Target
Gamma-aminobutyric acid (GABA) B receptor 1/type B receptor subunit 2 [41-940]
Ligand
BDBM24186
Substrate
BDBM24183
Meas. Tech.
[3H]GABA Filtration Binding Assay (Ki) and FLIPR Assay for Agonism (EC50)
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
94±32 nM
EC50
220±29 nM
Citation
 Alstermark, CAmin, KDinn, SRElebring, TFjellström, OFitzpatrick, KGeiss, WBGottfries, JGuzzo, PRHarding, JPHolmén, AKothare, MLehmann, AMattsson, JPNilsson, KSundén, GSwanson, Mvon Unge, SWoo, AMWyle, MJZheng, X Synthesis and pharmacological evaluation of novel gamma-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors. J Med Chem 51:4315-20 (2008) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid (GABA) B receptor 1/type B receptor subunit 2 [41-940]
Synonyms:
gamma-Aminobutyric Acid Type B Receptor
Type:
Heterodimer of GABA-B-R1 and GABA-B-R2.
Mol. Mass.:
n/a
Description:
Binding assays were using GABAb receptor sites in rat brain synaptic membranes.
Components:
This complex has 2 components.
Component 1
Name:
Gamma-aminobutyric acid (GABA) B receptor 1
Synonyms:
GABA-B receptor 1 | GABA-B-R1 | Gamma-aminobutyric acid type B receptor subunit 1 (GABA) | Gb1 | gamma-Aminobutyric Acid Type B Receptor Subunit 1
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
108221.06
Organism:
Rattus norvegicus (rat)
Description:
Q6MFX8
Residue:
960
Sequence:
MLLLLLVPLFLRPLGAGGAQTPNATSEGCQIIHPPWEGGIRYRGLTRDQVKAINFLPVDYEIEYVCRGEREVVGPKVRKCLANGSWTDMDTPSRCVRICSKSYLTLENGKVFLTGGDLPALDGARVEFRCDPDFHLVGSSRSVCSQGQWSTPKPHCQVNRTPHSERRAVYIGALFPMSGGWPGGQACQPAVEMALEDVNSRRDILPDYELKLIHHDSKCDPGQATKYLYELLYNDPIKIILMPGCSSVSTLVAEAARMWNLIVLSYGSSSPALSNRQRFPTFFRTHPSATLHNPTRVKLFEKWGWKKIATIQQTTEVFTSTLDDLEERVKEAGIEITFRQSFFSDPAVPVKNLKRQDARIIVGLFYETEARKVFCEVYKERLFGKKYVWFLIGWYADNWFKTYDPSINCTVEEMTEAVEGHITTEIVMLNPANTRSISNMTSQEFVEKLTKRLKRHPEETGGFQEAPLAYDAIWALALALNKTSGGGGRSGVRLEDFNYNNQTITDQIYRAMNSSSFEGVSGHVVFDASGSRMAWTLIEQLQGGSYKKIGYYDSTKDDLSWSKTDKWIGGSPPADQTLVIKTFRFLSQKLFISVSVLSSLGIVLAVVCLSFNIYNSHVRYIQNSQPNLNNLTAVGCSLALAAVFPLGLDGYHIGRSQFPFVCQARLWLLGLGFSLGYGSMFTKIWWVHTVFTKKEEKKEWRKTLEPWKLYATVGLLVGMDVLTLAIWQIVDPLHRTIETFAKEEPKEDIDVSILPQLEHCSSKKMNTWLGIFYGYKGLLLLLGIFLAYETKSVSTEKINDHRAVGMAIYNVAVLCLITAPVTMILSSQQDAAFAFASLAIVFSSYITLVVLFVPKMRRLITRGEWQSETQDTMKTGSSTNNNEEEKSRLLEKENRELEKIIAEKEERVSELRHQLQSRQQLRSRRHPPTPPDPSGGLPRGPSEPPDRLSCDGSRVHLLYK
  
Component 2
Name:
Gamma-aminobutyric acid type B receptor subunit 2 [41-940]
Synonyms:
G-protein coupled receptor 51 | GABA-B receptor 2 | GABA-B-R2 | GABABR2 | GABR2_RAT | Gabbr2 | Gb2 | Gpr51 | gamma-Aminobutyric Acid Type B Receptor Subunit 2
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
101631.48
Organism:
Rattus norvegicus (rat)
Description:
O88871[41-940]
Residue:
900
Sequence:
WTRGAPRPPPSSPPLSIMGLMPLTKEVAKGSIGRGVLPAVELAIEQIRNESLLRPYFLDLRLYDTECDNAKGLKAFYDAIKYGPNHLMVFGGVCPSVTSIIAESLQGWNLVQLSFAATTPVLADKKKYPYFFRTVPSDNAVNPAILKLLKHFRWRRVGTLTQDVQRFSEVRNDLTGVLYGEDIEISDTESFSNDPCTSVKKLKGNDVRIILGQFDQNMAAKVFCCAFEESMFGSKYQWIIPGWYEPAWWEQVHVEANSSRCLRRSLLAAMEGYIGVDFEPLSSKQIKTISGKTPQQFEREYNSKRSGVGPSKFHGYAYDGIWVIAKTLQRAMETLHASSRHQRIQDFNYTDHTLGKIILNAMNETNFFGVTGQVVFRNGERMGTIKFTQFQDSREVKVGEYNAVADTLEIINDTIRFQGSEPPKDKTIILEQLRKISLPLYSILSALTILGMIMASAFLFFNIKNRNQKLIKMSSPYMNNLIILGGMLSYASIFLFGLDGSFVSEKTFETLCTVRTWILTVGYTTAFGAMFAKTWRVHAIFKNVKMKKKIIKDQKLLVIVGGMLLIDLCILICWQAVDPLRRTVERYSMEPDPAGRDISIRPLLEHCENTHMTIWLGIVYAYKGLLMLFGCFLAWETRNVSIPALNDSKYIGMSVYNVGIMCIIGAAVSFLTRDQPNVQFCIVALVIIFCSTITLCLVFVPKLITLRTNPDAATQNRRFQFTQNQKKEDSKTSTSVTSVNQASTSRLEGLQSENHRLRMKITELDKDLEEVTMQLQDTPEKTTYIKQNHYQELNDILSLGNFTESTDGGKAILKNHLDQNPQLQWNTTEPSRTCKDPIEDINSPEHIQRRLSLQLPILHHAYLPSIGGVDASCVSPCVSPTASPRHRHVPPSFRVMVSGL
  
Inhibitor
Name:
BDBM24186
Synonyms:
(3-amino-2-hydroxypropyl)phosphinic acid | 3-aminopropylphosphinic derivative, (R)-3 | 3-aminopropylphosphinic derivative, (S)-3 | 3-aminopropylphosphinic derivative, 3 | CGP35583 | CHEMBL113453
Type:
Small organic molecule
Emp. Form.:
C3H8NO3P
Mol. Mass.:
137.0743
SMILES:
NCC(=O)CP(O)O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM24183
Synonyms:
4-amino-n-[2,3-3H]butyric acid | 4-aminobutanoic acid | Aminalon | CHEMBL96 | GABA | Gamma-Aminobutyric acid | [3H]GABA | cid_119
Type:
Radiolabeled ligand
Emp. Form.:
C4H9NO2
Mol. Mass.:
103.1198
SMILES:
NCCCC(O)=O
Structure:
Search PDB for entries with ligand similarity: