Found 1781 hits Enz. Inhib. hit(s) with Target = 'Sodium channel protein type 10 subunit alpha' Target/Host
(Institution) | Ligand | Target/Host
Links | Ligand
Links | Trg + Lig
Links | Ki
nM | ΔG°
kJ/mole | IC50
nM | Kd
nM | EC50/IC50
nM | koff
s-1 | kon
M-1s-1 | pH | Temp
°C |
|---|
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM26948
(8-[4,4-bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-tr...)Show SMILES Fc1ccc(cc1)C(CCCN1CCC2(CC1)N(CNC2=O)c1ccccc1)c1ccc(F)cc1 Show InChI InChI=1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35) | PDB
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| 130 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50178861
((1R,2R)-N1-methyl-N1-((2'-sulfamoylbiphenyl-4-yl)m...)Show SMILES CN(Cc1ccc(cc1)-c1ccccc1S(N)(=O)=O)C(=O)[C@@H]1CCC[C@H]1C(=O)NCc1ccc(OC(F)(F)F)cc1 Show InChI InChI=1S/C29H30F3N3O5S/c1-35(18-20-9-13-21(14-10-20)23-5-2-3-8-26(23)41(33,38)39)28(37)25-7-4-6-24(25)27(36)34-17-19-11-15-22(16-12-19)40-29(30,31)32/h2-3,5,8-16,24-25H,4,6-7,17-18H2,1H3,(H,34,36)(H2,33,38,39)/t24-,25-/m1/s1 | PDB
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antibodypedia
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| 180 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Purdue Pharma L.P.
Curated by ChEMBL
| Assay Description
Binding affinity to Nav1.8 sodium channel |
J Med Chem 50: 2583-8 (2007)
Article DOI: 10.1021/jm061005v
BindingDB Entry DOI: 10.7270/Q22J6BJB |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM21398
(4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1...)Show SMILES OC1(CCN(CCCC(=O)c2ccc(F)cc2)CC1)c1ccc(Cl)cc1 Show InChI InChI=1S/C21H23ClFNO2/c22-18-7-5-17(6-8-18)21(26)11-14-24(15-12-21)13-1-2-20(25)16-3-9-19(23)10-4-16/h3-10,26H,1-2,11-15H2 | PDB
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| 200 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM50026066
(1-(4,4-bis(4-fluorophenyl)butyl)-4-(4-chloro-3-(tr...)Show SMILES OC1(CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccc(Cl)c(c1)C(F)(F)F Show InChI InChI=1S/C28H27ClF5NO/c29-26-12-7-21(18-25(26)28(32,33)34)27(36)13-16-35(17-14-27)15-1-2-24(19-3-8-22(30)9-4-19)20-5-10-23(31)11-6-20/h3-12,18,24,36H,1-2,13-17H2 | PDB
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| 500 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM84994
(CAS_163091 | NSC_163091 | ORG-5222)Show InChI InChI=1S/C17H16ClNO/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19/h2-8,14-15H,9-10H2,1H3 | PDB
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| 630 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM22913
(CHEMBL1237146 | CHEMBL498770 | Iodophenpropit | {[...)Show SMILES NC(SCCCc1cnc[nH]1)=NCCc1ccc(I)cc1 |w:11.12| Show InChI InChI=1S/C15H19IN4S/c16-13-5-3-12(4-6-13)7-8-19-15(17)21-9-1-2-14-10-18-11-20-14/h3-6,10-11H,1-2,7-9H2,(H2,17,19)(H,18,20) | PDB
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| 1.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit
Curated by PDSP Ki Database
| |
Br J Pharmacol 116: 2315-21 (1995)
Article DOI: 10.1111/j.1476-5381.1995.tb15071.x
BindingDB Entry DOI: 10.7270/Q2ZK5F64 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM50001786
(1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl...)Show SMILES Fc1ccc(cc1)-n1cc(C2CCN(CCN3CCNC3=O)CC2)c2cc(Cl)ccc12 Show InChI InChI=1S/C24H26ClFN4O/c25-18-1-6-23-21(15-18)22(16-30(23)20-4-2-19(26)3-5-20)17-7-10-28(11-8-17)13-14-29-12-9-27-24(29)31/h1-6,15-17H,7-14H2,(H,27,31) | PDB
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| 1.19E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM35255
(2-Chlor-11-(2-dimethylaminoaethoxy)-dibenzo(b,f)-t...)Show InChI InChI=1S/C18H18ClNOS/c1-20(2)9-10-21-16-11-13-5-3-4-6-17(13)22-18-8-7-14(19)12-15(16)18/h3-8,11-12H,9-10H2,1-2H3 | PDB
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| 1.29E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM81483
(CAS_1893-33-0 | NSC_4830 | PIPAMPERONE)Show SMILES NC(=O)C1(CCN(CCCC(=O)c2ccc(F)cc2)CC1)N1CCCCC1 Show InChI InChI=1S/C21H30FN3O2/c22-18-8-6-17(7-9-18)19(26)5-4-12-24-15-10-21(11-16-24,20(23)27)25-13-2-1-3-14-25/h6-9H,1-5,10-16H2,(H2,23,27) | PDB
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| 2.13E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM50048803
(5-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)et...)Show SMILES Clc1cc2NC(=O)Cc2cc1CCN1CCN(CC1)c1nsc2ccccc12 Show InChI InChI=1S/C21H21ClN4OS/c22-17-13-18-15(12-20(27)23-18)11-14(17)5-6-25-7-9-26(10-8-25)21-16-3-1-2-4-19(16)28-24-21/h1-4,11,13H,5-10,12H2,(H,23,27) | PDB
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| 2.62E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM50001885
((risperidone)3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-...)Show SMILES Cc1nc2CCCCn2c(=O)c1CCN1CCC(CC1)c1noc2cc(F)ccc12 Show InChI InChI=1S/C23H27FN4O2/c1-15-18(23(29)28-10-3-2-4-21(28)25-15)9-13-27-11-7-16(8-12-27)22-19-6-5-17(24)14-20(19)30-26-22/h5-6,14,16H,2-4,7-13H2,1H3 | PDB
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| 3.86E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM22869
(6-chloro-10-(4-methylpiperazin-1-yl)-2,9-diazatric...)Show SMILES CN1CCN(CC1)C1=c2ccccc2=Nc2ccc(Cl)cc2N1 |c:8,15| Show InChI InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,21H,8-11H2,1H3 | PDB
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| 4.56E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM82479
(CAS_132539-06-1 | NSC_4585 | OLANZAPINE | USRE4934...)Show SMILES CN1CCN(CC1)C1=c2cc(C)sc2=Nc2ccccc2N1 |c:8,15| Show InChI InChI=1S/C17H20N4S/c1-12-11-13-16(21-9-7-20(2)8-10-21)18-14-5-3-4-6-15(14)19-17(13)22-12/h3-6,11,18H,7-10H2,1-2H3 | PDB
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| 5.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM50252513
(3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1...)Show SMILES Cc1nc2C(O)CCCn2c(=O)c1CCN1CCC(CC1)c1noc2cc(F)ccc12 Show InChI InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3 | PDB
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| 5.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM50095890
(2-[2-(4-Dibenzo[b,f][1,4]thiazepin-11-yl-1-piperaz...)Show SMILES OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2ccccc12 |t:13| Show InChI InChI=1S/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2 | PDB
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| 5.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM21398
(4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1...)Show SMILES OC1(CCN(CCCC(=O)c2ccc(F)cc2)CC1)c1ccc(Cl)cc1 Show InChI InChI=1S/C21H23ClFNO2/c22-18-7-5-17(6-8-18)21(26)11-14-24(15-12-21)13-1-2-20(25)16-3-9-19(23)10-4-16/h3-10,26H,1-2,11-15H2 | PDB
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| 7.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Synthélabo Recherche
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 280: 83-97 (1997)
BindingDB Entry DOI: 10.7270/Q2NZ865X |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM22914
(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)Show InChI InChI=1S/C15H24N4S/c20-15(18-13-4-2-1-3-5-13)19-8-6-12(7-9-19)14-10-16-11-17-14/h10-13H,1-9H2,(H,16,17)(H,18,20) | PDB
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| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit
Curated by PDSP Ki Database
| |
Br J Pharmacol 116: 2315-21 (1995)
Article DOI: 10.1111/j.1476-5381.1995.tb15071.x
BindingDB Entry DOI: 10.7270/Q2ZK5F64 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM81790
(Amisulpride | CAS_71675-85-9 | NSC_2159 | US101672...)Show InChI InChI=1S/C17H27N3O4S/c1-4-20-8-6-7-12(20)11-19-17(21)13-9-16(25(22,23)5-2)14(18)10-15(13)24-3/h9-10,12H,4-8,11,18H2,1-3H3,(H,19,21) | PDB
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| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Synthélabo Recherche
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 280: 83-97 (1997)
BindingDB Entry DOI: 10.7270/Q2NZ865X |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM50122872
(4-Amino-5-chloro-2,3-dihydro-benzofuran-7-carboxyl...)Show InChI InChI=1S/C18H26ClN3O3/c1-24-9-2-6-22-7-3-12(4-8-22)21-18(23)14-11-15(19)16(20)13-5-10-25-17(13)14/h11-12H,2-10,20H2,1H3,(H,21,23) | PDB
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| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
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Eur J Pharmacol 423: 71-83 (2001)
Article DOI: 10.1016/s0014-2999(01)01087-1
BindingDB Entry DOI: 10.7270/Q23T9FSX |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM81780
(CAS_6438382 | NSC_6438382 | SR 46349B)Show SMILES CN(C)CCON=C(C=Cc1ccc(O)cc1)c1ccccc1F |w:6.5,8.7| Show InChI InChI=1S/C19H21FN2O2/c1-22(2)13-14-24-21-19(17-5-3-4-6-18(17)20)12-9-15-7-10-16(23)11-8-15/h3-12,23H,13-14H2,1-2H3 | PDB
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| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Sanofi Recherche
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 262: 759-68 (1992)
BindingDB Entry DOI: 10.7270/Q27S7M7Z |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM22869
(6-chloro-10-(4-methylpiperazin-1-yl)-2,9-diazatric...)Show SMILES CN1CCN(CC1)C1=c2ccccc2=Nc2ccc(Cl)cc2N1 |c:8,15| Show InChI InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,21H,8-11H2,1H3 | PDB
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| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Synthélabo Recherche
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 280: 83-97 (1997)
BindingDB Entry DOI: 10.7270/Q2NZ865X |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547894
(CHEMBL4760292 | US11377438, Example 172)Show SMILES Cc1nc(N2CCCC(F)(F)CC2)c(cc1Cl)C(=O)Nc1ccnc(c1)S(N)(=O)=O | PDB
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| PC cid
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UniChem
| Article
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| n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assay |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00568
BindingDB Entry DOI: 10.7270/Q21Z481V |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547894
(CHEMBL4760292 | US11377438, Example 172)Show SMILES Cc1nc(N2CCCC(F)(F)CC2)c(cc1Cl)C(=O)Nc1ccnc(c1)S(N)(=O)=O | PDB
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| US Patent
| n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
The following buffers were used for the QubeŽ recordings: External buffer for Nav1.8 QubeŽ recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 1... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q22R3VXD |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547925
(CHEMBL4798938)Show SMILES COc1cc(Oc2ccc(OC(F)(F)F)c(F)c2OC)c(C(=O)Nc2ccnc(c2)C(N)=O)c(F)c1C(F)(F)F | PDB
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| n/a | n/a | 0.400 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00590
BindingDB Entry DOI: 10.7270/Q2NP281X |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547896
(CHEMBL4777598 | US11377438, Example 184)Show SMILES Cc1nc(N2CCCC(F)(F)CC2)c(cc1C(F)(F)F)C(=O)Nc1ccnc(c1)S(N)(=O)=O | PDB
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TBA
| Assay Description
The following buffers were used for the QubeŽ recordings: External buffer for Nav1.8 QubeŽ recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 1... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q22R3VXD |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547896
(CHEMBL4777598 | US11377438, Example 184)Show SMILES Cc1nc(N2CCCC(F)(F)CC2)c(cc1C(F)(F)F)C(=O)Nc1ccnc(c1)S(N)(=O)=O | PDB
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TBA
| Assay Description
Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assay |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00568
BindingDB Entry DOI: 10.7270/Q21Z481V |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM560005
(US11377438, Example 53)Show SMILES C[C@H]1CN(C[C@@H](C)C1(F)F)c1nc(C)c(Cl)cc1C(=O)Nc1ccnc(c1)S(N)(=O)=O | PDB
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| n/a | n/a | 0.800 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
The following buffers were used for the QubeŽ recordings: External buffer for Nav1.8 QubeŽ recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 1... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q22R3VXD |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM529546
(2,4-dichloro-6-(4-chloro-2- | US11203571, Compound...)Show SMILES COc1cc(Cl)ccc1Oc1cc(Cl)cc(Cl)c1C(=O)Nc1cccc(c1)S(N)(=O)=O | PDB
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| n/a | n/a | 0.800 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2NC64DM |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547926
(CHEMBL4753280)Show SMILES COc1c(Oc2cc(c(C)c(F)c2C(=O)Nc2ccnc(c2)C(N)=O)C(F)(F)F)ccc(OC(F)(F)F)c1F | PDB
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| n/a | n/a | 0.800 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00590
BindingDB Entry DOI: 10.7270/Q2NP281X |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547885
(CHEMBL4781110 | US11377438, Example 18)Show SMILES NS(=O)(=O)c1cc(NC(=O)c2ccc(CC3CC3)nc2N2CCCC(F)(F)CC2)ccn1 | PDB
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| n/a | n/a | 0.900 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assay |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00568
BindingDB Entry DOI: 10.7270/Q21Z481V |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM529543
(2,4-dichloro-6-(4-fluoro-2-methoxyphenoxy)-N-(3-su...)Show SMILES COc1cc(F)ccc1Oc1cc(Cl)cc(Cl)c1C(=O)Nc1cccc(c1)S(N)(=O)=O | PDB
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| n/a | n/a | 0.900 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2NC64DM |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547885
(CHEMBL4781110 | US11377438, Example 18)Show SMILES NS(=O)(=O)c1cc(NC(=O)c2ccc(CC3CC3)nc2N2CCCC(F)(F)CC2)ccn1 | PDB
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| n/a | n/a | 0.900 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
The following buffers were used for the QubeŽ recordings: External buffer for Nav1.8 QubeŽ recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 1... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q22R3VXD |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM161329
(US10087143, Compound 114 | US10738009, Compound 11...)Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1 Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-17-6-10(22)2-3-15(17)28-16-9-14(21)13(20)8-12(16)19(26)24-11-4-5-23-18(25)7-11/h2-9H,1H3,(H2,23,24,25,26) | PDB
KEGG
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VERTEX PHARMACEUTICALS INCORPORATED
US Patent
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
US Patent US9051270 (2015)
BindingDB Entry DOI: 10.7270/Q2B27T1F |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM181203
(US9139529, 46 | US9783501, Compound 46)Show SMILES COc1cc(F)ccc1Oc1nc2ccccc2nc1C(=O)Nc1cccc(c1)S(C)(=O)=O Show InChI InChI=1S/C23H18FN3O5S/c1-31-20-12-14(24)10-11-19(20)32-23-21(26-17-8-3-4-9-18(17)27-23)22(28)25-15-6-5-7-16(13-15)33(2,29)30/h3-13H,1-2H3,(H,25,28) | PDB
KEGG
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VERTEX PHARMACEUTICALS INCORPORATED
US Patent
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
US Patent US9139529 (2015)
BindingDB Entry DOI: 10.7270/Q2ZG6R1Z |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Rattus norvegicus (Rat)) | BDBM161329
(US10087143, Compound 114 | US10738009, Compound 11...)Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1 Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-17-6-10(22)2-3-15(17)28-16-9-14(21)13(20)8-12(16)19(26)24-11-4-5-23-18(25)7-11/h2-9H,1H3,(H2,23,24,25,26) | PDB
KEGG
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VERTEX PHARMACEUTICALS INCORPORATED
US Patent
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
US Patent US9163042 (2015)
BindingDB Entry DOI: 10.7270/Q21Z4361 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50330935
(CHEMBL1277958 | N-(m-Tolyl)-6-(4-ethoxyphenyl)-pyr...)Show InChI InChI=1S/C20H19N3O2/c1-3-25-17-9-7-15(8-10-17)18-12-21-13-19(23-18)20(24)22-16-6-4-5-14(2)11-16/h4-13H,3H2,1-2H3,(H,22,24) | PDB
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Abbott Laboratories
Curated by ChEMBL
| Assay Description
Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltageclamp electrophysiology assay |
Bioorg Med Chem 18: 7816-25 (2010)
Article DOI: 10.1016/j.bmc.2010.09.057
BindingDB Entry DOI: 10.7270/Q24B31KG |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM161329
(US10087143, Compound 114 | US10738009, Compound 11...)Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1 Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-17-6-10(22)2-3-15(17)28-16-9-14(21)13(20)8-12(16)19(26)24-11-4-5-23-18(25)7-11/h2-9H,1H3,(H2,23,24,25,26) | PDB
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
VERTEX PHARMACEUTICALS INCORPORATED
US Patent
| Assay Description
Sodium channels are voltage-dependent proteins that can be activated by inducing membrane voltage changes by applying electric fields. The electrical... |
US Patent US10087143 (2018)
BindingDB Entry DOI: 10.7270/Q2HD7XP6 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM161329
(US10087143, Compound 114 | US10738009, Compound 11...)Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1 Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-17-6-10(22)2-3-15(17)28-16-9-14(21)13(20)8-12(16)19(26)24-11-4-5-23-18(25)7-11/h2-9H,1H3,(H2,23,24,25,26) | PDB
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VERTEX PHARMACEUTICALS INCORPORATED
US Patent
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
US Patent US10738009 (2020)
BindingDB Entry DOI: 10.7270/Q21Z47HQ |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547890
(CHEMBL4745699 | US11377438, Example 46)Show SMILES NS(=O)(=O)c1cc(NC(=O)c2cc(CC3CC3)cnc2N2CCCC(F)(F)CC2)ccn1 | PDB
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TBA
| Assay Description
Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assay |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00568
BindingDB Entry DOI: 10.7270/Q21Z481V |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM161329
(US10087143, Compound 114 | US10738009, Compound 11...)Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1 Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-17-6-10(22)2-3-15(17)28-16-9-14(21)13(20)8-12(16)19(26)24-11-4-5-23-18(25)7-11/h2-9H,1H3,(H2,23,24,25,26) | PDB
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VERTEX PHARMACEUTICALS INCORPORATED
US Patent
| Assay Description
1) Pre-spotted compounds (in neat DMSO) into compound plates. Vehicle control (neat DMSO), the positive control (20 mM DMSO stock tetracaine, 125 ... |
US Patent US9758483 (2017)
BindingDB Entry DOI: 10.7270/Q28C9ZCT |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM161329
(US10087143, Compound 114 | US10738009, Compound 11...)Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1 Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-17-6-10(22)2-3-15(17)28-16-9-14(21)13(20)8-12(16)19(26)24-11-4-5-23-18(25)7-11/h2-9H,1H3,(H2,23,24,25,26) | PDB
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Vertex Pharmaceuticals Incorporated
US Patent
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
US Patent US10787472 (2020)
BindingDB Entry DOI: 10.7270/Q2377CSG |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547890
(CHEMBL4745699 | US11377438, Example 46)Show SMILES NS(=O)(=O)c1cc(NC(=O)c2cc(CC3CC3)cnc2N2CCCC(F)(F)CC2)ccn1 | PDB
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TBA
| Assay Description
The following buffers were used for the QubeŽ recordings: External buffer for Nav1.8 QubeŽ recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 1... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q22R3VXD |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM529544
(2,4-dichloro-6-(4-fluoro-2- | US11203571, Compound...)Show SMILES Cc1cc(F)ccc1Oc1cc(Cl)cc(Cl)c1C(=O)Nc1cccc(c1)S(N)(=O)=O | PDB
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TBA
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2NC64DM |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM529537
(2-(4-fluoro-2-methoxyphenoxy)-N-(3-sulfamoylphenyl...)Show SMILES COc1cc(F)ccc1Oc1cc(cc(c1C(=O)Nc1cccc(c1)S(N)(=O)=O)C(F)(F)F)C(F)(F)F | PDB
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TBA
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2NC64DM |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM529525
(4,5-dichloro-2-(4-fluoro-2-methoxyphenoxy)-N-(3-su...)Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cccc(c1)S(N)(=O)=O | PDB
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TBA
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2NC64DM |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM181203
(US9139529, 46 | US9783501, Compound 46)Show SMILES COc1cc(F)ccc1Oc1nc2ccccc2nc1C(=O)Nc1cccc(c1)S(C)(=O)=O Show InChI InChI=1S/C23H18FN3O5S/c1-31-20-12-14(24)10-11-19(20)32-23-21(26-17-8-3-4-9-18(17)27-23)22(28)25-15-6-5-7-16(13-15)33(2,29)30/h3-13H,1-2H3,(H,25,28) | PDB
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VERTEX PHARMACEUTICALS INCORPORATED
US Patent
| Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons... |
US Patent US9783501 (2017)
BindingDB Entry DOI: 10.7270/Q25B04NS |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM50547929
(CHEMBL4744908)Show SMILES COc1c(Cl)cc(Oc2ccc(OC(F)(F)F)c(F)c2OC)c(C(=O)Nc2ccnc(c2)C(N)=O)c1F | PDB
UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00590
BindingDB Entry DOI: 10.7270/Q2NP281X |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM560161
(US11377438, Example 201)Show SMILES Cc1nc(N2CCCCCC2)c(C(=O)Nc2ccnc(c2)S(N)(=O)=O)c(C)c1Cl | PDB
UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
The following buffers were used for the QubeŽ recordings: External buffer for Nav1.8 QubeŽ recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 1... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q22R3VXD |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM560001
(US11377438, Example 49)Show SMILES C[C@H]1CN(CCC1(Cl)Cl)c1ncc(cc1C(=O)Nc1ccnc(c1)S(N)(=O)=O)C(F)(F)F | PDB
UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1.40 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
The following buffers were used for the QubeŽ recordings: External buffer for Nav1.8 QubeŽ recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 1... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q22R3VXD |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 10 subunit alpha
(Homo sapiens (Human)) | BDBM560008
(US11377438, Example 55)Show SMILES C[C@H]1CN(CCC1(F)F)c1nc(C)c(Cl)cc1C(=O)Nc1ccnc(c1)S(N)(=O)=O | PDB
UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1.40 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
The following buffers were used for the QubeŽ recordings: External buffer for Nav1.8 QubeŽ recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 1... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q22R3VXD |
More data for this
Ligand-Target Pair | |
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