Target Information
| Target General Information | Top | |||||
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| Target ID |
T12119
(Former ID: TTDS00503)
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| Target Name |
Voltage-gated sodium channel alpha Nav1.7 (SCN9A)
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| Synonyms |
hNE-Na; Voltage-gated sodium channel subunit alpha Nav1.7; Sodium channel proteintype IX subunit alpha; Sodium channel proteintype 9 subunit alpha; Sodium channel protein type IX subunit alpha; Sodium channel protein type 9 subunit alpha; Peripheral sodium channel 1; PN1; Neuroendocrine sodium channel; NENA
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| Gene Name |
SCN9A
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 8 Target-related Diseases | + | ||||
| 1 | Bipolar disorder [ICD-11: 6A60] | |||||
| 2 | Extremities vasodilatation [ICD-11: EG00] | |||||
| 3 | Osteoarthritis [ICD-11: FA00-FA05] | |||||
| 4 | Radiculopathy [ICD-11: 8B93] | |||||
| 5 | Trigeminal nerve disorder [ICD-11: 8B82] | |||||
| 6 | Chronic pain [ICD-11: MG30] | |||||
| 7 | General pain disorder [ICD-11: 8E43] | |||||
| 8 | Pain [ICD-11: MG30-MG3Z] | |||||
| Function |
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. It is a tetrodotoxin-sensitive Na(+) channel isoform. Plays a role in pain mechanisms, especially in the development of inflammatory pain. Mediates the voltage-dependent sodium ion permeability of excitable membranes.
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| BioChemical Class |
Voltage-gated ion channel
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| UniProt ID | ||||||
| Sequence |
MAMLPPPGPQSFVHFTKQSLALIEQRIAERKSKEPKEEKKDDDEEAPKPSSDLEAGKQLP
FIYGDIPPGMVSEPLEDLDPYYADKKTFIVLNKGKTIFRFNATPALYMLSPFSPLRRISI KILVHSLFSMLIMCTILTNCIFMTMNNPPDWTKNVEYTFTGIYTFESLVKILARGFCVGE FTFLRDPWNWLDFVVIVFAYLTEFVNLGNVSALRTFRVLRALKTISVIPGLKTIVGALIQ SVKKLSDVMILTVFCLSVFALIGLQLFMGNLKHKCFRNSLENNETLESIMNTLESEEDFR KYFYYLEGSKDALLCGFSTDSGQCPEGYTCVKIGRNPDYGYTSFDTFSWAFLALFRLMTQ DYWENLYQQTLRAAGKTYMIFFVVVIFLGSFYLINLILAVVAMAYEEQNQANIEEAKQKE LEFQQMLDRLKKEQEEAEAIAAAAAEYTSIRRSRIMGLSESSSETSKLSSKSAKERRNRR KKKNQKKLSSGEEKGDAEKLSKSESEDSIRRKSFHLGVEGHRRAHEKRLSTPNQSPLSIR GSLFSARRSSRTSLFSFKGRGRDIGSETEFADDEHSIFGDNESRRGSLFVPHRPQERRSS NISQASRSPPMLPVNGKMHSAVDCNGVVSLVDGRSALMLPNGQLLPEVIIDKATSDDSGT TNQIHKKRRCSSYLLSEDMLNDPNLRQRAMSRASILTNTVEELEESRQKCPPWWYRFAHK FLIWNCSPYWIKFKKCIYFIVMDPFVDLAITICIVLNTLFMAMEHHPMTEEFKNVLAIGN LVFTGIFAAEMVLKLIAMDPYEYFQVGWNIFDSLIVTLSLVELFLADVEGLSVLRSFRLL RVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQLFGKSYKECVCKIN DDCTLPRWHMNDFFHSFLIVFRVLCGEWIETMWDCMEVAGQAMCLIVYMMVMVIGNLVVL