Reaction Details |
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Target | Voltage-dependent T-type calcium channel subunit alpha-1H |
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Ligand | BDBM50452245 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1747257 (CHEMBL4181767) |
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IC50 | 40±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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Voltage-dependent T-type calcium channel subunit alpha-1H |
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Name: | Voltage-dependent T-type calcium channel subunit alpha-1H |
Synonyms: | CAC1H_MOUSE | Cacna1h | Kiaa1120 | Voltage-dependent T-type calcium channel subunit alpha-1H | Voltage-gated calcium channel subunit alpha Cav3.2 |
Type: | PROTEIN |
Mol. Mass.: | 262043.32 |
Organism: | Mus musculus |
Description: | ChEMBL_109856 |
Residue: | 2365 |
Sequence: | MTEGTLAADEVRVPLGASPSAPAAPVRASPASPGVPGREEQRGSGSSVLAPESPGTECGA
DLGADEEQPVPYPALAATVFFCLGQTTRPRSWCLRLVSRRWFEHISMLVIMLNCVTLGMF
RPCEDVECRSERCSILEAFDDFIFAFFAVEMVIKMVALGLFGQKCYLGDTWNRLDFFIVM
AGMMEYSLDGHNVSLSAIRTVRVLRPLRAINRVPSMRILVTLLLDTLPMLGNVLLLCFFV
FFIFGIVGVQLWAGLLRNRCFLDSAFVRNNNLTFLRPYYQTEEGEENPFICSSRRDNGMQ
KCSHIPSRRELRVQCTLGWEAYGQPQAEDGGAGRNACINWNQYYNVCRSGEFNPHNGAIN
FDNIGYAWIAIFQVITLEGWVDIMYYVMDAHSFYNFIYFILLIIVGSFFMINLCLVVIAT
QFSETKQRENQLMREQRARYLSNDSTLASFSEPGSCYEELLKYVGHIFRKVKRRSLRLYA
RWQSRWRKKVDPSSTLHGQGPRRRPRRAGRRTASVHHLVYHHHHHHHHHYHFSHGGPRRP
SPEPGAGDTRLVRACVPPSPPSPGHGPPDSESVHSIYHADCHVEGPQERARVAHTIATAA
SLKLASGLGTMNYPTILPSGAVNSKGSTSSRPKGLRSAGTPGATAHSPLSLGSPSPYEKI
QHVVGEQGLGRASSHLSGLSVPCPLPSPQAGTLTCELKSCPYCASALEDPEFEFSGSESG
DSDAHGVYEFTQDVRHGDCRDPVQQPHEGGTPGHGNERWRPPLRTASQPGGLGRLWASFS
SKLRRIVDSKYFNRGIMAAILVNTLSMGVEYHEQPDELTNALEISNIVFTSMFALEMLLK
LLACGPLGYIRNPYNIFDGIVVIISVWEIVGQADGGLSVLRTFRLLRVLKLVRFLPALRR
QLVVLMRTMDNVATFCMLLMLFIFIFSILGMHLFGCKFSLKTDSGDTVPDRKNFDSLLWA
IVTVFQILTQEDWNVVLYNGMASTSSWAALYFVALMTFGNYVLFNLLVAILVEGFQAEGD
ATRSDTDEDKTSTHLEEDFDKLRDVQATEMKMYSLAVTPNGHLEGRGSLPPPLITHTAAT
PMPTPKSSPHLDMAHTLLDSRRSSSGSVDPQLGDQKSLASLRSSPCAPWGPNSAGSSRRS
SWNSLGRAPSLKRRSQCGERESLLSGEGKGSTDDEAEDSRPNSGTHPGASPGPRATPLRR
AESLGHRSTMDLCPPRPATLLPTKFRDCNGQMVALPSEFFLRIDSHKEDAAEFDDDIEDS
CCFRLHKVLEPYAPQWCSSRESWALYLFPPQNRLRVSCQKVIAHKMFDHVVLVFIFLNCI
TIALERPDIDPGSTERAFLSVSNYIFTAIFVVEMMVKVVALGLLWGEHAYLQSSWNVLDG
LLVLVSLVDIIVAVASAGGAKILGVLRVLRLLRTLRPLRVISRAPGLKLVVETLISSLRP
IGNIVLICCAFFIIFGILGVQLFKGKFYYCEGTDTRNITTKAECHAAHYRWVRRKYNFDN
LGQALMSLFVLSSKDGWVNIMYDGLDAVGIDQQPVQNHNPWMLLYFISFLLIVSFFVLNM
FVGVVVENFHKCRQHQEAEEARRREEKRLRRLERRRRSTFPNPEAQRRPYYADYSHTRRS
IHSLCTSHYLDLFITFIICLNVITMSMEHYNQPKSLDEALKYCNYVFTIVFVFEAALKLV
AFGFRRFFKDRWNQLDLAIVLLSIMGIALEEIEMNAALPINPTIIRIMRVLRIARVLKLL
KMATGMRALLDTVVQALPQVGNLGLLFMLLFFIYAALGVELFGRLECSEDNPCEGLSRHA
TFTNFGMAFLTLFRVSTGDNWNGIMKDTLRECTREDKHCLSYLPALSPVYFVTFVLVAQF
VLVNVVVAVLMKHLEESNKEAREDAEMDAEIELEIAQGSTAQPPSTAQESQGTEPDTPNL
LVVRKVSVSRMLSLPNDSYMFRPVAPAAAPHSHPLQEVEMETYTGPVTSAHSPSLEPRTS
FQVPSAASSPARVSDPLCALSPRDTPRSLSLSRILCRQEAMHAESLEGQIDDAGEDSIPD
YTEPAENISMSQAPLGTLRSPPCSPRPASVRTRKHTFGQHCISSRPPTLGGDDAEAADPA
DEEVSHITSSAHPWPATEPHSPEASPTASPAKGTVGSGRDPHRFCSVDAQSFLDKPGRPD
AQRWSSVELDNGDGHLESGEVRARASELEPALGARRKKKMSPPCISIDPPTEDEGSSRPP
AAEGGNTTLRRRTPSCEAALHRDCPESTEGPGTGGDPVAKGERWGQASCRAEHLTVPNFA
FEPLDMGGPGGDCFLDSDQSVTPEPRVSSLGAIVPLILETELSMPSGDPPEKEQGLYLTV
PQTPLKKPGSPPATPAPDDSGDEPV
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BDBM50452245 |
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n/a |
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Name | BDBM50452245 |
Synonyms: | Act-709478 |
Type | Small organic molecule |
Emp. Form. | C22H18F3N5O |
Mol. Mass. | 425.4064 |
SMILES | FC(F)(F)C1(CC1)c1ccc(CC(=O)Nc2ccn(Cc3ccc(cn3)C#N)n2)cc1 |
Structure |
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