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 Nav1.2,579,Q99250,Human,AFT-II,2613,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pEC50,,5.7,,,,,,=,,,,15169781, Nav1.2,579,Q99250,Human,ATX-II,2614,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pEC50,,8.1,,,,,,=,,,,15169781, Nav1.2,579,Q99250,Human,Bc-III,2615,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pEC50,,5.8,,,,,,=,,,,15169781, Nav1.2,579,P04775,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,,,,,pIC50,,8.0,,IC50,,11.2,,=,,,,15815630, Nav1.2,579,P04775,Rat,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,,,,,pKd,,5.9,,,,,,=,,,,6114956, Nav1.2,579,P04775,Rat,α-scorpion toxin 2,2618,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pEC50,,9.1,,,,,,=,,,,14978247, Nav1.2,579,P04775,Rat,α-scorpion toxin 2,2618,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pKd,,8.7,,,,,,=,,,,8663157, Nav1.2,579,P04775,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,Agonist,,,,,pKd,,9.1,,Kd,,0.794,,=,,,,9811906, Nav1.2,579,P04775,Rat,β-scorpion toxin Css IV,2620,,,,,,Activator,Partial agonist,,,,,pKd,,9.7,,,,,,,,,,9808476, Nav1.2,579,P04775,Rat,etidocaine,2621,,37497,CCCN(C(C(=O)Nc1c(C)cccc1C)CC)CC,"InChI=1S/C17H28N2O/c1-6-12-19(8-3)15(7-2)17(20)18-16-13(4)10-9-11-14(16)5/h9-11,15H,6-8,12H2,1-5H3,(H,18,20)",VTUSIVBDOCDNHS-UHFFFAOYSA-N,Channel blocker,Pore blocker,,,,,pIC50,,6.0,,,,,,=,,,,8085162, Nav1.2,579,P04775,Rat,lamotrigine,2622,,3878,Nc1nnc(c(n1)N)c1cccc(c1Cl)Cl,"InChI=1S/C9H7Cl2N5/c10-5-3-1-2-4(6(5)11)7-8(12)14-9(13)16-15-7/h1-3H,(H4,12,13,14,16)",PYZRQGJRPPTADH-UHFFFAOYSA-N,Channel blocker,Pore blocker,,,,,pIC50,,4.5,,,,,,=,,,,12604088|7491269, Nav1.2,579,P04775,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,,5.0,,,,,,=,,,,8799190, Nav1.2,579,Q99250,Human,phenytoin,2624,,1775,O=C1NC(=O)NC1(c1ccccc1)c1ccccc1,"InChI=1S/C15H12N2O2/c18-13-15(17-14(19)16-13,11-7-3-1-4-8-11)12-9-5-2-6-10-12/h1-10H,(H2,16,17,18,19)",CXOFVDLJLONNDW-UHFFFAOYSA-N,Channel blocker,Pore blocker,,,yes,,pIC50,,4.9,,,,,,=,,,,1658608, Nav1.2,579,P04775,Rat,phenytoin,2624,,1775,O=C1NC(=O)NC1(c1ccccc1)c1ccccc1,"InChI=1S/C15H12N2O2/c18-13-15(17-14(19)16-13,11-7-3-1-4-8-11)12-9-5-2-6-10-12/h1-10H,(H2,16,17,18,19)",CXOFVDLJLONNDW-UHFFFAOYSA-N,Channel blocker,Pore blocker,,,,,pIC50,,4.7,,,,,,=,,,,8799190, Nav1.2,579,P04775,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,,,,,pIC50,,8.8,,IC50,,1.7,,=,,,,15815630, Nav1.2,579,P04775,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,,,,,pKd,,5.2,,Kd,,6310.0,,=,,,,6114956, Nav1.2,579,P04775,Rat,lacosamide,7472,,219078,COC[C@H](C(=O)NCc1ccccc1)NC(=O)C,"InChI=1S/C13H18N2O3/c1-10(16)15-12(9-18-2)13(17)14-8-11-6-4-3-5-7-11/h3-7,12H,8-9H2,1-2H3,(H,14,17)(H,15,16)/t12-/m1/s1",VPPJLAIAVCUEMN-GFCCVEGCSA-N,Channel blocker,Antagonist,,,,,pIC50,,4.52,,IC50,,30000.0,,=,,,,24065921, Nav1.2,579,P04775,Rat,μ-conotoxin SmIIIA,7567,,,,,,Channel blocker,Pore blocker,,,,,pKd,,8.9,,,,,,=,,,,21652775, Nav1.2,579,P04775,Rat,δ-hexatoxin-Mg1a,7569,,,,,,Gating inhibitor,Slows inactivation,Inhibitor of fast activation,,,,pEC50,,4.5,,EC50,,,,=,,,,19592486, Nav1.2,579,Q99250,Human,huwentoxin IV,7570,,,,,,Gating inhibitor,Voltage-dependent inhibition,,,,,pKd,,7.8,,,,,,=,Automated patch clamp (QPatch) of transfected human embryonic kidney cells (HEK293),,,23760503, Nav1.2,579,Q99250,Human,protoxin II,7571,,,,,,Gating inhibitor,Voltage-dependent inhibition,,,,,pKi,,7.4,,,,,,=,Whole cell voltage clamp of transfected human embryonic kidney cells (HEK293),,,18728100, Nav1.2,579,Q99250,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,,8.15,,IC50,,7.0,,=,"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, Nav1.2,579,Q99250,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,,7.92,,Kd,,12.0,,=,Kd determined in a Dynaflow Manual Patch Clamp experiment.,,,30943032, Nav1.2,579,Q99250,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, Nav1.2,579,Q99250,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,,6.22,,IC50,,600.0,,=,Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay,,,31012583,