Reaction Details |
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Target | Metabotropic glutamate receptor 8 |
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Ligand | BDBM50301520 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_600495 (CHEMBL1046442) |
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IC50 | >10000±n/a nM |
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Citation | Satoh, A; Nagatomi, Y; Hirata, Y; Ito, S; Suzuki, G; Kimura, T; Maehara, S; Hikichi, H; Satow, A; Hata, M; Ohta, H; Kawamoto, H Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist. Bioorg Med Chem Lett19:5464-8 (2009) [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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BDBM50301520 |
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n/a |
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Name | BDBM50301520 |
Synonyms: | 4-fluoro-N-(4-(6-(isopropylamino)pyrimidin-4-yl)thiazol-2-yl)-N-methylbenzamide | CHEMBL566581 |
Type | Small organic molecule |
Emp. Form. | C18H18FN5OS |
Mol. Mass. | 371.432 |
SMILES | CC(C)Nc1cc(ncn1)-c1csc(n1)N(C)C(=O)c1ccc(F)cc1 |
Structure |
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