Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T43739 | Target Info | |||
| Target Name | Voltage-gated sodium channel alpha Nav1.8 (SCN10A) | ||||
| Synonyms | hPN3; Voltage-gated sodium channel subunit alpha Nav1.8; Sodium channel protein type X subunit alpha; Sodium channel protein type 10 subunit alpha; Peripheral nerve sodium channel 3; PN3 | ||||
| Target Type | Successful Target | ||||
| Gene Name | SCN10A | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: A-803467 | Ligand Info | |||||
| Structure Description | Human Nav1.8 with A-803467, class I | PDB:7WE4 | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [1] |
| PDB Sequence |
LIRRTAIKVS
127 VHSWFSLFIT137 VTILVNCVCM147 TRTDLPEKIE157 YVFTVIYTFE167 ALIKILARGF 177 CLNEFTYLRD187 PWNWLDFSVI197 TLAYVGTAID207 LRGISGLRTF217 RVLRALKTVS 227 VIPGLKVIVG237 ALIHSVKKLA247 DVTILTIFCL257 SVFALVGLQL267 FKGNLKNKCV 277 KNDMAYSSHR293 KPDIYINKRG303 TSDPLLCGNG313 SDSGHCPDGY323 ICLKTSDNPD 333 FNYTSFDSFA343 WAFLSLFRLM353 TQDSWERLYQ363 QTLRTSGKIY373 MIFFVLVIFL 383 GSFYLVNLIL393 AVVTMAYEEQ403 NQATWVKLKT656 ILFGLVTDPF666 AELTITLCIV 676 VNTIFMAMEH686 HGMSPTFEAM696 LQIGNIVFTI706 FFTAEMVFKI716 IAFDPYYYFQ 726 KKWNIFDCII736 VTVSLLELGV746 AKKGSLSVLR756 SFRLLRVFKL766 AKSWPTLNTL 776 IKIIGNSVGA786 LGNLTIILAI796 IVFVFALVGK806 QLLGENYRNN816 RKNISAPHED 826 WPRWHMHDFF836 HSFLIVFRIL846 CGEWIENMWA856 CMEVGQKSIC866 LILFLTVMVL 876 GNLVVLNLFI886 ALLLNSFFAD1136 VGWQVRKTCY1146 RIVEHSWFES1156 FIIFMILLSS 1166 GSLAFEDYYL1176 DQKPTVKALL1186 EYTDRVFTFI1196 FVFEMLLKWV1206 AYGFKKYFTN 1216 AWCWLDFLIV1226 NISLISLTAK1236 ILEYSEVAPI1246 KALRTLRALR1256 PLRALSRFEG 1266 MRVVVDALVG1276 AIPSIMNVLL1286 VCLIFWLIFS1296 IMGVNLFAGK1306 FWRCINYTDG 1316 EFSLVPLSIV1326 NNKSDCKIQN1336 STGSFFWVNV1346 KVNFDNVAMG1356 YLALLQVATF 1366 KGWMDIMYAA1376 VDSREVNMQP1386 KWEDNVYMYL1396 YFVIFIIFGG1406 FFTLNLFVGV 1416 IIDNFNQQKK1426 KLGGQDIFMT1436 EEQKKYYNAM1446 KKLGSKKPQK1456 PIPRPLNKFQ 1466 GFVFDIVTRQ1476 AFDITIMVLI1486 CLNMITMMVE1496 TDDQSEEKTK1506 ILGKINQFFV 1516 AVFTGECVMK1526 MFALRQYYFT1536 NGWNVFDFIV1546 VVLSIASLIF1556 SAILKSLQSY 1566 FSPTLFRVIR1576 LARIGRILRL1586 IRAAKGIRTL1596 LFALMMSLPA1606 LFNIGLLLFL 1616 VMFIYSIFGM1626 SSFPHVRWEA1636 GIDDMFNFQT1646 FANSMLCLFQ1656 ITTSAGWDGL 1666 LSPILNTGPP1676 YCDPNLPNSN1686 GTRGDCGSPA1696 VGIIFFTTYI1706 IISFLIMVNM 1716 YIAVILENFN1726 VA
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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 Nav1.8 with A-803467, class I | PDB:7WE4 | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [1] |
