Reaction Details |
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Target | Metabotropic glutamate receptor 8 |
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Ligand | BDBM50121643 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1518616 (CHEMBL3619431) |
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IC50 | >12500±n/a nM |
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Citation | Monn, JA; Prieto, L; Taboada, L; Hao, J; Reinhard, MR; Henry, SS; Beadle, CD; Walton, L; Man, T; Rudyk, H; Clark, B; Tupper, D; Baker, SR; Lamas, C; Montero, C; Marcos, A; Blanco, J; Bures, M; Clawson, DK; Atwell, S; Lu, F; Wang, J; Russell, M; Heinz, BA; Wang, X; Carter, JH; Getman, BG; Catlow, JT; Swanson, S; Johnson, BG; Shaw, DB; McKinzie, DL Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective J Med Chem58:7526-48 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Metabotropic glutamate receptor 8 |
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Name: | Metabotropic glutamate receptor 8 |
Synonyms: | GPRC1H | GRM8 | GRM8_HUMAN | MGLUR8 | Metabotropic glutamate receptor 8 | metabotropic glutamate 8 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 101759.58 |
Organism: | Homo sapiens (Human) |
Description: | metabotropic glutamate 8 GRM8 HUMAN::O00222 |
Residue: | 908 |
Sequence: | MVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGER
GVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFV
QALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTA
PELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISR
EIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQS
GHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFA
EFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMH
KDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITN
KSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCER
CEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTF
VIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMC
FSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPH
IIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEA
KPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYI
IIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTY
ISYSNHSI
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BDBM50121643 |
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n/a |
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Name | BDBM50121643 |
Synonyms: | CHEMBL3616847 |
Type | Small organic molecule |
Emp. Form. | C10H12N4O4S |
Mol. Mass. | 284.292 |
SMILES | [H][C@]12[C@H](C(O)=O)[C@@]1([H])[C@@](N)(C[C@H]2Sc1nnc[nH]1)C(O)=O |r| |
Structure |
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