| Reaction Details |
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 | Report a problem with these data |
| Target | Voltage-dependent L-type calcium channel subunit beta-3/N-type calcium channel subunit alpha-1B/calcium channel subunit alpha-2/delta-1 |
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| Ligand | BDBM246326 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Functional Drug Screening System (FDSS) |
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| IC50 | 21.5±n/a nM |
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| Citation |  Wall, M; Subasinghe, N; Sui, Z; Flores, C Substituted pyrazoles as N-type calcium channel blockers US Patent US9434693 Publication Date 9/6/2016 |
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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 beta-3/N-type calcium channel subunit alpha-1B/calcium channel subunit alpha-2/delta-1 |
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| Name: | Voltage-dependent L-type calcium channel subunit beta-3/N-type calcium channel subunit alpha-1B/calcium channel subunit alpha-2/delta-1 |
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| Synonyms: | N-type calcium channel subunits alpha 1B (Cav2.2) Beta 3 and Alpha 2 Delta | N-type calcium channel subunits alpha 1B (Cav2.2), Beta 3, and Alpha 2 Delta |
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| Type: | Enzyme |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | Voltage-dependent N-type calcium channel subunit alpha-1B |
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| Synonyms: | BIII | Brain calcium channel III | CAC1B_HUMAN | CACH5 | CACNA1B | CACNL1A5 | Calcium channel (Type N) | Calcium channel, L type, alpha-1 polypeptide isoform 5 | Voltage-dependent N-type calcium channel subunit alpha-1B | Voltage-dependent N-type calcium channel subunit alpha-1B/Voltage-dependent calcium channel subunit alpha-2/delta-1/Voltage-dependent L-type calcium channel subunit beta-3 | Voltage-gated N-type calcium channel alpha-1B subunit | Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1 | Voltage-gated calcium channel | Voltage-gated calcium channel subunit alpha Cav2.2 | Voltage-gated calcium channel subunit alpha Cav2.2 ((alpha 1B, beta 1b, alpha 2 delta-1) | calcium channel, voltage-dependent, N type, alpha 1B subunit |
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| Type: | Enzyme |
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| Mol. Mass.: | 262548.16 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q00975 |
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| Residue: | 2339 |
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| Sequence: | MVRFGDELGGRYGGPGGGERARGGGAGGAGGPGPGGLQPGQRVLYKQSIAQRARTMALYN
PIPVKQNCFTVNRSLFVFSEDNVVRKYAKRITEWPPFEYMILATIIANCIVLALEQHLPD
GDKTPMSERLDDTEPYFIGIFCFEAGIKIIALGFVFHKGSYLRNGWNVMDFVVVLTGILA
TAGTDFDLRTLRAVRVLRPLKLVSGIPSLQVVLKSIMKAMVPLLQIGLLLFFAILMFAII
GLEFYMGKFHKACFPNSTDAEPVGDFPCGKEAPARLCEGDTECREYWPGPNFGITNFDNI
