target,target_id,target_uniprot,target_species,ligand,ligand_id,ligand_species,ligand_pubchem_cid,smiles,inchi,inchikey,type,action,action_comment,endogenous,primary_target,concentration_range,affinity_parameter,affinity_high,affinity_median,affinity_low,original_affinity_units,original_affinity_low_nm,original_affinity_median_nm,original_affinity_high_nm,original_affinity_relation,assay_description,receptor_site,ligand_context,pubmed_id Nav1.5,582,P15389,Rat,quinidine,2342,,441074,C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@H](c1ccnc2c1cc(OC)cc2)O,"InChI=1S/C20H24N2O2/c1-3-13-12-22-9-7-14(13)10-19(22)20(23)16-6-8-21-18-5-4-15(24-2)11-17(16)18/h3-6,8,11,13-14,19-20,23H,1,7,9-10,12H2,2H3/t13-,14-,19+,20-/m0/s1",LOUPRKONTZGTKE-LHHVKLHASA-N,Channel blocker,Pore blocker,,,,,pIC50,5.0,,4.4,,,,,=,,,,2546048|8301556, Nav1.5,582,Q14524,Human,bupivacaine,2397,,2474,CCCCN1CCCCC1C(=O)Nc1c(C)cccc1C,"InChI=1S/C18H28N2O/c1-4-5-12-20-13-7-6-11-16(20)18(21)19-17-14(2)9-8-10-15(17)3/h8-10,16H,4-7,11-13H2,1-3H3,(H,19,21)",LEBVLXFERQHONN-UHFFFAOYSA-N,Channel blocker,Pore blocker,Blockade of inactivated channel,,,,pIC50,,5.66,,IC50,,2180.0,,=,,,,25692452, Nav1.5,582,Q14524,Human,bupivacaine,2397,,2474,CCCCN1CCCCC1C(=O)Nc1c(C)cccc1C,"InChI=1S/C18H28N2O/c1-4-5-12-20-13-7-6-11-16(20)18(21)19-17-14(2)9-8-10-15(17)3/h8-10,16H,4-7,11-13H2,1-3H3,(H,19,21)",LEBVLXFERQHONN-UHFFFAOYSA-N,Channel blocker,Pore blocker,Open-channel block,,,,pIC50,,4.16,,IC50,,69500.0,,=,,,,25692452, Nav1.5,582,P15389,Rat,amiodarone,2566,,2157,CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2,"InChI=1S/C25H29I2NO3/c1-4-7-11-22-23(18-10-8-9-12-21(18)31-22)24(29)17-15-19(26)25(20(27)16-17)30-14-13-28(5-2)6-3/h8-10,12,15-16H,4-7,11,13-14H2,1-3H3",IYIKLHRQXLHMJQ-UHFFFAOYSA-N,Channel blocker,Pore blocker,,,,,pIC50,,5.7,,,,,,=,,,,2546697, Nav1.5,582,Q14524,Human,jingzhaotoxin-III,2574,,,,,,Gating inhibitor,Voltage-dependent inhibition,,,,,pKi,,6.5,,,,,,=,Whole-cell voltage clamp of human embryonic kidney cells (HEK293) transfected with human