| PDB Sequence |
LIRRTAIKVS
127 VHSWFSLFIT137 VTILVNCVCM147 TRTDLPEKIE157 YVFTVIYTFE167 ALIKILARGF 177 CLNEFTYLRD187 PWNWLDFSVI197 TLAYVGTAID207 LRGISGLRTF217 RVLRALKTVS 227 VIPGLKVIVG237 ALIHSVKKLA247 DVTILTIFCL257 SVFALVGLQL267 FKGNLKNKCV 277 KNDMAYSSHR293 KPDIYINKRG303 TSDPLLCGNG313 SDSGHCPDGY323 ICLKTSDNPD 333 FNYTSFDSFA343 WAFLSLFRLM353 TQDSWERLYQ363 QTLRTSGKIY373 MIFFVLVIFL 383 GSFYLVNLIL393 AVVTMAYEEQ403 NQATWVKLKT656 ILFGLVTDPF666 AELTITLCIV 676 VNTIFMAMEH686 HGMSPTFEAM696 LQIGNIVFTI706 FFTAEMVFKI716 IAFDPYYYFQ 726 KKWNIFDCII736 VTVSLLELGV746 AKKGSLSVLR756 SFRLLRVFKL766 AKSWPTLNTL 776 IKIIGNSVGA786 LGNLTIILAI796 IVFVFALVGK806 QLLGENYRNN816 RKNISAPHED 826 WPRWHMHDFF836 HSFLIVFRIL846 CGEWIENMWA856 CMEVGQKSIC866 LILFLTVMVL 876 GNLVVLNLFI886 ALLLNSFFAD1136 VGWQVRKTCY1146 RIVEHSWFES1156 FIIFMILLSS 1166 GSLAFEDYYL1176 DQKPTVKALL1186 EYTDRVFTFI1196 FVFEMLLKWV1206 AYGFKKYFTN 1216 AWCWLDFLIV1226 NISLISLTAK1236 ILEYSEVAPI1246 KALRTLRALR1256 PLRALSRFEG 1266 MRVVVDALVG1276 AIPSIMNVLL1286 VCLIFWLIFS1296 IMGVNLFAGK1306 FWRCINYTDG 1316 EFSLVPLSIV1326 NNKSDCKIQN1336 STGSFFWVNV1346 KVNFDNVAMG1356 YLALLQVATF 1366 KGWMDIMYAA1376 VDSREVNMQP1386 KWEDNVYMYL1396 YFVIFIIFGG1406 FFTLNLFVGV 1416 IIDNFNQQKK1426 KLGGQDIFMT1436 EEQKKYYNAM1446 KKLGSKKPQK1456 PIPRPLNKFQ 1466 GFVFDIVTRQ1476 AFDITIMVLI1486 CLNMITMMVE1496 TDDQSEEKTK1506 ILGKINQFFV 1516 AVFTGECVMK1526 MFALRQYYFT1536 NGWNVFDFIV1546 VVLSIASLIF1556 SAILKSLQSY 1566 FSPTLFRVIR1576 LARIGRILRL1586 IRAAKGIRTL1596 LFALMMSLPA1606 LFNIGLLLFL 1616 VMFIYSIFGM1626 SSFPHVRWEA1636 GIDDMFNFQT1646 FANSMLCLFQ1656 ITTSAGWDGL 1666 LSPILNTGPP1676 YCDPNLPNSN1686 GTRGDCGSPA1696 VGIIFFTTYI1706 IISFLIMVNM 1716 YIAVILENFN1726 VA
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SER341
3.722
PHE342
3.978
ALA343
4.152
ASN390
4.613
LEU393
3.340
THR397
3.590
GLU401
3.224
VAL676
4.483
THR679
3.671
ILE680
4.320
VAL763
4.569
LEU766
3.435
SER769
3.583
TRP770
3.436
PRO771
4.165
PHE885
4.150
ILE886
3.760
LEU889
3.713
LEU890
4.837
PHE1214
4.086
THR1215
3.645
ALA1217
3.650
TRP1220
3.541
LEU1224
4.496
LEU1286
4.586
ILE1290
3.419
LEU1293
4.284
VAL1414
3.489
ILE1418
3.182
ASN1422
4.675
ILE1491
4.213
MET1494
3.696
VAL1495
3.479
THR1497
4.099
LYS1504
4.111
PHE1710
4.066
MET1713
2.666
VAL1714
3.266
TYR1717
3.069
ILE1718
3.596
ILE1721
2.629
LEU1722
4.900
PHE1725
3.736
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Lpc-Ether | Ligand Info | |||||
| Structure Description | Human Nav1.8 with A-803467, class I | PDB:7WE4 | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [1] |
| PDB Sequence |
LIRRTAIKVS
127 VHSWFSLFIT137 VTILVNCVCM147 TRTDLPEKIE157 YVFTVIYTFE167 ALIKILARGF 177 CLNEFTYLRD187 PWNWLDFSVI197 TLAYVGTAID207 LRGISGLRTF217 RVLRALKTVS 227 VIPGLKVIVG237 ALIHSVKKLA247 DVTILTIFCL257 SVFALVGLQL267 FKGNLKNKCV 277 KNDMAYSSHR293 KPDIYINKRG303 TSDPLLCGNG313 SDSGHCPDGY323 ICLKTSDNPD 333 FNYTSFDSFA343 WAFLSLFRLM353 TQDSWERLYQ363 QTLRTSGKIY373 MIFFVLVIFL 383 GSFYLVNLIL393 AVVTMAYEEQ403 NQATWVKLKT656 ILFGLVTDPF666 AELTITLCIV 676 VNTIFMAMEH686 HGMSPTFEAM696 LQIGNIVFTI706 FFTAEMVFKI716 IAFDPYYYFQ 726 KKWNIFDCII736 VTVSLLELGV746 AKKGSLSVLR756 SFRLLRVFKL766 AKSWPTLNTL 776 IKIIGNSVGA786 LGNLTIILAI796 IVFVFALVGK806 QLLGENYRNN816 RKNISAPHED 826 WPRWHMHDFF836 HSFLIVFRIL846 CGEWIENMWA856 CMEVGQKSIC866 LILFLTVMVL 876 GNLVVLNLFI886 ALLLNSFFAD1136 VGWQVRKTCY1146 RIVEHSWFES1156 FIIFMILLSS 1166 GSLAFEDYYL1176 DQKPTVKALL1186 EYTDRVFTFI1196 FVFEMLLKWV1206 AYGFKKYFTN 1216 AWCWLDFLIV1226 NISLISLTAK1236 ILEYSEVAPI1246 KALRTLRALR1256 PLRALSRFEG 1266 MRVVVDALVG1276 AIPSIMNVLL1286 VCLIFWLIFS1296 IMGVNLFAGK1306 FWRCINYTDG 1316 EFSLVPLSIV1326 NNKSDCKIQN1336 STGSFFWVNV1346 KVNFDNVAMG1356 YLALLQVATF 1366 KGWMDIMYAA1376 VDSREVNMQP1386 KWEDNVYMYL1396 YFVIFIIFGG1406 FFTLNLFVGV 1416 IIDNFNQQKK1426 KLGGQDIFMT1436 EEQKKYYNAM1446 KKLGSKKPQK1456 PIPRPLNKFQ 1466 GFVFDIVTRQ1476 AFDITIMVLI1486 CLNMITMMVE1496 TDDQSEEKTK1506 ILGKINQFFV 1516 AVFTGECVMK1526 MFALRQYYFT1536 NGWNVFDFIV1546 VVLSIASLIF1556 SAILKSLQSY 1566 FSPTLFRVIR1576 LARIGRILRL1586 IRAAKGIRTL1596 LFALMMSLPA1606 LFNIGLLLFL 1616 VMFIYSIFGM1626 SSFPHVRWEA1636 GIDDMFNFQT1646 FANSMLCLFQ1656 ITTSAGWDGL 1666 LSPILNTGPP1676 YCDPNLPNSN1686 GTRGDCGSPA1696 VGIIFFTTYI1706 IISFLIMVNM 1716 YIAVILENFN1726 VA
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .LPE or .LPE2 or .LPE3 or :3LPE;style chemicals stick;color identity;select .A:260 or .A:263 or .A:267 or .A:372 or .A:373 or .A:375 or .A:376 or .A:379 or .A:382 or .A:677 or .A:680 or .A:681 or .A:684 or .A:686 or .A:690 or .A:692 or .A:693 or .A:696 or .A:780 or .A:783 or .A:784 or .A:791 or .A:794 or .A:843 or .A:846 or .A:847 or .A:881 or .A:884 or .A:1163 or .A:1166 or .A:1167 or .A:1170 or .A:1171 or .A:1173 or .A:1216 or .A:1217 or .A:1218 or .A:1221 or .A:1255 or .A:1257 or .A:1258 or .A:1260 or .A:1261 or .A:1271 or .A:1272 or .A:1275 or .A:1289 or .A:1354 or .A:1357 or .A:1366 or .A:1402 or .A:1403 or .A:1404 or .A:1406 or .A:1407 or .A:1408 or .A:1410 or .A:1438 or .A:1439 or .A:1442 or .A:1445 or .A:1446 or .A:1449 or .A:1567 or .A:1568 or .A:1570 or .A:1571 or .A:1574 or .A:1577 or .A:1601 or .A:1604 or .A:1605 or .A:1607 or .A:1608 or .A:1611 or .A:1614 or .A:1615 or .A:1616 or .A:1619 or .A:1647 or .A:1716; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE260
4.788
VAL263
4.060
LEU267
4.429
ILE372
4.163
TYR373
3.876
ILE375
4.523
PHE376
3.763
LEU379
3.869
PHE382
4.295
VAL677
4.556
ILE680
3.020
PHE681
4.267
MET684
3.377
HIS686
4.463
SER690
3.161
THR692
2.433
PHE693
4.309
MET696
3.936
ILE780
3.851
SER783
3.800
VAL784
3.353
THR791
3.989
LEU794
3.888
PHE843
3.532
LEU846
3.424
CYS847
4.147
VAL881
3.832
LEU884
3.705
LEU1163
4.609
SER1166
3.712
GLY1167
3.441
ALA1170
2.670
PHE1171
2.831
ASP1173
4.136
ASN1216
3.374
ALA1217
3.547
TRP1218
3.626
LEU1221
4.597
LEU1255
4.061
PRO1257
4.636
LEU1258
4.619
ALA1260
4.811
LEU1261
4.497
VAL1271
4.840
ASP1272
4.338
VAL1275
4.648
LEU1289
4.304
ALA1354
4.066
TYR1357
4.203
PHE1366
3.861
ILE1402
3.642
ILE1403
3.503
PHE1404
3.894
GLY1406
4.983
PHE1407
3.275
PHE1408
3.746
LEU1410
4.941
GLU1438
4.821
GLN1439
3.210
TYR1442
3.824
ALA1445
4.368
MET1446
4.098
LEU1449
3.257
PHE1567
2.522
SER1568
3.354
THR1570
3.584
LEU1571
3.092
VAL1574
3.275
LEU1577
4.428
MET1601
4.723
LEU1604
4.117
PRO1605
3.527
LEU1607
3.916
PHE1608
3.844
GLY1611
3.882
LEU1614
4.751
PHE1615
3.603
LEU1616
3.291
PHE1619
3.705
PHE1647
3.331
MET1716
3.840
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Phosphatidylserine | Ligand Info | |||||
| Structure Description | Human Nav1.8 with A-803467, class I | PDB:7WE4 | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [1] |
| PDB Sequence |
LIRRTAIKVS
127 VHSWFSLFIT137 VTILVNCVCM147 TRTDLPEKIE157 YVFTVIYTFE167 ALIKILARGF 177 CLNEFTYLRD187 PWNWLDFSVI197 TLAYVGTAID207 LRGISGLRTF217 RVLRALKTVS 227 VIPGLKVIVG237 ALIHSVKKLA247 DVTILTIFCL257 SVFALVGLQL267 FKGNLKNKCV 277 KNDMAYSSHR293 KPDIYINKRG303 TSDPLLCGNG313 SDSGHCPDGY323 ICLKTSDNPD 333 FNYTSFDSFA343 WAFLSLFRLM353 TQDSWERLYQ363 QTLRTSGKIY373 MIFFVLVIFL 383 GSFYLVNLIL393 AVVTMAYEEQ403 NQATWVKLKT656 ILFGLVTDPF666 AELTITLCIV 676 VNTIFMAMEH686 HGMSPTFEAM696 LQIGNIVFTI706 FFTAEMVFKI716 IAFDPYYYFQ 726 KKWNIFDCII736 VTVSLLELGV746 AKKGSLSVLR756 SFRLLRVFKL766 AKSWPTLNTL 776 IKIIGNSVGA786 LGNLTIILAI796 IVFVFALVGK806 QLLGENYRNN816 RKNISAPHED 826 WPRWHMHDFF836 HSFLIVFRIL846 CGEWIENMWA856 CMEVGQKSIC866 LILFLTVMVL 876 GNLVVLNLFI886 ALLLNSFFAD1136 VGWQVRKTCY1146 RIVEHSWFES1156 FIIFMILLSS 1166 GSLAFEDYYL1176 DQKPTVKALL1186 EYTDRVFTFI1196 FVFEMLLKWV1206 AYGFKKYFTN 1216 AWCWLDFLIV1226 NISLISLTAK1236 ILEYSEVAPI1246 KALRTLRALR1256 PLRALSRFEG 1266 MRVVVDALVG1276 AIPSIMNVLL1286 VCLIFWLIFS1296 IMGVNLFAGK1306 FWRCINYTDG 1316 EFSLVPLSIV1326 NNKSDCKIQN1336 STGSFFWVNV1346 KVNFDNVAMG1356 YLALLQVATF 1366 KGWMDIMYAA1376 VDSREVNMQP1386 KWEDNVYMYL1396 YFVIFIIFGG1406 FFTLNLFVGV 1416 IIDNFNQQKK1426 KLGGQDIFMT1436 EEQKKYYNAM1446 KKLGSKKPQK1456 PIPRPLNKFQ 1466 GFVFDIVTRQ1476 AFDITIMVLI1486 CLNMITMMVE1496 TDDQSEEKTK1506 ILGKINQFFV 1516 AVFTGECVMK1526 MFALRQYYFT1536 NGWNVFDFIV1546 VVLSIASLIF1556 SAILKSLQSY 1566 FSPTLFRVIR1576 LARIGRILRL1586 IRAAKGIRTL1596 LFALMMSLPA1606 LFNIGLLLFL 1616 VMFIYSIFGM1626 SSFPHVRWEA1636 GIDDMFNFQT1646 FANSMLCLFQ1656 ITTSAGWDGL 1666 LSPILNTGPP1676 YCDPNLPNSN1686 GTRGDCGSPA1696 VGIIFFTTYI1706 IISFLIMVNM 1716 YIAVILENFN1726 VA
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .P5S or .P5S2 or .P5S3 or :3P5S;style chemicals stick;color identity;select .A:254 or .A:257 or .A:336 or .A:343 or .A:344 or .A:346 or .A:347 or .A:350 or .A:858 or .A:863 or .A:864 or .A:867 or .A:868 or .A:871 or .A:872 or .A:875 or .A:1285 or .A:1288 or .A:1289 or .A:1292 or .A:1352 or .A:1354 or .A:1355 or .A:1357 or .A:1358 or .A:1361 or .A:1468 or .A:1471 or .A:1472 or .A:1475 or .A:1477 or .A:1478 or .A:1481 or .A:1482 or .A:1518 or .A:1525 or .A:1673 or .A:1695 or .A:1696 or .A:1699 or .A:1700 or .A:1703 or .A:1704 or .A:1707; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE254
4.866
LEU257
4.720
TYR336
3.523
ALA343
4.053
TRP344
3.333
PHE346
4.075
LEU347
4.024
PHE350
3.350
MET858
4.696
LYS863
3.309
SER864
3.744
LEU867
3.970
ILE868
4.149
LEU871
2.793
THR872
3.553
VAL875
4.532
LEU1285
3.863
CYS1288
3.658
LEU1289
3.949
TRP1292
3.883
ASN1352
3.826
ALA1354
3.456
MET1355
3.654
TYR1357
4.386
LEU1358
4.189
LEU1361
3.938
PHE1468
3.533
ASP1471
4.793
ILE1472
3.590
ARG1475
2.678
ALA1477
4.218
PHE1478
3.881
THR1481
4.403
ILE1482
4.562
VAL1518
4.034
MET1525
3.483
THR1673
4.642
PRO1695
3.707
ALA1696
3.592
ILE1699
3.685
ILE1700
3.885
THR1703
3.815
THR1704
3.751
ILE1707
3.584
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural basis for high-voltage activation and subtype-specific inhibition of human Na(v)1.8. Proc Natl Acad Sci U S A. 2022 Jul 26;119(30):e2208211119. | ||||
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