Reaction Details |
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Target | Voltage-dependent L-type calcium channel subunit alpha-1C |
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Ligand | BDBM50029417 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_42931 (CHEMBL654574) |
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IC50 | 17±n/a nM |
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Citation | Campiani, G; Fiorini, I; De Filippis, MP; Ciani, SM; Garofalo, A; Nacci, V; Giorgi, G; Sega, A; Botta, M; Chiarini, A; Budriesi, R; Bruni, G; Romeo, MR; Manzoni, C; Mennini, T Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers. J Med Chem39:2922-38 (1996) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Voltage-dependent L-type calcium channel subunit alpha-1C |
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Name: | Voltage-dependent L-type calcium channel subunit alpha-1C |
Synonyms: | CAC1C_RAT | Cach2 | Cacn2 | Cacna1c | Cacnl1a1 | Calcium channel | Calcium channel (Type L) | Calcium channel diltiazem | Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle | Cchl1a1 | RBC | Rat brain class C | Voltage-dependent L-type calcium channel subunit alpha-1C | Voltage-gated L-type calcium channel | Voltage-gated L-type calcium channel alpha-1C subunit | Voltage-gated calcium channel subunit alpha Cav1.2 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 243492.26 |
Organism: | RAT |
Description: | Calcium channel 0 RAT::P22002 |
Residue: | 2169 |
Sequence: | MIRAFAQPSTPPYQPLSSCLSEDTERKFKGKVVHEAQLNCFYISPGGSNYGSPRPAHANM
NANAAAGLAPEHIPTPGAALSWLAAIDAARQAKLMGSAGNATISTVSSTQRKRQQYGKPK
KQGGTTATRPPRALLCLTLKNPIRRACISIVEWKPFEIIILLTIFANCVALAIYIPFPED
DSNATNSNLERVEYLFLIIFTVEAFLKVIAYGLLFHPNAYLRNGWNLLDFIIVVVGLFSA
ILEQATKADGANALGGKGAGFDVKALRAFRVLRPLRLVSGVPSLQVVLNSIIKAMVPLLH
IALLVLFVIIIYAIIGLELFMGKMHKTCYNQEGIIDVPAEEDPSPCALETGHGRQCQNGT
VCKPGWDGPKHGITNFDNFAFAMLTVFQCITMEGWTDVLYWMQDAMGYELPWVYFVSLVI
FGSFFVLNLVLGVLSGEFSKEREKAKARGDFQKLREKQQLEEDLKGYLDWITQAEDIDPE
NEDEGMDEDKPRNMSMPTSETESVNTENVAGGDIEGENCGARLAHRISKSKFSRYWRRWN
RFCRRKCRAAVKSNVFYWLVIFLVFLNTLTIASEHYNQPHWLTEVQDTANKALLALFTAE
MLLKMYSLGLQAYFVSLFNRFDCFIVCGGILETILVETKIMSPLGISCWRCVRLLRIFKI
TRYWNSLSNLVASLLNSLRSIASLLLLLFLFIIIFSLLGMQLFGGKFNFDEMQTRRSTFD
NFPQSLLTVFQILTGEDWNSVMYDGIMAYGGPSFPGMLVCIYFIILFISPNYILLNLFLA
IAVDNLADAESLTSAQKEEEEEKERKKLARTASPEKKQEVMEKPAVEESKEEKIELKSIT
ADGESPPTTKINMDDLQPSENEDKSPHSNPDTAGEEDEEEPEMPVGPRPRPLSELHLKEK
AVPMPEASAFFIFSPNNRFRLQCHRIVNDTIFTNLILFFILLSSISLAAEDPVQHTSFRN
HILFYFDIVFTTIFTIEIALKMTAYGAFLHKGSFCRNYFNILDLLVVSVSLISFGIQSSA
INVVKILRVLRVLRPLRINRAKGLKHVVQCVFVAIRTIGNIVIVTTLLQFMFACIGVQLF
KGKLYTCSDSSKQTEAESKGNYITYKTGEVDHPIIQPRSWENSKFDFDNVLAAMMALFTV
STFEGWPELLYRSIDSHTEDKGPIYNYRVEISIFFIIYIIIIAFFMMNIFVGFVIVTFQE
QGEQEYKNCELDKNQRQCVEYALKARPLPRYIPKNQHQYKVWYVVNSTYFEYLMFVLILL
NTICLAMQHYGQSCLFKIAMNILNMLFTGLFTVEMILKLIAFKPKHYFCDAWNTFDALIV
VGSIVDIAITEVHPAEHTQCSPSMSAEENSRISITFFRLFRVMRLVKLLSRGEGIRTLLW
TFIKSFQALPYVALLIVMLFFIYAVIGMQVFGKIALNDTTEINRNNNFQTFPQAVLLLFR
CATGEAWQDIMLACMPGKKCAPESEPSNSTEGETPCGSSFAVFYFISFYMLCAFLIINLF
VAVIMDNFDYLTRDWSILGPHHLDEFKRIWAEYDPEAKGRIKHLDVVTLLRRIQPPLGFG
KLCPHRVACKRLVSMNMPLNSDGTVMFNATLFALVRTALRIKTEGNLEQANEELRAIIKK
IWKRTSMKLLDQVVPPAGDDEVTVGKFYATFLIQEYFRKFKKRKEQGLVGKPSQRNALSL
QAGLRTLHDIGPEIRRAISGDLTAEEELDKAMKEAVSAASEDDIFRRAGGLFGNHVSYYQ
SDSRSNFPQTFATQRPLHINKTGNNQADTESPSHEKLVDSTFTPSSYSSTGSNANINNAN
NTALGRFPHPAGYSSTVSTVEGHGPPLSPAVRVQEAAWKLSSKRCHSRESQGATVSQDMF
PDETRSSVRLSEEVEYCSEPSLLSTDILSYQDDENRQLTCLEEDKREIQPCPKRSFLRSA
SLGRRASFHLECLKRQKDQGGDISQKTALPLHLVHHQALAVAGLSPLLQRSHSPSTFPRP
RPTPPVTPGSRGRPLQPIPTLRLEGAESSEKLNSSFPSIHCSSWSEETTACSGGSSMARR
ARPVSLTVPSQAGAPGRQFHGSASSLVEAVLISEGLGQFAQDPKFIEVTTQELADACDMT
IEEMENAADNILSGGAQQSPNGTLLPFVNCRDPGQDRAVVPEDESCVYALGRGRSEEALP
DSRSYVSNL
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BDBM50029417 |
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n/a |
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Name | BDBM50029417 |
Synonyms: | CHEMBL277363 | [4-(4-Methoxy-phenyl)-4H-benzo[b]pyrrolo[1,2-d][1,4]thiazin-1-ylmethyl]-dimethyl-amine |
Type | Small organic molecule |
Emp. Form. | C21H22N2OS |
Mol. Mass. | 350.477 |
SMILES | COc1ccc(cc1)C1Sc2ccccc2-n2c(CN(C)C)ccc12 |
Structure |
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