NLFLALLLSSFSSDNLTAIEEDPDANNLQIAVTRIKKGINYVKQTLREFILKAFSKKPKI SREIRQAEDLNTKKENYISNHTLAEMSKGHNFLKEKDKISGFGSSVDKHLMEDSDGQSFI HNPSLTVTVPIAPGESDLENMNAEELSSDSDSEYSKVRLNRSSSSECSTVDNPLPGEGEE AEAEPMNSDEPEACFTDGCVWRFSCCQVNIESGKGKIWWNIRKTCYKIVEHSWFESFIVL MILLSSGALAFEDIYIERKKTIKIILEYADKIFTYIFILEMLLKWIAYGYKTYFTNAWCW LDFLIVDVSLVTLVANTLGYSDLGPIKSLRTLRALRPLRALSRFEGMRVVVNALIGAIPS IMNVLLVCLIFWLIFSIMGVNLFAGKFYECINTTDGSRFPASQVPNRSECFALMNVSQNV RWKNLKVNFDNVGLGYLSLLQVATFKGWTIIMYAAVDSVNVDKQPKYEYSLYMYIYFVVF IIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRP GNKIQGCIFDLVTNQAFDISIMVLICLNMVTMMVEKEGQSQHMTEVLYWINVVFIILFTG ECVLKLISLRHYYFTVGWNIFDFVVVIISIVGMFLADLIETYFVSPTLFRVIRLARIGRI LRLVKGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYAIFGMSNFAYVKKEDGINDMFN FETFGNSMICLFQITTSAGWDGLLAPILNSKPPDCDPKKVHPGSSVEGDCGNPSVGIFYF VSYIIISFLVVVNMYIAVILENFSVATEESTEPLSEDDFEMFYEVWEKFDPDATQFIEFS KLSDFAAALDPPLLIAKPNKVQLIAMDLPMVSGDRIHCLDILFAFTKRVLGESGEMDSLR SQMEERFMSANPSKVSYEPITTTLKRKQEDVSATVIQRAYRRYRLRQNVKNISSIYIKDG DRDDDLLNKKDMAFDNVNENSSPEKTDATSSTTSPPSYDSVTKPDKEKYEQDRTEKEDKG KDSKESKK Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 12 Clinical Trial Drugs | + | ||||
| 1 | BIIB074 | Drug Info | Phase 2 | Lumbosacral radiculopathy | [2] | |
| 2 | PF-05089771 | Drug Info | Phase 2 | Chronic pain | [3] | |
| 3 | XEN-402 | Drug Info | Phase 2 | Osteoarthritis | [4] | |
| 4 | BIIB095 | Drug Info | Phase 1 | Pain | [2] | |
| 5 | CC8464 | Drug Info | Phase 1 | Neuropathic pain | [2] | |
| 6 | DSP-2230 | Drug Info | Phase 1 | Neuropathic pain | [2], [5] | |
| 7 | DSP-3905 | Drug Info | Phase 1 | Neuropathic pain | [2] | |
| 8 | DWJ-208 | Drug Info | Phase 1 | Cancer related pain | [2] | |
| 9 | GDC0310 | Drug Info | Phase 1 | Chronic pain | [5] | |
| 10 | PF-05186462 | Drug Info | Phase 1 | Pain | [6] | |
| 11 | PF-05241328 | Drug Info | Phase 1 | Pain | [6] | |
| 12 | RG7893 | Drug Info | Phase 1 | Pain | [7] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | Corus 1030 | Drug Info | Discontinued in Phase 2 | Asthma | [8] | |
| 2 | SIPATRIGINE | Drug Info | Discontinued in Phase 2 | Neurological disorder | [9] | |
| Mode of Action | [+] 7 Modes of Action | + | ||||
| Inhibitor | [+] 25 Inhibitor drugs | + | ||||
| 1 | BIIB074 | Drug Info | [2], [5] | |||
| 2 | XEN-402 | Drug Info | [1] | |||
| 3 | BIIB095 | Drug Info | [2] | |||
| 4 | CC8464 | Drug Info | [2] | |||
| 5 | DSP-2230 | Drug Info | [2], [5] | |||
| 6 | DSP-3905 | Drug Info | [2] | |||
| 7 | GDC0310 | Drug Info | [5] | |||
| 8 | PF-05186462 | Drug Info | [11] | |||
| 9 | PF-05241328 | Drug Info | [12] | |||
| 10 | RG7893 | Drug Info | [13], [14] | |||
