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TargetVoltage-dependent T-type calcium channel subunit alpha-1H
LigandBDBM50452245
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1747257 (CHEMBL4181767)
IC50 40±n/a nM
Citation Bezençon, OHeidmann, BSiegrist, RStamm, SRichard, SPozzi, DCorminboeuf, ORoch, CKessler, MErtel, EAReymond, IPfeifer, Tde Kanter, RToeroek-Schafroth, MMoccia, LGMawet, JMoon, RRey, MCapeleto, BFournier, 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
More Info.:Get all data from this article,  Assay Method
 
Voltage-dependent T-type calcium channel subunit alpha-1H
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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  Blast E-value cutoff:
BDBM50452245
n/a
NameBDBM50452245
Synonyms:Act-709478
TypeSmall organic molecule
Emp. Form.C22H18F3N5O
Mol. Mass.425.4064
SMILESFC(F)(F)C1(CC1)c1ccc(CC(=O)Nc2ccn(Cc3ccc(cn3)C#N)n2)cc1
Structure
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