| Reaction Details |
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 | Report a problem with these data |
| Target | T-type calcium channel alpha 1G subunit |
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| Ligand | BDBM50452245 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1747256 (CHEMBL4181766) |
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| IC50 | 6.4±n/a nM |
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| Citation |  Bezençon, O; Heidmann, B; Siegrist, R; Stamm, S; Richard, S; Pozzi, D; Corminboeuf, O; Roch, C; Kessler, M; Ertel, EA; Reymond, I; Pfeifer, T; de Kanter, R; Toeroek-Schafroth, M; Moccia, LG; Mawet, J; Moon, R; Rey, M; Capeleto, B; Fournier, E Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. J Med Chem60:9769-9789 (2017) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| T-type calcium channel alpha 1G subunit |
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| Name: | T-type calcium channel alpha 1G subunit |
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| Synonyms: | Cacna1g | T-type calcium channel alpha 1G subunit |
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| Type: | PROTEIN |
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| Mol. Mass.: | 250746.67 |
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| Organism: | Mus musculus |
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| Description: | ChEMBL_118081 |
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| Residue: | 2265 |
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| Sequence: | MDEEEDGAGAEESGQPRSFTQLNDLSGAGGRQGPGSTEKDPGSADSEAEGLPYPALAPVV
FFYLSQDSRPRSWCLRTVCNPWFERVSMLVILLNCVTLGMFRPCEDIACDSQRCRILQAF
DDFIFAFFAVEMVVKMVALGIFGKKCYLGDTWNRLDFFIVIAGMLEYSLDLQNVSFSAVR
TVRVLRPLRAINRVPSMRILVTLLLDTLPMLGNVLLLCFFVFFIFGIVGVQLWAGLLRNR
CFLPENFSLPLSVDLEPYYQTENEDESPFICSQPRENGMRSCRSVPTLRGEGGGGPPCGL
DYEAYNSSSNTTCVNWNQYYTNCSAGEHNPFKGAINFDNIGYAWIAIFQVITLEGWVDIM
YFVMDAHSFYNFIYFILLIIVGSFFMINLCLVVIATQFSETKQRESQLMREQRVRFLSNA
STLASFSEPGSCYEELLKYLVYILRKAARRLAQVSRAVGVRAGLLSSPVVRGGQEPQPSG
SCSRSHRRLSVHHLVHHHHHHHHHYHLGNGTLRVPRASPEIQDRDANGSRWLMLPPPSTP
TPSGGPPRGAESVHSFYHADCHLEPVRCQAPPPRSPSEASGRTVGSGKVYPTVHTSPPPE
MLKDKALVEVAPSPGPPTLTSFNIPPGPFSSMHKLLETQSTGACHSSCKISSPCSKADSG
ACGPDSCPYCARTGAGEPESADHEMPDSDSEAVYEFTQDAQHSDLRDPHRRRRPSLGPDA
EPSSVLAFWRLICDTFRKIVDSKYFGRGIMIAILVNTLSMGIEYHEQPEELTNALEISNI
VFTSLFALEMLLKLLVYGPFGYIKNPYNIFDGVIVVISVWEIVGQQGGGLSVLRTFRLMR
VLKLVRFLPALQRQLVVLMKTMDNVATFCMLLMLFIFIFSILGMHLFGCKFASERDGDTL
PDRKNFDSLLWAIVTVFQILTQEDWNKVLYNGMASTSSWAALYFIALMTFGNYVLFNLLV
AILVEGFQAEGDATKSESEPDFFSPSVDGDGDRKKRLALVALGEHSELRKSLLPPLIIHT
AATPMSLPKSSSTGVGEALGSGSRRTSSSGSAEPGTAHHEMKSPPSARSSPHSPWSAASS
WTSRRSSRNSLGRAPSLKRRSPSGERRSLLSGEGQESQDEEESSEEDRASPAGSDHRHRG
SLEREAKSSFDLPDTLQVPGLHRTASGRSSASEHQDCNGKSASGRLARTLRADDPPLDGD
DGDDEGNLSKGERLRAWVRARLPACCRERDSWSAYIFPPQSRFRLLCHRIITHKMFDHVV
LVIIFLNCITIAMERPKIDPHSAERIFLTLSNYIFTAVFLAEMTVKVVALGWCFGEQAYL
RSSWNVLDGLLVLISVIDILVSMVSDSGTKILGMLRVLRLLRTLRPLRVISRAQGLKLVV
ETLMSSLKPIGNIVVICCAFFIIFGILGVQLFKGKFFVCQGEDTRNITNKSDCAEASYRW
VRHKYNFDNLGQALMSLFVLASKDGWVDIMYDGLDAVGVDQQPIMNHNPWMLLYFISFLL
IVAFFVLNMFVGVVVENFHKCRQHQEEEEARRREEKRLKRLEKKRRNLMLDDVIASGSSA
SAASEAQCKPYYSDYSRFRLLVHHLCTSHYLDLFITGVIGLNVVTMAMEHYQQPQILDEA
LKICNYIFTVIFVLESVFKLVAFGFRRFFQDRWNQLDLAIVLLSIMGITLEEIEVNASLP
INPTIIRIMRVLRIARVLKLLKMAVGMRALLDTVMQALPQVGNLGLLFMLLFFIFAALGV
ELFGDLECDETHPCEGLGRHATFRNFGMAFLTLFRVSTGDNWNGIMKDTLRDCDQESTCY
NTVISPIYFVSFVLTAQFVLVNVVIAVLMKHLEESNKEAKEEAELEAELELEMKTLSPQP
HSPLGSPFLWPGVEGVNSPDSPKPGAPHTTAHIGAASSGFSLEHPTMVPHTEEGPVPLGP
DLLTVRKSGVSRTHSLPNDSYMCRNGSTAERSLGHRGWGLPKAQSGSILSVHSQPADTSC
ILQLPKDAHYLLQPHGAPTWGAIPKLPPPGRSPLAQRPLRRQAAIRTDSLDVQGLGSRED
LLSEVSGPSCPLTRSSSFWGGSSIQVQQRSGSQSKVSKHIRLPAPCPGLEPSWAKDPQET
RSSLELDTELSWISGDLLPSSQEEPLSPRDLKKCYSVEAQSCRRRPGSWLDEQRRHSIAV
SCLDSGSQPRLCPSPSSLGGQPLGGPGSRPKKKLSPPSISIDPPESQGPRPPCSPGVCLR
RRAPASDSKDPSASSPLDSTAASPSPKKDALSLSGLSSDPTDLDP
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| BDBM50452245 |
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| n/a |
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| Name | BDBM50452245 |
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| Synonyms: | Act-709478 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H18F3N5O |
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| Mol. Mass. | 425.4064 |
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| SMILES | FC(F)(F)C1(CC1)c1ccc(CC(=O)Nc2ccn(Cc3ccc(cn3)C#N)n2)cc1 |
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| Structure | 
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