| 11 | Aryl carboxamide derivative 1 | Drug Info | [15] | |||
| 12 | Aryl carboxamide derivative 2 | Drug Info | [15] | |||
| 13 | Aryl carboxamide derivative 4 | Drug Info | [15] | |||
| 14 | Benzene sulfonamide derivative 11 | Drug Info | [15] | |||
| 15 | Benzene sulfonamide derivative 12 | Drug Info | [15] | |||
| 16 | Methylsulfonylbenzamide derivative 2 | Drug Info | [15] | |||
| 17 | Pyrrolo-pyridinone derivative 5 | Drug Info | [15] | |||
| 18 | Pyrrolo-pyridinone derivative 6 | Drug Info | [15] | |||
| 19 | Tarizine derivative 1 | Drug Info | [15] | |||
| 20 | SIPATRIGINE | Drug Info | [18] | |||
| 21 | V-102862 | Drug Info | [19] | |||
| 22 | 4-(2'-(trifluoromethoxy)biphenyl-3-yl)oxazole | Drug Info | [19] | |||
| 23 | 4-(2'-(trifluoromethoxy)biphenyl-3-yl)thiazole | Drug Info | [19] | |||
| 24 | 4-(2'-(trifluoromethyl)biphenyl-3-yl)oxazole | Drug Info | [19] | |||
| 25 | XEN-907 | Drug Info | [20] | |||
| Blocker | [+] 11 Blocker drugs | + | ||||
| 1 | PF-05089771 | Drug Info | [10] | |||
| 2 | Benzene sulfonamide derivative 15 | Drug Info | [15] | |||
| 3 | Benzene sulfonamide derivative 9 | Drug Info | [15] | |||
| 4 | Cyclopropyl-spiro piperidine derivative 1 | Drug Info | [15] | |||
| 5 | Cyclopropyl-spiro piperidine derivative 2 | Drug Info | [15] | |||
| 6 | Cyclopropyl-spiro piperidine derivative 3 | Drug Info | [15] | |||
| 7 | Cyclopropyl-spiro piperidine derivative 4 | Drug Info | [15] | |||
| 8 | Dihydrobenzoxazine and tetrahydroquinoxaline sulfonamide derivative 1 | Drug Info | [15] | |||
| 9 | Enzoxazolinone sulfonamide derivative 1 | Drug Info | [15] | |||
| 10 | Pyrimidine derivative 1 | Drug Info | [15] | |||
| 11 | Pyrrolo-benzo-diazine derivative 1 | Drug Info | [15] | |||
| Antagonist | [+] 1 Antagonist drugs | + | ||||
| 1 | DWJ-208 | Drug Info | [2] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | Corus 1030 | Drug Info | [16], [17] | |||
| Activator | [+] 2 Activator drugs | + | ||||
| 1 | batrachotoxin | Drug Info | [20] | |||
| 2 | veratridine | Drug Info | [20] | |||
| Inhibitor (gating inhibitor) | [+] 1 Inhibitor (gating inhibitor) drugs | + | ||||
| 1 | N-Me-aminopyrimidinone 9 | Drug Info | [21] | |||
| Blocker (channel blocker) | [+] 1 Blocker (channel blocker) drugs | + | ||||
| 1 | pyrrolopyrimidine 48 | Drug Info | [22] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Tetrodotoxin | Ligand Info | |||||
| Structure Description | Cryo-EM structure of human Nav1.7(E406K) in complex with auxiliary beta subunits, ProTx-II and tetrodotoxin (S6IV pi helix conformer) | PDB:7W9M | ||||
| Method | Electron microscopy | Resolution | 3.00 Å | Mutation | Yes | [23] |
| PDB Sequence |
GPQSFVHFTK
17 QSLALIEQRI27 AERKSKEPKP49 SSDLEAGKQL59 PFIYGDIPPG69 MVSEPLEDLD 79 PYYADKKTFI89 VLNKGKTIFR99 FNATPALYML109 SPFSPLRRIS119 IKILVHSLFS 129 MLIMCTILTN139 CIFMTMNNPP149 DWTKNVEYTF159 TGIYTFESLV169 KILARGFCVG 179 EFTFLRDPWN189 WLDFVVIVFA199 YLTEFVNNVS211 ALRTFRVLRA221 LKTISVIPGL 231 KTIVGALIQS241 VKKLSDVMIL251 TVFCLSVFAL261 IGLQLFMGNL271 KHKCFRNSLE 281 NNETLESIMN291 TLESEEDFRK301 YFYYLEGSKD311 ALLCGFSTDS321 GQCPEGYTCV 331 KIGRNPDYGY341 TSFDTFSWAF351 LALFRLMTQD361 YWENLYQQTL371 RAAGKTYMIF 381 FVVVIFLGSF391 YLINLILAVV401 AMAYKEQNQA411 NIEEAKQKEL421 EFQQMLDRLK 431 KEQEPYWIKF733 KKCIYFIVMD743 PFVDLAITIC753 IVLNTLFMAM763 EHHPMTEEFK 773 NVLAIGNLVF783 TGIFAAEMVL793 KLIAMDPYEY803 FQVGWNIFDS813 LIVTLSLVEL 823 FLADVEGLSV833 LRSFRLLRVF843 KLAKSWPTLN853 MLIKIIGNSV863 GALGNLTLVL 873 AIIVFIFAVV883 GMQLFGKSYK893 ECVCKINDDC903 TLPRWHMNDF913 FHSFLIVFRV 923 LCGEWIETMW933 DCMEVAGQAM943 CLIVYMMVMV953 IGNLVVLNLF963 LALLLSSFSS 973 DNLTAIEEDP983 DANNLQIAVT993 RIKKGINYVK1003 QTLREFILKA1013 FGKIWWNIRK 1183 TCYKIVEHSW1193 FESFIVLMIL1203 LSSGALAFED1213 IYIERKKTIK1223 IILEYADKIF 1233 TYIFILEMLL1243 KWIAYGYKTY1253 FTNAWCWLDF1263 LIVDVSLVTL1273 VANTLGYSDL 1283 GPIKSLRTLR1293 ALRPLRALSR1303 FEGMRVVVNA1313 LIGAIPSIMN1323 VLLVCLIFWL 1333 IFSIMGVNLF1343 AGKFYECINT1353 TDGSRFPASQ1363 VPNRSECFAL1373 MNVSQNVRWK 1383 NLKVNFDNVG1393 LGYLSLLQVA1403 TFKGWTIIMY1413 AAVDSVNVDK1423 QPKYEYSLYM 1433 YIYFVVFIIF1443 GSFFTLNLFI1453 GVIIDNFNQQ1463 KKKLGGQDIF1473 MTEEQKKYYN 1483 AMKKLGSKKP1493 QKPIPRPGNK1503 IQGCIFDLVT1513 NQAFDISIMV1523 LICLNMVTMM 1533 VEKEGQSQHM1543 TEVLYWINVV1553 FIILFTGECV1563 LKLISLRHYY1573 FTVGWNIFDF 1583 VVVIISIVGM1593 FLADLIETYF1603 VSPTLFRVIR1613 LARIGRILRL1623 VKGAKGIRTL 1633 LFALMMSLPA1643 LFNIGLLLFL1653 VMFIYAIFGM1663 SNFAYVKKED1673 GINDMFNFET 1683 FGNSMICLFQ1693 ITTSAGWDGL1703 LAPILNSKPP1713 DCDPKKVHPG1723 SSVEGDCGNP 1733 SVGIFYFVSY1743 IIISFLVVVN1753 MYIAVILENF1763 SVATEESTEP1773 LSEDDFEMFY 1783 EVWEKFDPDA1793 TQFIEFSKLS1803 DFAAALDPPL1813 LIAKPNKVQL1823 IAMDLPMVSG 1833 DRIHCLDILF1843 AFTKRVLGES1853 GEMDSLRSQM1863 EERFMSANPS1873 KVSYEPITTT 1883 LKRKQEDV
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Human Nav1.7 mutant class-I | PDB:7XVE | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | Yes | [24] |
| PDB Sequence |
GPQSFVHFTK