LFAILTVFQCITMEGWTDILYNTNDAAGNTWNWLYFIPLIIIGSFFMLNLVLGVLSGEFA
KERERVENRRAFLKLRRQQQIERELNGYLEWIFKAEEVMLAEEDRNAEEKSPLDVLKRAA
TKKSRNDLIHAEEGEDRFADLCAVGSPFARASLKSGKTESSSYFRRKEKMFRFFIRRMVK
AQSFYWVVLCVVALNTLCVAMVHYNQPRRLTTTLYFAEFVFLGLFLTEMSLKMYGLGPRS
YFRSSFNCFDFGVIVGSVFEVVWAAIKPGSSFGISVLRALRLLRIFKVTKYWSSLRNLVV
SLLNSMKSIISLLFLLFLFIVVFALLGMQLFGGQFNFQDETPTTNFDTFPAAILTVFQIL
TGEDWNAVMYHGIESQGGVSKGMFSSFYFIVLTLFGNYTLLNVFLAIAVDNLANAQELTK
DEEEMEEAANQKLALQKAKEVAEVSPMSAANISIAARQQNSAKARSVWEQRASQLRLQNL
RASCEALYSEMDPEERLRFATTRHLRPDMKTHLDRPLVVELGRDGARGPVGGKARPEAAE
APEGVDPPRRHHRHRDKDKTPAAGDQDRAEAPKAESGEPGAREERPRPHRSHSKEAAGPP
EARSERGRGPGPEGGRRHHRRGSPEEAAEREPRRHRAHRHQDPSKECAGAKGERRARHRG
GPRAGPREAESGEEPARRHRARHKAQPAHEAVEKETTEKEATEKEAEIVEADKEKELRNH
QPREPHCDLETSGTVTVGPMHTLPSTCLQKVEEQPEDADNQRNVTRMGSQPPDPNTIVHI
PVMLTGPLGEATVVPSGNVDLESQAEGKKEVEADDVMRSGPRPIVPYSSMFCLSPTNLLR
RFCHYIVTMRYFEVVILVVIALSSIALAAEDPVRTDSPRNNALKYLDYIFTGVFTFEMVI
KMIDLGLLLHPGAYFRDLWNILDFIVVSGALVAFAFSGSKGKDINTIKSLRVLRVLRPLK
TIKRLPKLKAVFDCVVNSLKNVLNILIVYMLFMFIFAVIAVQLFKGKFFYCTDESKELER
DCRGQYLDYEKEEVEAQPRQWKKYDFHYDNVLWALLTLFTVSTGEGWPMVLKHSVDATYE
EQGPSPGYRMELSIFYVVYFVVFPFFFVNIFVALIIITFQEQGDKVMSECSLEKNERACI
DFAISAKPLTRYMPQNRQSFQYKTWTFVVSPPFEYFIMAMIALNTVVLMMKFYDAPYEYE
LMLKCLNIVFTSMFSMECVLKIIAFGVLNYFRDAWNVFDFVTVLGSITDILVTEIAETNN
FINLSFLRLFRAARLIKLLRQGYTIRILLWTFVQSFKALPYVCLLIAMLFFIYAIIGMQV
FGNIALDDDTSINRHNNFRTFLQALMLLFRSATGEAWHEIMLSCLSNQACDEQANATECG
SDFAYFYFVSFIFLCSFLMLNLFVAVIMDNFEYLTRDSSILGPHHLDEFIRVWAEYDPAA
CGRISYNDMFEMLKHMSPPLGLGKKCPARVAYKRLVRMNMPISNEDMTVHFTSTLMALIR
TALEIKLAPAGTKQHQCDAELRKEISVVWANLPQKTLDLLVPPHKPDEMTVGKVYAALMI
FDFYKQNKTTRDQMQQAPGGLSQMGPVSLFHPLKATLEQTQPAVLRGARVFLRQKSSTSL
SNGGAIQNQESGIKESVSWGTQRTQDAPHEARPPLERGHSTEIPVGRSGALAVDVQMQSI
TRRGPDGEPQPGLESQGRAASMPRLAAETQPVTDASPMKRSISTLAQRPRGTHLCSTTPD
RPPPSQASSHHHHHRCHRRRDRKQRSLEKGPSLSADMDGAPSSAVGPGLPPGEGPTGCRR
ERERRQERGRSQERRQPSSSSSEKQRFYSCDRFGGREPPKPKPSLSSHPTSPTAGQEPGP
HPQGSGSVNGSPLLSTSGASTPGRGGRRQLPQTPLTPRPSITYKTANSSPIHFAGAQTSL
PAFSPGRLSRGLSEHNALLQRDPLSQPLAPGSRIGSDPYLGQRLDSEASVHALPEDTLTF
EEAVATNSGRSSRTSYVSSLTSQSHPLRRVPNGYHCTLGLSSGGRARHSYHHPDQDHWC
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| Component 2 |
| Name: | Voltage-dependent L-type calcium channel subunit beta-3 |
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| Synonyms: | CACB3_HUMAN | CACNB3 | CACNLB3 | Calcium channel voltage-dependent subunit beta 3 |
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| Type: | Enzyme |
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| Mol. Mass.: | 54529.25 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P54284 |
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| Residue: | 484 |
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| Sequence: | MYDDSYVPGFEDSEAGSADSYTSRPSLDSDVSLEEDRESARREVESQAQQQLERAKHKPV
AFAVRTNVSYCGVLDEECPVQGSGVNFEAKDFLHIKEKYSNDWWIGRLVKEGGDIAFIPS
PQRLESIRLKQEQKARRSGNPSSLSDIGNRRSPPPSLAKQKQKQAEHVPPYDVVPSMRPV
VLVGPSLKGYEVTDMMQKALFDFLKHRFDGRISITRVTADLSLAKRSVLNNPGKRTIIER