Nav1.5.,,,21665957, Nav1.5,582,Q14524,Human,AFT-II,2613,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pEC50,,7.2,,,,,,=,,,,15169781, Nav1.5,582,Q14524,Human,ATX-II,2614,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pEC50,,7.3,,,,,,=,,,,15169781, Nav1.5,582,Q14524,Human,Bc-III,2615,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pEC50,,6.5,,,,,,=,,,,15169781, Nav1.5,582,P15389,Rat,tetrodotoxin,2616,,6324668,OC[C@@]1(O)[C@H]2O[C@]3(O[C@@H]1[C@H]1[C@@]([C@H]2O)([C@@H]3O)NC(=N[C@@H]1O)N)O,"InChI=1S/C11H17N3O8/c12-8-13-6(17)2-4-9(19,1-15)5-3(16)10(2,14-8)7(18)11(20,21-4)22-5/h2-7,15-20H,1H2,(H3,12,13,14)/t2-,3+,4-,5+,6-,7+,9+,10-,11+/m1/s1",CFMYXEVWODSLAX-QYIGHCJRSA-N,Channel blocker,Pore blocker,,,,,pKd,,5.8,,Kd,,1520.0,,=,,,,8967455|2175715, Nav1.5,582,Q14524,Human,aconitine,2617,,245005,COC[C@@]12CN(CC)C3[C@]4([C@@H]2[C@@H](OC)[C@@H]3[C@@]2([C@@H]3[C@H]4C[C@@]([C@@H]3OC(=O)c3ccccc3)([C@H]([C@@H]2O)OC)O)OC(=O)C)[C@H](C[C@H]1O)OC,"InChI=1S/C34H47NO11/c1-7-35-15-31(16-41-3)20(37)13-21(42-4)33-19-14-32(40)28(45-30(39)18-11-9-8-10-12-18)22(19)34(46-17(2)36,27(38)29(32)44-6)23(26(33)35)24(43-5)25(31)33/h8-12,19-29,37-38,40H,7,13-16H2,1-6H3/t19-,20-,21+,22-,23+,24+,25-,26?,27+,28-,29+,31+,32-,33+,34-/m1/s1",XFSBVAOIAHNAPC-XTHSEXKGSA-N,Activator,Partial agonist,,,,30-100,,,,,,,,,=,,,,11826163|2433183, Nav1.5,582,P15389,Rat,α-scorpion toxin 2,2618,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pKd,,7.7,,,,,,=,,,,8663157, Nav1.5,582,P15389,Rat,batrachotoxin,2619,,6324647,CN1CCO[C@@]23[C@](C1)(C[C@@H](O)[C@]14C3=CC[C@H]3[C@]4(C)CC[C@](O1)(O)C3)C(=CC2)[C@@H](OC(=O)c1c(C)c[nH]c1C)C,"InChI=1S/C31H42N2O6/c1-18-16-32-19(2)25(18)26(35)38-20(3)22-8-9-30-23-7-6-21-14-29(36)11-10-27(21,4)31(23,39-29)24(34)15-28(22,30)17-33(5)12-13-37-30/h7-8,16,20-21,24,32,34,36H,6,9-15,17H2,1-5H3/t20-,21+,24+,27-,28-,29+,30-,31-/m0/s1",ISNYUQWBWALXEY-OMIQOYQYSA-N,Activator,Full agonist,,,,,pKd,,7.6,,Kd,,25.1,,=,,,,2431264, Nav1.5,582,P15389,Rat,lidocaine,2623,,3676,CCN(CC(=O)Nc1c(C)cccc1C)CC,"InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)",NNJVILVZKWQKPM-UHFFFAOYSA-N,Channel blocker,Pore blocker,,,,,pIC50,,4.2,,,,,,=,,,,2546048, Nav1.5,582,Q14524,Human,lidocaine,2623,,3676,CCN(CC(=O)Nc1c(C)cccc1C)CC,"InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)",NNJVILVZKWQKPM-UHFFFAOYSA-N,Channel blocker,Pore