Reaction Details |
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Target | Sodium channel protein type 5 subunit alpha |
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Ligand | BDBM371772 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1995818 (CHEMBL4629713) |
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IC50 | 2516±n/a nM |
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Citation | Ramdas, V; Talwar, R; Kanoje, V; Loriya, RM; Banerjee, M; Patil, P; Joshi, AA; Datrange, L; Das, AK; Walke, DS; Kalhapure, V; Khan, T; Gote, G; Dhayagude, U; Deshpande, S; Shaikh, J; Chaure, G; Pal, RR; Parkale, S; Suravase, S; Bhoskar, S; Gupta, RV; Kalia, A; Yeshodharan, R; Azhar, M; Daler, J; Mali, V; Sharma, G; Kishore, A; Vyawahare, R; Agarwal, G; Pareek, H; Budhe, S; Nayak, A; Warude, D; Gupta, PK; Joshi, P; Joshi, S; Darekar, S; Pandey, D; Wagh, A; Nigade, PB; Mehta, M; Patil, V; Modi, D; Pawar, S; Verma, M; Singh, M; Das, S; Gundu, J; Nemmani, K; Bock, MG; Sharma, S; Bakhle, D; Kamboj, RK; Palle, VP Discovery of Potent, Selective, and State-Dependent Na J Med Chem63:6107-6133 (2020) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Sodium channel protein type 5 subunit alpha |
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Name: | Sodium channel protein type 5 subunit alpha |
Synonyms: | HH1 | SCN5A | SCN5A_HUMAN | Sodium channel alpha subunit | Sodium channel protein type 5 subunit alpha/beta-1/beta-2 | Sodium channel protein type V alpha subunit | Voltage-gated sodium channel subunit alpha Nav1.5 |
Type: | Enzyme |
Mol. Mass.: | 226908.60 |
Organism: | Homo sapiens (Human) |
Description: | Q14524 |
Residue: | 2016 |
Sequence: | MANFLLPRGTSSFRRFTRESLAAIEKRMAEKQARGSTTLQESREGLPEEEAPRPQLDLQA
SKKLPDLYGNPPQELIGEPLEDLDPFYSTQKTFIVLNKGKTIFRFSATNALYVLSPFHPI
RRAAVKILVHSLFNMLIMCTILTNCVFMAQHDPPPWTKYVEYTFTAIYTFESLVKILARG
FCLHAFTFLRDPWNWLDFSVIIMAYTTEFVDLGNVSALRTFRVLRALKTISVISGLKTIV
GALIQSVKKLADVMVLTVFCLSVFALIGLQLFMGNLRHKCVRNFTALNGTNGSVEADGLV
WESLDLYLSDPENYLLKNGTSDVLLCGNSSDAGTCPEGYRCLKAGENPDHGYTSFDSFAW
AFLALFRLMTQDCWERLYQQTLRSAGKIYMIFFMLVIFLGSFYLVNLILAVVAMAYEEQN
QATIAETEEKEKRFQEAMEMLKKEHEALTIRGVDTVSRSSLEMSPLAPVNSHERRSKRRK
RMSSGTEECGEDRLPKSDSEDGPRAMNHLSLTRGLSRTSMKPRSSRGSIFTFRRRDLGSE
ADFADDENSTAGESESHHTSLLVPWPLRRTSAQGQPSPGTSAPGHALHGKKNSTVDCNGV
VSLLGAGDPEATSPGSHLLRPVMLEHPPDTTTPSEEPGGPQMLTSQAPCVDGFEEPGARQ
RALSAVSVLTSALEELEESRHKCPPCWNRLAQRYLIWECCPLWMSIKQGVKLVVMDPFTD
LTITMCIVLNTLFMALEHYNMTSEFEEMLQVGNLVFTGIFTAEMTFKIIALDPYYYFQQG
WNIFDSIIVILSLMELGLSRMSNLSVLRSFRLLRVFKLAKSWPTLNTLIKIIGNSVGALG
NLTLVLAIIVFIFAVVGMQLFGKNYSELRDSDSGLLPRWHMMDFFHAFLIIFRILCGEWI
ETMWDCMEVSGQSLCLLVFLLVMVIGNLVVLNLFLALLLSSFSADNLTAPDEDREMNNLQ
LALARIQRGLRFVKRTTWDFCCGLLRQRPQKPAALAAQGQLPSCIATPYSPPPPETEKVP
PTRKETRFEEGEQPGQGTPGDPEPVCVPIAVAESDTDDQEEDEENSLGTEEESSKQQESQ
PVSGGPEAPPDSRTWSQVSATASSEAEASASQADWRQQWKAEPQAPGCGETPEDSCSEGS
TADMTNTAELLEQIPDLGQDVKDPEDCFTEGCVRRCPCCAVDTTQAPGKVWWRLRKTCYH
IVEHSWFETFIIFMILLSSGALAFEDIYLEERKTIKVLLEYADKMFTYVFVLEMLLKWVA
YGFKKYFTNAWCWLDFLIVDVSLVSLVANTLGFAEMGPIKSLRTLRALRPLRALSRFEGM
RVVVNALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFGRCINQTEGDLPLNYTIVNN
KSQCESLNLTGELYWTKVKVNFDNVGAGYLALLQVATFKGWMDIMYAAVDSRGYEEQPQW
EYNLYMYIYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKK
LGSKKPQKPIPRPLNKYQGFIFDIVTKQAFDVTIMFLICLNMVTMMVETDDQSPEKINIL
AKINLLFVAIFTGECIVKLAALRHYYFTNSWNIFDFVVVILSIVGTVLSDIIQKYFFSPT
LFRVIRLARIGRILRLIRGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMANFA
YVKWEAGIDDMFNFQTFANSMLCLFQITTSAGWDGLLSPILNTGPPYCDPTLPNSNGSRG
DCGSPAVGILFFTTYIIISFLIVVNMYIAIILENFSVATEESTEPLSEDDFDMFYEIWEK
FDPEATQFIEYSVLSDFADALSEPLRIAKPNQISLINMDLPMVSGDRIHCMDILFAFTKR
VLGESGEMDALKIQMEEKFMAANPSKISYEPITTTLRRKHEEVSAMVIQRAFRRHLLQRS
LKHASFLFRQQAGSGLSEEDAPEREGLIAYVMSENFSRPLGPPSSSSISSTSFPPSYDSV
TRATSDNLQVRGSDYSHSEDLADFPPSPDRDRESIV
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BDBM371772 |
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n/a |
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Name | BDBM371772 |
Synonyms: | (R)-4-(2-(5-fluoropyridin-2-yl)-4-(trifluoromethyl)phenyl)-N-(pyrimidin-4-yl)chroman-7-sulfonamide | US10239869, Example 198 |
Type | Small organic molecule |
Emp. Form. | C25H18F4N4O3S |
Mol. Mass. | 530.494 |
SMILES | Fc1ccc(nc1)-c1cc(ccc1[C@H]1CCOc2cc(ccc12)S(=O)(=O)Nc1ccncn1)C(F)(F)F |
Structure |
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