17 QSLALIEQRI27 AERKSKEPKP49 SSDLEAGKQL59 PFIYGDIPPG69 MVSEPLEDLD 79 PYYADKKTFI89 VLNKGKTIFR99 FNATPALYML109 SPFSPLRRIS119 IKILVHSLFS 129 MLIMCTILTN139 CIFMTMNNPP149 DWTKNVKYTF159 TGIYTFESLV169 KILARGFCVG 179 EFTFLRDPWN189 WLDFVVIVFA199 YLTEFVNLGN209 VSALRTFRVL219 RALKTISVIP 229 GLKTIVGALI239 QSVKKLSDVM249 ILTVFCLSVF259 ALIGLQLFMG269 NLKHKCFRNS 279 LENNETLESI289 MNTLESEEDF299 RKYFYYLEGS309 KDALLCGFST319 DSGQCPEGYT 329 CVKIGRNPDY339 GYTSFDTFSW349 AFLALFRLMT359 QDYWENLYQQ369 TLRAAGKTYM 379 IFFVVVIFLG389 SFYLINLILA399 VVAMAYEEQN409 QANIEEAKQK419 ELEFQQMLCS 727 PYWIKFKKCI737 YFIVMDPFVD747 LAITICIVLN757 TLFMAMEHHP767 MTEEFKNVLA 777 IRNLVFTGIF787 AAEMVLKLIA797 MDPYEYFQVG807 WNIFDSLIVT817 LSLVELFGLS 832 VLRSFRLLRV842 FKLAKSWPTL852 NMLIKIIGNS862 VGAFGNLMLV872 LFIIVFIFAV 882 VGMQLFGKSY892 KECVCKINDD902 CTLPRWHMND912 FFHSFLIVFR922 VLCGEWIETM 932 WDCMEVAGQA942 MCLIFYMMVF952 FIGNLVVLNL962 FLALLLSSFS972 SDANNLQIAV 992 TRIKKGINYV1002 KQTLREFILK1012 AFGKIWWNIR1182 KTCYKIVEHS1192 WFESFIVLMI 1202 LLSSGALAFE1212 DIYIERKKTI1222 KIILEYADKI1232 FTYIFILEML1242 LKWIAYGYKT 1252 YFTNAWCWLD1262 FLIVDVSLVT1272 LVANTLGYSD1282 LGPIKSLRTL1292 RALRPLRALS 1302 RFEGMRVVVN1312 ALIGAIPSIM1322 NVLLVCLIFW1332 LIFSIMGVNL1342 FAGKFYECIN 1352 TTDGSRFPAS1362 QVPNRSECFA1372 LMNVSQNVRW1382 KNLKVNFDNV1392 GLGYLSLLQV 1402 ATFKGWTIIM1412 YAAVDSVNVD1422 KQPKYEYSLY1432 MYIYFIFFII1442 FGSFFTLNLF 1452 ICVIIDNFNQ1462 QKKKLGGQDI1472 FMTEEQKKYY1482 NAMKKLGSKK1492 PQKPIPRPGN 1502 KIQGCIFDLV1512 TNQAFDISIM1522 VLICLNMVTM1532 MVEKEGQSQH1542 MTEVLYWINV 1552 VFIILFTGEC1562 VLKLISLRHY1572 YFTVGWNIFD1582 FVVVIISIVG1592 MFLADLIETY 1602 FVSPTLFRVI1612 RLARIGRILR1622 LVKGAKGIRT1632 LLFALMMSLP1642 ALFNIGLLLF 1652 LVMFIYAIFG1662 MSNFAYVKKE1672 DGINDMFNFE1682 TFGNSMICLF1692 QITTSAGWDG 1702 LLAPILNSKP1712 PDCDPKKVHP1722 GSSVEGDCGN1732 PSVGIFYFVS1742 YIIISFLVVV 1752 NMYIAVILEN1762 FSVATE
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ILE228
3.871
PRO229
3.991
VAL833
4.037
PHE837
4.057
VAL863
4.228
GLY864
3.761
GLY867
3.422
ASN868
3.461
MET870
3.826
LEU871
3.901
PHE874
2.515
TYR1250
3.690
LYS1251
3.841
PHE1254
3.525
THR1255
3.430
ASN1256
4.180
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Pathway Affiliation
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| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
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| Sodium/hydrogen exchanger 11 (SLC9C2) | 26.515 (35/132) | 3.73E-04 |
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Taste transduction | hsa04742 | Affiliated Target |
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| Class: Organismal Systems => Sensory system | Pathway Hierarchy | ||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Drug Resistance Mutation (DRM) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Interaction between L1 and Ankyrins | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Treatment of Na(v)1.7-mediated pain in inherited erythromelalgia using a novel sodium channel blocker. Pain. 2012 Jan;153(1):80-5. | |||||