blocker,,,yes,,pKd,,4.8,,,,,,=,,,,8786356, Nav1.5,582,P15389,Rat,saxitoxin,2625,,56947150,NC(=O)OC[C@@H]1N=C(N)N2[C@@]3([C@H]1NC(=N3)N)C(O)(O)CC2,"InChI=1S/C10H17N7O4/c11-6-15-5-4(3-21-8(13)18)14-7(12)17-2-1-9(19,20)10(5,17)16-6/h4-5,19-20H,1-3H2,(H2,12,14)(H2,13,18)(H3,11,15,16)/t4-,5-,10-/m0/s1",RPQXVSUAYFXFJA-HGRQIUPRSA-N,Channel blocker,Pore blocker,,,,,pKd,,7.4,,,,,,=,,,,8967455|2175715, Nav1.5,582,P15389,Rat,veratridine,2626,,6280,COc1ccc(cc1OC)C(=O)O[C@H]1CC[C@]2([C@H]3[C@]1(O)O[C@]12C[C@@]2([C@@]([C@@H]1CC3)(O)C[C@@H]([C@]1([C@H]2CN2C[C@@H](C)CC[C@H]2[C@@]1(C)O)O)O)O)C,"InChI=1S/C36H51NO11/c1-19-6-11-26-31(3,40)35(43)25(17-37(26)16-19)33(42)18-34-24(32(33,41)15-27(35)38)10-9-23-30(34,2)13-12-28(36(23,44)48-34)47-29(39)20-7-8-21(45-4)22(14-20)46-5/h7-8,14,19,23-28,38,40-44H,6,9-13,15-18H2,1-5H3/t19-,23-,24-,25-,26-,27-,28-,30-,31+,32+,33+,34+,35-,36-/m0/s1",FVECELJHCSPHKY-YFUMOZOISA-N,Activator,Partial agonist,,,,,pEC50,,6.3,,EC50,,501.0,,=,,,,2154667, Nav1.5,582,P15389,Rat,μ-conotoxin SmIIIA,7567,,,,,,Channel blocker,Pore blocker,,,,,pKi,,5.5,,,,,,=,Two-microelectrode of Xenopus oocytes expression rat Nav1.5.,,,21652775, Nav1.5,582,Q14524,Human,protoxin II,7571,,,,,,Gating inhibitor,Voltage-dependent inhibition,,,,,pKi,,6.5,,,,,,=,Whole-cell voltage clamp of human Nav1.5 channels expressed in human embryonic kidney cells (HEK293).,,,12475222, Nav1.5,582,Q14524,Human,ropivacaine,7602,,175805,CCCN1CCCC[C@H]1C(=O)Nc1c(C)cccc1C,"InChI=1S/C17H26N2O/c1-4-11-19-12-6-5-10-15(19)17(20)18-16-13(2)8-7-9-14(16)3/h7-9,15H,4-6,10-12H2,1-3H3,(H,18,20)/t15-/m0/s1",ZKMNUMMKYBVTFN-HNNXBMFYSA-N,Channel blocker,Pore blocker,Blockade of inactivated channel,,,,pIC50,,4.56,,IC50,,27300.0,,=,,,,25692452, Nav1.5,582,Q14524,Human,ropivacaine,7602,,175805,CCCN1CCCC[C@H]1C(=O)Nc1c(C)cccc1C,"InChI=1S/C17H26N2O/c1-4-11-19-12-6-5-10-15(19)17(20)18-16-13(2)8-7-9-14(16)3/h7-9,15H,4-6,10-12H2,1-3H3,(H,18,20)/t15-/m0/s1",ZKMNUMMKYBVTFN-HNNXBMFYSA-N,Channel blocker,Pore blocker,Open-channel block,,,,pIC50,,3.49,,IC50,,322200.0,,=,,,,25692452, Nav1.5,582,Q14524,Human,eleclazine,8413,,71183216,O=C1N(CCOc2c1cc(cc2)c1ccc(cc1)OC(F)(F)F)Cc1ncccn1,"InChI=1S/C21H16F3N3O3/c22-21(23,24)30-16-5-2-14(3-6-16)15-4-7-18-17(12-15)20(28)27(10-11-29-18)13-19-25-8-1-9-26-19/h1-9,12H,10-11,13H2",YNUAEEJQYHYLMS-UHFFFAOYSA-N,Inhibitor,Inhibition,,,yes,,,,,,,,,,=,,,,, Nav1.5,582,Q14524,Human,GS-458967,9858,,58118983,FC(Oc1ccc(cc1)c1ccc2n(c1)c(nn2)C(F)(F)F)(F)F,"InChI=1S/C14H7F6N3O/c15-13(16,17)12-22-21-11-6-3-9(7-23(11)12)8-1-4-10(5-2-8)24-14(18,19)20/h1-7H",FEVBKJITJDHASC-UHFFFAOYSA-N,Inhibitor,Inhibition,,,,,pIC50,,6.89,,IC50,,130.0,,=,,,,27080178|29582428, Nav1.5,582,Q14524,Human,GNE-131,10003,,91666633,O=S(=O)(C1CC1)Nc1nnc2n1cc(C1CC1)c(c2)OCC12CC3CC(C2)CC(C1)C3,"InChI=1S/C23H30N4O3S/c28-31(29,18-3-4-18)26-22-25-24-21-8-20(19(12-27(21)22)17-1-2-17)30-13-23-9-14-5-15(10-23)7-16(6-14)11-23/h8,12,14-18H,1-7,9-11,13H2,(H,25,26)",FPERPEQIXLOVIK-UHFFFAOYSA-N,Inhibitor,Inhibition,,,,,pIC50,,6.96,,IC50,,110.0,,=,"IC50s were generated on a PatchXpress automated voltage-clamp platform, with the membrane potential maintained at a voltage yielding full inactivation of the channel.",,,29737846, Nav1.5,582,Q14524,Human,AM-6120,10119,,,,,,Inhibitor,Inhibition,,,,,pIC50,,5.18,,IC50,,6640.0,,=,Determined in a PatchXpress electrophysiology experiment using HEK293 cells stably expressing hNaV1.5.,,,30346167, Nav1.5,582,Q14524,Human,GNE-616,10355,,138393286,Fc1cc2c(cc1S(=O)(=O)Nc1ccncn1)OCC[C@@H]2N1CC[C@@H](C[C@@H]1c1ccccn1)C(F)(F)F,"InChI=1S/C24H23F4N5O3S/c25-17-12-16-19(33-9-5-15(24(26,27)28)11-20(33)18-3-1-2-7-30-18)6-10-36-21(16)13-22(17)37(34,35)32-23-4-8-29-14-31-23/h1-4,7-8,12-15,19-20H,5-6,9-11H2,(H,29,31,32)/t15-,19-,20+/m0/s1",XQUOWYVEKSXNET-RYGJVYDSSA-N,Channel blocker,Inhibition,,,,,pKd,,6.0,,Kd,,1000.0,,>,Kd determined in a Dynaflow Manual Patch Clamp experiment.,,,30943032, Nav1.5,582,Q14524,Human,relutrigine,12643,,147075611,CCOC(C1=NN=C2N1C=C(N=C2)C3=CC(=C(N=C3)OCC(F)(F)F)F)(F)F,"InChI=1S/C15H11F6N5O2/c1-2-28-15(20,21)13-25-24-11-5-22-10(6-26(11)13)8-3-9(16)12(23-4-8)27-7-14(17,18)19/h3-6H,2,7H2,1H3",BFXBSYMVTNEFRF-UHFFFAOYSA-N,Inhibitor,Inhibition,,,,,pIC50,,6.76,,IC50,,172.0,,=,,,,35037706, Nav1.5,582,Q14524,Human,funapide,12644,,49836093,C1[C@]2(C3=CC=CC=C3N(C2=O)CC4=CC=C(O4)C(F)(F)F)C5=CC6=C(C=C5O1)OCO6,"InChI=1S/C22H14F3NO5/c23-22(24,25)19-6-5-12(31-19)9-26-15-4-2-1-3-13(15)21(20(26)27)10-28-16-8-18-17(7-14(16)21)29-11-30-18/h1-8H,9-11H2/t21-/m0/s1",NEBUOXBYNAHKFV-NRFANRHFSA-N,Inhibitor,Inhibition,,,,,pIC50,,7.08,,IC50,,84.0,,=,Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay,,,31012583,