| Reaction Details |
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 | Report a problem with these data |
| Target | Gamma-aminobutyric acid (GABA) B receptor 1/type B receptor subunit 2 [41-940] |
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| Ligand | BDBM24186 |
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| Substrate/Competitor | BDBM24183 |
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| Meas. Tech. | [3H]GABA Filtration Binding Assay (Ki) and FLIPR Assay for Agonism (EC50) |
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| pH | 7.4±n/a |
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| Temperature | 295.15±n/a K |
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| Ki | 2100±570 nM |
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| EC50 | 1100±n/a nM |
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| Citation |  Alstermark, C; Amin, K; Dinn, SR; Elebring, T; Fjellström, O; Fitzpatrick, K; Geiss, WB; Gottfries, J; Guzzo, PR; Harding, JP; Holmén, A; Kothare, M; Lehmann, A; Mattsson, JP; Nilsson, K; Sundén, G; Swanson, M; von Unge, S; Woo, AM; Wyle, MJ; Zheng, X Synthesis and pharmacological evaluation of novel gamma-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors. J Med Chem51:4315-20 (2008) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| |
| Gamma-aminobutyric acid (GABA) B receptor 1/type B receptor subunit 2 [41-940] |
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| Name: | Gamma-aminobutyric acid (GABA) B receptor 1/type B receptor subunit 2 [41-940] |
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| Synonyms: | gamma-Aminobutyric Acid Type B Receptor |
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| Type: | Heterodimer of GABA-B-R1 and GABA-B-R2. |
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| Mol. Mass.: | n/a |
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| Description: | Binding assays were using GABAb receptor sites in rat brain synaptic membranes. |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Gamma-aminobutyric acid (GABA) B receptor 1 |
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| 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 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 108221.06 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | Q6MFX8 |
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| Residue: | 960 |
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| Sequence: | MLLLLLVPLFLRPLGAGGAQTPNATSEGCQIIHPPWEGGIRYRGLTRDQVKAINFLPVDY
EIEYVCRGEREVVGPKVRKCLANGSWTDMDTPSRCVRICSKSYLTLENGKVFLTGGDLPA
LDGARVEFRCDPDFHLVGSSRSVCSQGQWSTPKPHCQVNRTPHSERRAVYIGALFPMSGG
WPGGQACQPAVEMALEDVNSRRDILPDYELKLIHHDSKCDPGQATKYLYELLYNDPIKII
LMPGCSSVSTLVAEAARMWNLIVLSYGSSSPALSNRQRFPTFFRTHPSATLHNPTRVKLF
EKWGWKKIATIQQTTEVFTSTLDDLEERVKEAGIEITFRQSFFSDPAVPVKNLKRQDARI
IVGLFYETEARKVFCEVYKERLFGKKYVWFLIGWYADNWFKTYDPSINCTVEEMTEAVEG
HITTEIVMLNPANTRSISNMTSQEFVEKLTKRLKRHPEETGGFQEAPLAYDAIWALALAL
NKTSGGGGRSGVRLEDFNYNNQTITDQIYRAMNSSSFEGVSGHVVFDASGSRMAWTLIEQ
LQGGSYKKIGYYDSTKDDLSWSKTDKWIGGSPPADQTLVIKTFRFLSQKLFISVSVLSSL
GIVLAVVCLSFNIYNSHVRYIQNSQPNLNNLTAVGCSLALAAVFPLGLDGYHIGRSQFPF
VCQARLWLLGLGFSLGYGSMFTKIWWVHTVFTKKEEKKEWRKTLEPWKLYATVGLLVGMD
VLTLAIWQIVDPLHRTIETFAKEEPKEDIDVSILPQLEHCSSKKMNTWLGIFYGYKGLLL
LLGIFLAYETKSVSTEKINDHRAVGMAIYNVAVLCLITAPVTMILSSQQDAAFAFASLAI
VFSSYITLVVLFVPKMRRLITRGEWQSETQDTMKTGSSTNNNEEEKSRLLEKENRELEKI
IAEKEERVSELRHQLQSRQQLRSRRHPPTPPDPSGGLPRGPSEPPDRLSCDGSRVHLLYK
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| Component 2 |
| Name: | Gamma-aminobutyric acid type B receptor subunit 2 [41-940] |
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| 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 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 101631.48 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | O88871[41-940] |
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| Residue: | 900 |
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| Sequence: | WTRGAPRPPPSSPPLSIMGLMPLTKEVAKGSIGRGVLPAVELAIEQIRNESLLRPYFLDL
RLYDTECDNAKGLKAFYDAIKYGPNHLMVFGGVCPSVTSIIAESLQGWNLVQLSFAATTP
VLADKKKYPYFFRTVPSDNAVNPAILKLLKHFRWRRVGTLTQDVQRFSEVRNDLTGVLYG
EDIEISDTESFSNDPCTSVKKLKGNDVRIILGQFDQNMAAKVFCCAFEESMFGSKYQWII
PGWYEPAWWEQVHVEANSSRCLRRSLLAAMEGYIGVDFEPLSSKQIKTISGKTPQQFERE
YNSKRSGVGPSKFHGYAYDGIWVIAKTLQRAMETLHASSRHQRIQDFNYTDHTLGKIILN
AMNETNFFGVTGQVVFRNGERMGTIKFTQFQDSREVKVGEYNAVADTLEIINDTIRFQGS
EPPKDKTIILEQLRKISLPLYSILSALTILGMIMASAFLFFNIKNRNQKLIKMSSPYMNN
LIILGGMLSYASIFLFGLDGSFVSEKTFETLCTVRTWILTVGYTTAFGAMFAKTWRVHAI
FKNVKMKKKIIKDQKLLVIVGGMLLIDLCILICWQAVDPLRRTVERYSMEPDPAGRDISI
RPLLEHCENTHMTIWLGIVYAYKGLLMLFGCFLAWETRNVSIPALNDSKYIGMSVYNVGI
MCIIGAAVSFLTRDQPNVQFCIVALVIIFCSTITLCLVFVPKLITLRTNPDAATQNRRFQ
FTQNQKKEDSKTSTSVTSVNQASTSRLEGLQSENHRLRMKITELDKDLEEVTMQLQDTPE
KTTYIKQNHYQELNDILSLGNFTESTDGGKAILKNHLDQNPQLQWNTTEPSRTCKDPIED
INSPEHIQRRLSLQLPILHHAYLPSIGGVDASCVSPCVSPTASPRHRHVPPSFRVMVSGL
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| BDBM24186 |
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| BDBM24183 |
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| Name | BDBM24186 |
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| Synonyms: | (3-amino-2-hydroxypropyl)phosphinic acid | 3-aminopropylphosphinic derivative, (R)-3 | 3-aminopropylphosphinic derivative, (S)-3 | 3-aminopropylphosphinic derivative, 3 | CGP35583 | CHEMBL113453 |
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| Type | Small organic molecule |
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| Emp. Form. | C3H8NO3P |
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| Mol. Mass. | 137.0743 |
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| SMILES | NCC(=O)CP(O)O |
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| Structure | 
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