKTLEPWKLYATVGLLVGMDVLTLAIWQIVDPLHRTIETFAKEEPKEDIDVSILPQLEHCSSKKMNTWLGELWSFAVSSDVQRRATVGGDSPICVWPAPESIFYGYKGLLLLLGIFLAYETKSVSTEKINDHRAVGMAIYNVAVLCLITAPVTMILSSQQDAAFAFASLAIVFSSYITLVVLFVPKMRRLITRGEWQSETQDTMKTGSSTNNNEEEKSRLLEKENRELEKIIAEKEERVSELRHQLQSRQQLRSRRHPPTPPDPSGGLPRGPSEPPDRLSCDGSRVHLLYK
  
Inhibitor
Name:
BDBM24182
Synonyms:
4-amino-3-(4-chlorophenyl)butanoic acid | Baclofen | Baclophen | CHEMBL701 | Gabalon | Lioresal
Type:
Small organic molecule
Emp. Form.:
C10H12ClNO2
Mol. Mass.:
213.661
SMILES:
NCC(CC(O)=O)c1ccc(Cl)cc1
Structure:
Search PDB for entries with ligand similarity: