Protein Information

General Information of the Protein

Protein ID	PT01000
Protein Name	Sodium channel protein type 9 subunit alpha
Secondarily Protein Name	Neuroendocrine sodium channel Peripheral sodium channel 1 Sodium channel protein type IX subunit alpha Voltage-gated sodium channel subunit alpha Nav1.7
Gene Name	SCN9A
Secondarily Gene Name	NENA
Sequence	MAMLPPPGPQSFVHFTKQSLALIEQRIAERKSKEPKEEKKDDDEEAPKPSSDLEAGKQLPFIYGDIPPGMVSEPLEDLDPYYADKKTFIVLNKGKTIFRFNATPALYMLSPFSPLRRISIKILVHSLFSMLIMCTILTNCIFMTMNNPPDWTKNVEYTFTGIYTFESLVKILARGFCVGEFTFLRDPWNWLDFVVIVFAYLTEFVNLGNVSALRTFRVLRALKTISVIPGLKTIVGALIQSVKKLSDVMILTVFCLSVFALIGLQLFMGNLKHKCFRNSLENNETLESIMNTLESEEDFRKYFYYLEGSKDALLCGFSTDSGQCPEGYTCVKIGRNPDYGYTSFDTFSWAFLALFRLMTQDYWENLYQQTLRAAGKTYMIFFVVVIFLGSFYLINLILAVVAMAYEEQNQANIEEAKQKELEFQQMLDRLKKEQEEAEAIAAAAAEYTSIRRSRIMGLSESSSETSKLSSKSAKERRNRRKKKNQKKLSSGEEKGDAEKLSKSESEDSIRRKSFHLGVEGHRRAHEKRLSTPNQSPLSIRGSLFSARRSSRTSLFSFKGRGRDIGSETEFADDEHSIFGDNESRRGSLFVPHRPQERRSSNISQASRSPPMLPVNGKMHSAVDCNGVVSLVDGRSALMLPNGQLLPEVIIDKATSDDSGTTNQIHKKRRCSSYLLSEDMLNDPNLRQRAMSRASILTNTVEELEESRQKCPPWWYRFAHKFLIWNCSPYWIKFKKCIYFIVMDPFVDLAITICIVLNTLFMAMEHHPMTEEFKNVLAIGNLVFTGIFAAEMVLKLIAMDPYEYFQVGWNIFDSLIVTLSLVELFLADVEGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQLFGKSYKECVCKINDDCTLPRWHMNDFFHSFLIVFRVLCGEWIETMWDCMEVAGQAMCLIVYMMVMVIGNLVVLNLFLALLLSSFSSDNLTAIEEDPDANNLQIAVTRIKKGINYVKQTLREFILKAFSKKPKISREIRQAEDLNTKKENYISNHTLAEMSKGHNFLKEKDKISGFGSSVDKHLMEDSDGQSFIHNPSLTVTVPIAPGESDLENMNAEELSSDSDSEYSKVRLNRSSSSECSTVDNPLPGEGEEAEAEPMNSDEPEACFTDGCVWRFSCCQVNIESGKGKIWWNIRKTCYKIVEHSWFESFIVLMILLSSGALAFEDIYIERKKTIKIILEYADKIFTYIFILEMLLKWIAYGYKTYFTNAWCWLDFLIVDVSLVTLVANTLGYSDLGPIKSLRTLRALRPLRALSRFEGMRVVVNALIGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYECINTTDGSRFPASQVPNRSECFALMNVSQNVRWKNLKVNFDNVGLGYLSLLQVATFKGWTIIMYAAVDSVNVDKQPKYEYSLYMYIYFVVFIIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPGNKIQGCIFDLVTNQAFDISIMVLICLNMVTMMVEKEGQSQHMTEVLYWINVVFIILFTGECVLKLISLRHYYFTVGWNIFDFVVVIISIVGMFLADLIETYFVSPTLFRVIRLARIGRILRLVKGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYAIFGMSNFAYVKKEDGINDMFNFETFGNSMICLFQITTSAGWDGLLAPILNSKPPDCDPKKVHPGSSVEGDCGNPSVGIFYFVSYIIISFLVVVNMYIAVILENFSVATEESTEPLSEDDFEMFYEVWEKFDPDATQFIEFSKLSDFAAALDPPLLIAKPNKVQLIAMDLPMVSGDRIHCLDILFAFTKRVLGESGEMDSLRSQMEERFMSANPSKVSYEPITTTLKRKQEDVSATVIQRAYRRYRLRQNVKNISSIYIKDGDRDDDLLNKKDMAFDNVNENSSPEKTDATSSTTSPPSYDSVTKPDKEKYEQDRTEKEDKGKDSKESKK Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Ion channel > Voltage-gated ion channel > Voltage-gated sodium channel
Function	Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:7720699, PubMed:17167479, PubMed:25240195, PubMed:26680203, PubMed:15385606, PubMed:16988069, PubMed:17145499, PubMed:19369487, PubMed:24311784). It is a tetrodotoxin-sensitive Na(+) channel isoform (PubMed:7720699). Plays a role in pain mechanisms, especially in the development of inflammatory pain (PubMed:17167479, PubMed:17145499, PubMed:19369487, PubMed:24311784). Show/Hide
Uniprot ID	Primary ID: Q15858 Secondarily ID: A1BUH5 Q6B4R9 Q6B4S0 Q6B4S1 Q70HX1 Q70HX2 Q8WTU1 Q8WWN4 Show/Hide
Ensembl ID	ENSG00000169432
HGNC ID	HGNC:10597
Subcellular Location	Cell membrane Cell projection Neuron projection

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000011 , CHO

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0510908 Compound Info	6-[5-[4-(trifluoromethyl)phenyl]-3,4-dihydro-2H-1,5-benzoxazepin-8-yl]pyridine-2-carboxamide Show/Hide	C22H18F3N3O2	1
1	IC50 = 340 nM Bioactivity Info	TI LI LO TS
CP0504533 Compound Info	6-[1-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1-benzazepin-7-yl]pyridine-2-carboxamide Show/Hide	C23H20F3N3O	1
1	IC50 = 360 nM Bioactivity Info	TI LI LO TS
CP0286809 Compound Info	(1S)-1-[6-[5-methyl-3-(trifluoromethyl)-6H-benzo[b][1,4]benzoxazepin-8-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C22H19F3N2O3	1
1	IC50 = 370 nM Bioactivity Info	TI LI LO TS
CP0271294 Compound Info	6-[4-acetyl-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridine-2-carboxamide Show/Hide	C24H21F3N4O2	1
1	IC50 = 380 nM Bioactivity Info	TI LI LO TS
CP0547742 Compound Info	6-[1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-4,1-benzoxazepin-7-yl]pyridine-2-carboxamide Show/Hide	C22H18F3N3O2	1
1	IC50 = 400 nM Bioactivity Info	TI LI LO TS
CP0504535 Compound Info	(1S)-1-[6-[4-methylsulfonyl-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C24H24F3N3O4S	1
1	IC50 = 470 nM Bioactivity Info	TI LI LO TS
CP0488270 Compound Info	2-[7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]acetonitrile Show/Hide	C25H23F3N4O2	1
1	IC50 = 580 nM Bioactivity Info	TI LI LO TS
CP0259741 Compound Info	6-[4-methyl-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridine-2-carboxamide Show/Hide	C23H21F3N4O	1
1	IC50 = 610 nM Bioactivity Info	TI LI LO TS
CP0066012 Compound Info	2-[7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]-N-methylacetamide Show/Hide	C26H27F3N4O3	1
1	IC50 = 640 nM Bioactivity Info	TI LI LO TS
CP0066011 Compound Info	1-[7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]ethanone Show/Hide	C25H24F3N3O3	1
1	IC50 = 660 nM Bioactivity Info	TI LI LO TS
CP0388927 Compound Info	(1S)-1-[6-[4-(1H-imidazol-2-ylmethyl)-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C27H26F3N5O2	1
1	IC50 = 670 nM Bioactivity Info	TI LI LO TS
CP0325805 Compound Info	US9174999, Table 1, Compound 1 Show/Hide	C10H17N7O4	1
1	IC50 = 702 nM Bioactivity Info	TI LI LO TS
CP0560835 Compound Info	6-(3-chloro-11-methyl-5,6-dihydrobenzo[b][1]benzazepin-8-yl)pyridine-2-carboxamide Show/Hide	C21H18ClN3O	1
1	IC50 = 840 nM Bioactivity Info	TI LI LO TS
CP0504532 Compound Info	6-[1-[4-(trifluoromethyl)phenyl]-3,4-dihydro-2H-quinolin-6-yl]pyridine-2-carboxamide Show/Hide	C22H18F3N3O	1
1	IC50 = 910 nM Bioactivity Info	TI LI LO TS
CP0066014 Compound Info	7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepine-4-carboxamide Show/Hide	C24H23F3N4O3	1
1	IC50 = 970 nM Bioactivity Info	TI LI LO TS
CP0420369 Compound Info	(1S)-1-[6-[5-methyl-8-(trifluoromethyl)-6H-benzo[b][1,4]benzoxazepin-3-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C22H19F3N2O3	1
1	IC50 = 1030 nM Bioactivity Info	TI LI LO TS
CP0152366 Compound Info	2-[7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]acetamide Show/Hide	C25H25F3N4O3	1
1	IC50 = 1050 nM Bioactivity Info	TI LI LO TS
CP0283937 Compound Info	(2R,3S)-2,3-dihydroxy-3-[6-[5-methyl-3-(trifluoromethyl)-6H-benzo[b][1,4]benzoxazepin-8-yl]pyridin-2-yl]propanamide Show/Hide	C23H20F3N3O4	1
1	IC50 = 1050 nM Bioactivity Info	TI LI LO TS
CP0283936 Compound Info	(1S)-1-[6-[11-methyl-3-(trifluoromethyl)-5,6-dihydrobenzo[b][1]benzazepin-8-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C23H21F3N2O2	1
1	IC50 = 1080 nM Bioactivity Info	TI LI LO TS
CP0066013 Compound Info	(1S)-1-[6-[4-(cyclopropylmethyl)-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C27H28F3N3O2	1
1	IC50 = 1320 nM Bioactivity Info	TI LI LO TS
CP0566575 Compound Info	2-[8-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-3-(trifluoromethyl)-6H-benzo[b][1,4]benzoxazepin-5-yl]acetamide Show/Hide	C23H20F3N3O4	1
1	IC50 = 1800 nM Bioactivity Info	TI LI LO TS
CP0504534 Compound Info	6-[1-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,4-benzodiazepin-7-yl]pyridine-2-carboxamide Show/Hide	C22H19F3N4O	1
1	IC50 = 1920 nM Bioactivity Info	TI LI LO TS
CP0294578 Compound Info	6-(3-chloro-6,11-dihydro-5H-benzo[b][1]benzazepin-8-yl)pyridine-2-carboxamide Show/Hide	C20H16ClN3O	1
1	IC50 = 1960 nM Bioactivity Info	TI LI LO TS
CP0386203 Compound Info	(1S)-1-[6-[3-(trifluoromethyl)-5,6-dihydrobenzo[b][1,4]benzoxazepin-8-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C21H17F3N2O3	1
1	IC50 = 2570 nM Bioactivity Info	TI LI LO TS
CP0369072 Compound Info	6-(11-acetyl-3-chloro-5,6-dihydrobenzo[b][1]benzazepin-8-yl)pyridine-2-carboxamide Show/Hide	C22H18ClN3O2	1
1	IC50 = 7620 nM Bioactivity Info	TI LI LO TS
CP0541000 Compound Info	6-(3-chloro-11-ethyl-5,6-dihydrobenzo[b][1]benzazepin-8-yl)pyridine-2-carboxamide Show/Hide	C22H20ClN3O	1
1	IC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0510907 Compound Info	6-[1-[4-(trifluoromethyl)phenyl]-2,3-dihydroindol-5-yl]pyridine-2-carboxamide Show/Hide	C21H16F3N3O	1
1	IC50 > 20000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000131 , HEK293-F

Cell Line Info

Cell Line ID: CL000004 , SH-SY5Y

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0116756 Compound Info	US8952169, 64 Show/Hide	C24H31FN2O4S	1
1	IC50 = 0.4 nM
CP0154464 Compound Info	(4S)-6-fluoro-4-[(2R,4S)-2-(4-fluorophenyl)-4-(trifluoromethyl)piperidin-1-yl]-N-pyrimidin-4-yl-3,4-dihydro-2H-chromene-7-sulfonamide Show/Hide	C25H23F5N4O3S	1
1	IC50 = 0.5 nM
CP0204850 Compound Info	4-[2-(3-amino-1,2-benzoxazol-5-yl)-4-chlorophenoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C21H12ClF2N5O4S2	1
1	IC50 = 0.6 nM
CP0185874 Compound Info	4-[2-[3-(azetidin-1-ylmethyl)phenyl]-4-chlorophenoxy]-3-cyano-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C25H20ClN5O3S2	1
1	IC50 = 1.6 nM
CP0235884 Compound Info	3-cyano-4-[2-(5-methyl-1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy]-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C20H13F3N6O3S2	1
1	IC50 = 2.4 nM
CP0008828 Compound Info	4-[4-chloro-2-[2-(1-methylazetidin-3-yl)pyrazol-3-yl]phenoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C21H17ClF2N6O3S2	1
1	IC50 = 2.6 nM
CP0117181 Compound Info	US9260446, (I-S) Show/Hide	C22H14F3NO5	1
1	IC50 = 3 nM
CP0051988 Compound Info	4-[2-(5-amino-1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy]-5-chloro-2-fluoro-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide Show/Hide	C18H11ClF4N6O3S2	1
1	IC50 = 3.1 nM
CP0052824 Compound Info	4-[[(3S,4R)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C20H19ClF2N4O3S2	1
1	IC50 = 3.3 nM
CP0130944 Compound Info	4-[4-chloro-2-(1H-pyrazol-4-yl)phenoxy]-3-cyano-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C18H11ClN6O3S2	1
1	IC50 = 3.7 nM
CP0303021 Compound Info	US8952169, 6 Show/Hide	C19H23ClFNO4S	1
1	IC50 = 3.8 nM
CP0153084 Compound Info	4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C18H12ClF2N5O3S2	1
1	IC50 = 4.8 nM
CP0119710 Compound Info	4-[2-(5-amino-1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide Show/Hide	C19H12ClF4N5O3S2	1
1	IC50 = 5 nM
CP0340775 Compound Info	US9260446, (I) Show/Hide	C22H14F3NO5	1
1	IC50 = 7 nM
CP0130941 Compound Info	4-[4-chloro-2-[2-(1-methylazetidin-3-yl)pyrazol-3-yl]phenoxy]-2,5-difluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide Show/Hide	C22H18ClF2N5O3S2	1
1	IC50 = 7.3 nM
CP0345299 Compound Info	4-[2-[3-(azetidin-1-ylmethyl)phenyl]-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide Show/Hide	C24H19Cl2FN4O3S2	1
1	IC50 = 7.8 nM
CP0345297 Compound Info	4-[2-[3-(aminomethyl)phenyl]-4-chlorophenoxy]-3-cyano-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C22H16ClN5O3S2	1
1	IC50 = 8.4 nM
CP0319124 Compound Info	4-[2-(2-aminopyridin-4-yl)-4-chlorophenoxy]-3-cyano-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C20H13ClN6O3S2	1
1	IC50 = 8.5 nM
CP0010999 Compound Info	4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide Show/Hide	C18H12Cl2FN5O3S2	1
