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 GABAA receptor α4 subunit,407,P48169,Human,Zn2+,566,,32051,,,,Allosteric modulator,Inhibition,,yes,,,,,,,,,,,=,,,,, GABAA receptor α4 subunit,407,P48169,Human,bicuculline,2312,,10237,CN1CCc2c([C@H]1[C@@H]1OC(=O)c3c1ccc1c3OCO1)cc1c(c2)OCO1,"InChI=1S/C20H17NO6/c1-21-5-4-10-6-14-15(25-8-24-14)7-12(10)17(21)18-11-2-3-13-19(26-9-23-13)16(11)20(22)27-18/h2-3,6-7,17-18H,4-5,8-9H2,1H3/t17-,18+/m0/s1",IYGYMKDQCDOMRE-ZWKOTPCHSA-N,Antagonist,Antagonist,,,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,picrotoxin,4051,,31304,CC(=C)[C@@H]1C2OC(=O)C1[C@]1([C@]3([C@@H]2OC(=O)[C@]23C(C1)O2)C)O.O=C1OC2[C@H](C1[C@]1(O)C[C@@H]3[C@]4([C@@]1([C@@H]2OC4=O)C)O3)C(O)(C)C,"InChI=1S/C15H18O7.C15H16O6/c1-12(2,18)6-7-10(16)20-8(6)9-13(3)14(7,19)4-5-15(13,22-5)11(17)21-9;1-5(2)7-8-11(16)19-9(7)10-13(3)14(8,18)4-6-15(13,21-6)12(17)20-10/h5-9,18-19H,4H2,1-3H3;6-10,18H,1,4H2,2-3H3/t5-,6+,7?,8?,9-,13-,14-,15+;6?,7-,8?,9?,10+,13+,14+,15-/m10/s1",VJKUPQSHOVKBCO-ZTYBEOBUSA-N,Channel blocker,None,,,,,,,,,,,,,=,,,,, GABAA receptor α4 subunit,407,P48169,Human,[3H]gabazine,4083,,107896,COc1ccc(cc1)c1ccc(=N)n(n1)CCCC(=O)O,"InChI=1S/C15H17N3O3/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20/h4-9,16H,2-3,10H2,1H3,(H,19,20)",ACVGNKYJVGNLIL-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,[3H]muscimol,4090,,4266,NCc1cc(=O)[nH]o1,"InChI=1S/C4H6N2O2/c5-2-3-1-4(7)6-8-3/h1H,2,5H2,(H,6,7)",ZJQHPWUVQPJPQT-UHFFFAOYSA-N,Agonist,Full agonist,,,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,5α-pregnan-3α-ol-20-one,4108,,92786,O[C@@H]1CC[C@]2([C@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2C(=O)C)C)C,"InChI=1S/C21H34O2/c1-13(22)17-6-7-18-16-5-4-14-12-15(23)8-10-20(14,2)19(16)9-11-21(17,18)3/h14-19,23H,4-12H2,1-3H3/t14-,15+,16-,17+,18-,19-,20-,21+/m0/s1",AURFZBICLPNKBZ-SYBPFIFISA-N,Allosteric modulator,Potentiation,,yes,,,,,,,,,,,=,,,,, GABAA receptor α4 subunit,407,P48169,Human,bretazenil,4146,,107926,O=C(c1ncn2c1[C@@H]1CCCN1C(=O)c1c2cccc1Br)OC(C)(C)C,"InChI=1S/C19H20BrN3O3/c1-19(2,3)26-18(25)15-16-13-8-5-9-22(13)17(24)14-11(20)6-4-7-12(14)23(16)10-21-15/h4,6-7,10,13H,5,8-9H2,1-3H3/t13-/m0/s1",LWUDDYHYYNNIQI-ZDUSSCGKSA-N,Allosteric modulator,Full agonist,,,,,,,,,,,,,=,,benzodiazepine site,,20303942, GABAA receptor α4 subunit,407,P28471,Rat,flumazenil,4192,,3373,CCOC(=O)c1ncn2c1CN(C)C(=O)c1c2ccc(c1)F,"InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3",OFBIFZUFASYYRE-UHFFFAOYSA-N,Allosteric modulator,Positive,"Antagonist at α1 