| REF 2 | Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. | |||||
| REF 3 | ClinicalTrials.gov (NCT01529346) Efficacy Of PF-05089771 In Treating Postoperative Dental Pain. U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT02068599) A Study to Evaluate the Safety and Efficacy of Topically Applied TV-45070 Ointment) in Participants With Primary Osteoarthritis (OA) Affecting a Single Knee. U.S. National Institutes of Health. | |||||
| REF 5 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 6 | ClinicalTrials.gov (NCT01165736) To Calculate the Pharmacokinetics (Concentration of Compound in and Rate of Excretion From the Blood) Following a Very Low Dose of Compound Which Will Not Have Any Pharmacological Activity. U.S. National Institutes of Health. | |||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041740) | |||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017745) | |||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003904) | |||||
| REF 10 | Primary erythromelalgia: a review. Orphanet J Rare Dis. 2015 Sep 30;10:127. | |||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026875) | |||||
| REF 12 | Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9. | |||||
| REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041740) | |||||
| REF 14 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 15 | Sodium channel blockers: a patent review (2010 - 2014).Expert Opin Ther Pat. 2015 Mar;25(3):279-90. | |||||
| REF 16 | Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaine. Br J Pharmacol. 2004 Jun;142(3):576-84. | |||||
| REF 17 | Lidocaine reduces the transition to slow inactivation in Na(v)1.7 voltage-gated sodium channels.Br J Pharmacol.2011 Sep;164(2b):719-30. | |||||
| REF 18 | Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones. J Med Chem. 2009 May 14;52(9):2694-707. | |||||
| REF 19 | Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5536-40. | |||||
| REF 20 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 584). | |||||
| REF 21 | Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1055-60. | |||||
| REF 22 | Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists. Bioorg Med Chem Lett. 2012 Mar 1;22(5):2052-62. | |||||
| REF 23 | High-resolution structures of human Na(v)1.7 reveal gating modulation through Alpha-Pi helical transition of S6(IV). Cell Rep. 2022 Apr 26;39(4):110735. | |||||
| REF 24 | Unwinding and spiral sliding of S4 and domain rotation of VSD during the electromechanical coupling in Na(v)1.7. Proc Natl Acad Sci U S A. 2022 Aug 16;119(33):e2209164119. | |||||
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