1	IC50 = 8.6 nM
CP0247326 Compound Info	4-[4-chloro-2-(1H-pyrazol-4-yl)phenoxy]-3-cyano-N-(1,3-thiazol-2-yl)benzenesulfonamide Show/Hide	C19H12ClN5O3S2	1
1	IC50 = 8.999 nM
CP0153087 Compound Info	4-[4-chloro-2-[2-(1-ethylazetidin-3-yl)pyrazol-3-yl]phenoxy]-2,5-difluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide Show/Hide	C23H20ClF2N5O3S2	1
1	IC50 = 9.701 nM
CP0323607 Compound Info	3-cyano-4-[2-pyridazin-4-yl-4-(trifluoromethyl)phenoxy]-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C20H11F3N6O3S2	1
1	IC50 = 9.799 nM
CP0133600 Compound Info	US9212182, 469 Show/Hide	C26H19ClFN3O5S	1
1	IC50 = 10 nM
CP0247320 Compound Info	4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-3-cyano-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C18H12ClN7O3S2	1
1	IC50 = 11 nM
CP0254953 Compound Info	5-chloro-2-fluoro-4-[2-pyridazin-4-yl-4-(trifluoromethyl)phenoxy]-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide Show/Hide	C19H10ClF4N5O3S2	1
1	IC50 = 13 nM
CP0345285 Compound Info	3-cyano-4-[2-(1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy]-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C19H11F3N6O3S2	1
1	IC50 = 17 nM
CP0247315 Compound Info	4-[4-chloro-2-[2-(1-ethylazetidin-3-yl)pyrazol-3-yl]phenoxy]-3-cyano-N-(1,3-thiazol-4-yl)benzenesulfonamide Show/Hide	C24H21ClN6O3S2	1
1	IC50 = 19 nM
CP0119705 Compound Info	5-chloro-4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-2-fluoro-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide Show/Hide	C18H12Cl2FN5O3S2	1
1	IC50 = 20 nM
CP0168191 Compound Info	4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-3-cyano-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C19H13ClN6O3S2	1
1	IC50 = 20 nM
CP0123958 Compound Info	10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diazatetracyclo[7.3.1.13,11.03,8]tetradecane-1,2,7,10,14-pentaol Show/Hide	C11H17N3O8	2
1	IC50 = 25 nM
2	IC50 < 30 nM
CP0676320 Compound Info	(3S)-3-amino-3-{[(1R,4S,10S,13S,16S,19S,22S,25R,30R,33S,36S,39S,42S,45S,48S,51R,54S,57S,60S,63S,69S,72R,77R,80S,86S,89S,92S,95S)-30-{[(1S)-5-amino-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}-2-methylpropyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]carbamoyl}pentyl]carbamoyl}-22,36,95-tris(4-aminobutyl)-4-[(2S)-butan-2-yl]-45,69,92-tris(3-carbamimidamidopropyl)-16,60-bis(carbamoylmethyl)-13,19-bis(carboxymethyl)-42-[(1R)-1-hydroxyethyl]-48-(hydroxymethyl)-39-(1H-imidazol-5-ylmethyl)-33-(1H-indol-3-ylmethyl)-86-methyl-57,80-bis(2-methylpropyl)-89-[2-(methylsulfanyl)ethyl]-2,5,11,14,17,20,23,32,35,38,41,44,47,50,53,56,59,62,68,71,78,81,84,87,90,93,96,103-octacosaoxo-54-(propan-2-yl)-27,28,74,75,99,100-hexathia-3,6,12,15,18,21,24,31,34,37,40,43,46,49,52,55,58,61,67,70,79,82,85,88,91,94,97,102-octacosaazapentacyclo[49.46.4.2^{25,72}.0^{6,10}.0^{63,67}]103n-77-yl]carbamoyl}propanoic acid Show/Hide	C170H267N53O45S7	1
1	IC50 = 27 nM
CP0095952 Compound Info	3-cyano-4-[2-(2-methylpyrazol-3-yl)phenoxy]-N-(1,3-thiazol-2-yl)benzenesulfonamide Show/Hide	C20H15N5O3S2	2
1	IC50 = 28 nM
2	IC50 = 70 nM
CP0221557 Compound Info	N-[(2R)-1-[[(3R)-7-chloro-2-oxo-1-propan-2-yl-4,5-dihydro-3H-1-benzazepin-3-yl]amino]-3-(2-fluorophenyl)-1-oxopropan-2-yl]-4-fluoro-2-(trifluoromethyl)benzamide Show/Hide	C30H27ClF5N3O3	1
1	IC50 = 30 nM
CP0165599 Compound Info	5-chloro-4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-2-fluoro-N-pyrimidin-4-ylbenzenesulfonamide Show/Hide	C20H14Cl2FN5O3S	1
1	IC50 = 30 nM
CP0235883 Compound Info	4-[4-chloro-2-(1H-pyrazol-5-yl)phenoxy]-3-cyano-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C18H11ClN6O3S2	1
1	IC50 = 30 nM
CP0119708 Compound Info	5-chloro-2-fluoro-4-[2-pyridazin-4-yl-4-(trifluoromethyl)phenoxy]-N-(1,3-thiazol-4-yl)benzenesulfonamide Show/Hide	C20H11ClF4N4O3S2	1
1	IC50 = 32 nM
CP0185901 Compound Info	5-chloro-4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide Show/Hide	C19H13Cl2FN4O3S2	1
1	IC50 = 34 nM
CP0112138 Compound Info	tert-butyl N-[(2R)-1-oxo-1-[[(3R)-2-oxo-1-propan-2-yl-4,5-dihydro-3H-1-benzazepin-3-yl]amino]-3-[2-(trifluoromethoxy)phenyl]propan-2-yl]carbamate Show/Hide	C28H34F3N3O5	2
1	IC50 = 35 nM
2	Ki = 40 nM
CP0319111 Compound Info	4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-3-fluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C18H13ClFN5O3S2	1
1	IC50 = 36 nM
CP0169863 Compound Info	5-chloro-4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-2-fluoro-N-(5-fluoropyridin-2-yl)benzenesulfonamide Show/Hide	C21H14Cl2F2N4O3S	1
1	IC50 = 57 nM
CP0177241 Compound Info	tert-butyl N-[(2R)-1-[[(3R)-7-chloro-2-oxo-1-propan-2-yl-4,5-dihydro-3H-1-benzazepin-3-yl]amino]-1-oxo-3-[2-(trifluoromethoxy)phenyl]propan-2-yl]carbamate Show/Hide	C28H33ClF3N3O5	1
1	IC50 = 108 nM
CP0257284 Compound Info	(2S)-N-[6-[4-(4-fluorophenoxy)phenyl]pyridin-2-yl]-3-(1H-imidazol-5-yl)-2-(methanesulfonamido)propanamide Show/Hide	C24H22FN5O4S	1
1	IC50 = 140 nM
CP0051985 Compound Info	4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-3-cyano-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide Show/Hide	C19H13ClN6O3S2	1
1	IC50 = 239.99 nM
CP0186940 Compound Info	3-cyano-4-[2-pyrimidin-4-yl-4-(trifluoromethyl)phenoxy]-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C20H11F3N6O3S2	1
1	IC50 = 319.96 nM
CP0193560 Compound Info	3-cyano-4-[2-pyridazin-3-yl-4-(trifluoromethyl)phenoxy]-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Show/Hide	C20H11F3N6O3S2	1
1	IC50 = 319.96 nM
CP0197731 Compound Info	4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-3-cyano-N-(1,3-thiazol-4-yl)benzenesulfonamide Show/Hide	C20H14ClN5O3S2	1
1	IC50 = 470 nM
CP0552334 Compound Info	1-[5-fluoro-4-(3-fluorophenyl)-2-methoxyphenyl]-N-(1,2-oxazol-3-yl)-2-oxoquinazoline-6-sulfonamide Show/Hide	C24H16F2N4O5S	1
1	IC50 = 1750 nM
CP0312051 Compound Info	US9260446, (I-R) Show/Hide	C22H14F3NO5	1
1	IC50 = 4200 nM
CP0069734 Compound Info	2,2-diphenyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]acetamide Show/Hide	C23H19N3O3S2	1
1	IC50 = 5200 nM
CP0051021 Compound Info	5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide Show/Hide	C19H16ClNO4	1
1	IC50 = 6740 nM
CP0442481 Compound Info	US9163008, 64 Show/Hide	C20H17ClFN5O3	1
1	Ki = 16 nM
CP0479218 Compound Info	US9163008, 14 Show/Hide	C21H18F3N5O3	1
1	Ki = 24 nM
CP0566251 Compound Info	US9163008, 42 Show/Hide	C20H19FN4O3	1
1	Ki = 24 nM
CP0273964 Compound Info	US9163008, 7 Show/Hide	C21H18FN5O3	1
1	Ki = 53 nM
CP0342528 Compound Info	US9163008, 56 Show/Hide	C20H17FN4O4	1
1	Ki = 53 nM
CP0561026 Compound Info	US9163008, 98 Show/Hide	C21H17F3N4O4	1
1	Ki = 54 nM
CP0342527 Compound Info	US9163008, 1 Show/Hide	C20H18FN5O3	1
1	Ki = 57 nM
CP0523896 Compound Info	US9163008, 38 Show/Hide	C20H17ClFN5O3	1
1	Ki = 67 nM
CP0142186 Compound Info	US9163008, 5 Show/Hide	C22H20FN5O3	1
1	Ki = 78 nM
CP0174160 Compound Info	US9163008, 99 Show/Hide	C21H17F3N6O3	1
1	Ki = 83 nM
CP0504535 Compound Info	(1S)-1-[6-[4-methylsulfonyl-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C24H24F3N3O4S	1
1	Ki = 230 nM
CP0556901 Compound Info	US9163008, 21 Show/Hide	C20H18FN5O3	1
1	Ki = 230 nM
CP0206388 Compound Info	(1R,2R)-N1-methyl-N1-((2'-sulfamoylbiphenyl-4-yl)methyl)-N2-(4-(trifluoromethoxy)benzyl)cyclopentane-1,2-dicarboxamide Show/Hide	C29H30F3N3O5S	2
1	Ki = 250 nM
2	Ki = 290 nM
CP0273963 Compound Info	US9163008, 6 Show/Hide	C24H22FN7O3	1
1	Ki = 250 nM
CP0518879 Compound Info	US9163008, 53 Show/Hide	C21H21FN4O6S	1
1	Ki = 270 nM
CP0152366 Compound Info	2-[7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]acetamide Show/Hide	C25H25F3N4O3	1
1	Ki = 300 nM
CP0271294 Compound Info	6-[4-acetyl-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridine-2-carboxamide Show/Hide	C24H21F3N4O2	1
1	Ki = 300 nM
CP0313456 Compound Info	US9163008, 15 Show/Hide	C23H21FN4O4	1
1	Ki = 350 nM
CP0259741 Compound Info	6-[4-methyl-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridine-2-carboxamide Show/Hide	C23H21F3N4O	1
1	Ki = 400 nM
CP0142187 Compound Info	US9163008, 13 Show/Hide	C20H17F3N6O3	1
1	Ki = 420 nM
CP0066012 Compound Info	2-[7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]-N-methylacetamide Show/Hide	C26H27F3N4O3	1
1	Ki = 440 nM
CP0286809 Compound Info	(1S)-1-[6-[5-methyl-3-(trifluoromethyl)-6H-benzo[b][1,4]benzoxazepin-8-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C22H19F3N2O3	1
1	Ki = 440 nM
CP0066014 Compound Info	7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepine-4-carboxamide Show/Hide	C24H23F3N4O3	1
1	Ki = 450 nM
CP0066013 Compound Info	(1S)-1-[6-[4-(cyclopropylmethyl)-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-7-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C27H28F3N3O2	1
1	Ki = 550 nM
CP0420369 Compound Info	(1S)-1-[6-[5-methyl-8-(trifluoromethyl)-6H-benzo[b][1,4]benzoxazepin-3-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C22H19F3N2O3	1
1	Ki = 560 nM
CP0347248 Compound Info	US9163008, 2 Show/Hide	C19H16FN5O3	1
1	Ki = 590 nM
CP0273965 Compound Info	US9163008, 63 Show/Hide	C19H17ClN6O3	1
1	Ki = 600 nM
CP0066011 Compound Info	1-[7-[6-[(1S)-1,2-dihydroxyethyl]pyridin-2-yl]-1-[4-(trifluoromethyl)phenyl]-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]ethanone Show/Hide	C25H24F3N3O3	1
1	Ki = 630 nM
CP0294578 Compound Info	6-(3-chloro-6,11-dihydro-5H-benzo[b][1]benzazepin-8-yl)pyridine-2-carboxamide Show/Hide	C20H16ClN3O	1
1	Ki = 650 nM
CP0283937 Compound Info	(2R,3S)-2,3-dihydroxy-3-[6-[5-methyl-3-(trifluoromethyl)-6H-benzo[b][1,4]benzoxazepin-8-yl]pyridin-2-yl]propanamide Show/Hide	C23H20F3N3O4	1
1	Ki = 920 nM
CP0283936 Compound Info	(1S)-1-[6-[11-methyl-3-(trifluoromethyl)-5,6-dihydrobenzo[b][1]benzazepin-8-yl]pyridin-2-yl]ethane-1,2-diol Show/Hide	C23H21F3N2O2	1
1	Ki = 1030 nM
CP0369072 Compound Info	6-(11-acetyl-3-chloro-5,6-dihydrobenzo[b][1]benzazepin-8-yl)pyridine-2-carboxamide Show/Hide	C22H18ClN3O2	1
1	Ki = 3030 nM
CP0322043 Compound Info	US9163008, 35 Show/Hide	C20H17FN4O4	1
1	Ki = 20500 nM
CP0071077 Compound Info	5H-dibenzo[b,f]azepine-5-carboxamide Show/Hide	C15H12N2O	1
1	Ki = 32700 nM
CP0319033 Compound Info	US9163008, 40 Show/Hide	C20H16FN3O5	1
1	Ki = 41050 nM

Clinical Information about the Protein

Target 1 ( Voltage-gated sodium channel alpha Nav1.7 (SCN9A) )

Target Type	Clinical trial Target
Disease	5 Target-related Diseases				5
1	Lumbosacral radiculopathy [ICD-11: 8B93.Y]
2	Chronic pain [ICD-11: MG30]
3	Osteoarthritis [ICD-11: FA00-FA05]
4	Pain [ICD-11: MG30-MG3Z]
5	Neurological disorder [ICD-11: 6B60]
Clinical Trial Drug(s)	5 Clinical Trial Drugs				5
1	BIIB074	Drug Info	Phase 2	Lumbosacral radiculopathy
2	PF-05089771	Drug Info	Phase 2	Chronic pain
3	XEN-402	Drug Info	Phase 2	Osteoarthritis
4	GDC0310	Drug Info	Phase 1	Chronic pain
5	PF-05241328	Drug Info	Phase 1	Pain
Discontinued Drug(s)	1 Discontinued Drug				1
1	SIPATRIGINE	Drug Info	Discontinued in Phase 2	Neurological disorder
Investigative Drug(s)	1 Investigative Drug				1
1	XEN-907	Drug Info	Investigative	Pain

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT04404	Sodium channel protein type 9 subunit alpha	Rattus norvegicus, Rat	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han