SSARSSIAEVQSEIERIFELAKSLQLVVLDADTINHPAQLAKTSLAPIIVFVKVSSPKVL
QRLIRSRGKSQMKHLTVQMMAYDKLVQCPPESFDVILDENQLEDACEHLAEYLEVYWRAT
HHPAPGPGLLGPPSAIPGLQNQQLLGERGEEHSPLERDSLMPSDEASESSRQAWTGSSQR
SSRHLEEDYADAYQDLYQPHRQHTSGLPSANGHDPQDRLLAQDSEHNHSDRNWQRNRPWP
KDSY
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| Component 3 |
| Name: | Voltage-dependent calcium channel subunit alpha-2/delta-1 |
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| Synonyms: | CA2D1_HUMAN | CACNA2D1 | CACNL2A | CCHL2A | MHS3 | Voltage-dependent calcium channel subunit alpha-2-1 | Voltage-dependent calcium channel subunit delta-1 | Voltage-gated calcium channel | Voltage-gated calcium channel alpha2/delta subunit 1 | Voltage-gated calcium channel subunit alpha-2/delta-1 |
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| Type: | Enzyme |
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| Mol. Mass.: | 124544.88 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P54289 |
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| Residue: | 1103 |
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| Sequence: | MAAGCLLALTLTLFQSLLIGPSSEEPFPSAVTIKSWVDKMQEDLVTLAKTASGVNQLVDI
YEKYQDLYTVEPNNARQLVEIAARDIEKLLSNRSKALVRLALEAEKVQAAHQWREDFASN
EVVYYNAKDDLDPEKNDSEPGSQRIKPVFIEDANFGRQISYQHAAVHIPTDIYEGSTIVL
NELNWTSALDEVFKKNREEDPSLLWQVFGSATGLARYYPASPWVDNSRTPNKIDLYDVRR
RPWYIQGAASPKDMLILVDVSGSVSGLTLKLIRTSVSEMLETLSDDDFVNVASFNSNAQD
VSCFQHLVQANVRNKKVLKDAVNNITAKGITDYKKGFSFAFEQLLNYNVSRANCNKIIML
FTDGGEERAQEIFNKYNKDKKVRVFTFSVGQHNYDRGPIQWMACENKGYYYEIPSIGAIR
INTQEYLDVLGRPMVLAGDKAKQVQWTNVYLDALELGLVITGTLPVFNITGQFENKTNLK
NQLILGVMGVDVSLEDIKRLTPRFTLCPNGYYFAIDPNGYVLLHPNLQPKPIGVGIPTIN
LRKRRPNIQNPKSQEPVTLDFLDAELENDIKVEIRNKMIDGESGEKTFRTLVKSQDERYI
DKGNRTYTWTPVNGTDYSLALVLPTYSFYYIKAKLEETITQARYSETLKPDNFEESGYTF
IAPRDYCNDLKISDNNTEFLLNFNEFIDRKTPNNPSCNADLINRVLLDAGFTNELVQNYW
SKQKNIKGVKARFVVTDGGITRVYPKEAGENWQENPETYEDSFYKRSLDNDNYVFTAPYF
NKSGPGAYESGIMVSKAVEIYIQGKLLKPAVVGIKIDVNSWIENFTKTSIRDPCAGPVCD
CKRNSDVMDCVILDDGGFLLMANHDDYTNQIGRFFGEIDPSLMRHLVNISVYAFNKSYDY
QSVCEPGAAPKQGAGHRSAYVPSVADILQIGWWATAAAWSILQQFLLSLTFPRLLEAVEM
EDDDFTASLSKQSCITEQTQYFFDNDSKSFSGVLDCGNCSRIFHGEKLMNTNLIFIMVES
KGTCPCDTRLLIQAEQTSDGPNPCDMVKQPRYRKGPDVCFDNNVLEDYTDCGGVSGLNPS
LWYIIGIQFLLLWLVSGSTHRLL
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| BDBM246326 |
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| n/a |
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| Name | BDBM246326 |
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| Synonyms: | US9434693, 20 |
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| Type | Small organic molecule |
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| Emp. Form. | C24H28ClN3O4S |
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| Mol. Mass. | 490.015 |
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| SMILES | CC(C)Oc1ccccc1-n1nc(OC2CCN(CC2)S(C)(=O)=O)cc1-c1ccc(Cl)cc1 |
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| Structure | 
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