receptors, but allosteric modulator at other subtypes.",,,,pKi,,7.03,,Ki,,94.0,,=,Antagonism of complexes containing α4β2γ2 subunits heterologously expressed in vitro.,,,7799410, GABAA receptor α4 subunit,407,P48169,Human,gabazine,4197,,107896,COc1ccc(cc1)c1ccc(=N)n(n1)CCCC(=O)O,"InChI=1S/C15H17N3O3/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20/h4-9,16H,2-3,10H2,1H3,(H,19,20)",ACVGNKYJVGNLIL-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,isoguvacine,4226,,3765,OC(=O)C1=CCNCC1,"InChI=1S/C6H9NO2/c8-6(9)5-1-3-7-4-2-5/h1,7H,2-4H2,(H,8,9)",KRVDMABBKYMBHG-UHFFFAOYSA-N,Agonist,Full agonist,,,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,isonipecotic acid,4227,,3773,OC(=O)C1CCNCC1,"InChI=1S/C6H11NO2/c8-6(9)5-1-3-7-4-2-5/h5,7H,1-4H2,(H,8,9)",SRJOCJYGOFTFLH-UHFFFAOYSA-N,Agonist,Full agonist,"relatively high efficacy, partially selective",,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,muscimol,4259,,4266,NCc1cc(=O)[nH]o1,"InChI=1S/C4H6N2O2/c5-2-3-1-4(7)6-8-3/h1H,2,5H2,(H,6,7)",ZJQHPWUVQPJPQT-UHFFFAOYSA-N,Agonist,Full agonist,,,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,piperidine-4-sulphonic acid,4287,,4838,OS(=O)(=O)C1CCNCC1,"InChI=1S/C5H11NO3S/c7-10(8,9)5-1-3-6-4-2-5/h5-6H,1-4H2,(H,7,8,9)",UGBJGGRINDTHIH-UHFFFAOYSA-N,Agonist,Full agonist,low efficacy,,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,Ro15-4513,4296,,5081,CCOC(=O)c1ncn2c1CN(C)C(=O)c1c2ccc(c1)N=[N+]=[N-],"InChI=1S/C15H14N6O3/c1-3-24-15(23)13-12-7-20(2)14(22)10-6-9(18-19-16)4-5-11(10)21(12)8-17-13/h4-6,8H,3,7H2,1-2H3",CFSOJZTUTOQNIA-UHFFFAOYSA-N,Allosteric modulator,Full agonist,,,,,,,,,,,,,=,,benzodiazepine site,,, GABAA receptor α4 subunit,407,P48169,Human,TBPS,4320,,104781,CC(C12COP(=S)(OC1)OC2)(C)C,"InChI=1S/C8H15O3PS/c1-7(2,3)8-4-9-12(13,10-5-8)11-6-8/h4-6H2,1-3H3",VTBHBNXGFPTBJL-UHFFFAOYSA-N,Channel blocker,None,,,,,,,,,,,,,=,,,,, GABAA receptor α4 subunit,407,P48169,Human,tetrahydrodeoxycorticosterone,4321,,101771,OCC(=O)[C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)CC[C@H](C2)O,"InChI=1S/C21H34O3/c1-20-9-7-14(23)11-13(20)3-4-15-16-5-6-18(19(24)12-22)21(16,2)10-8-17(15)20/h13-18,22-23H,3-12H2,1-2H3/t13-,14+,15-,16-,17-,18+,20-,21-/m0/s1",CYKYBWRSLLXBOW-GDYGHMJCSA-N,Allosteric modulator,Potentiation,,yes,,,,,,,,,,,=,,,,, GABAA receptor α4 subunit,407,P48169,Human,gaboxadol,4322,,3448,O=c1[nH]oc2c1CCNC2,"InChI=1S/C6H8N2O2/c9-6-4-1-2-7-3-5(4)10-8-6/h7H,1-3H2,(H,8,9)",ZXRVKCBLGJOCEE-UHFFFAOYSA-N,Agonist,Agonist,,,,,,,,,,,,,=,,GABA site,,, GABAA receptor α4 subunit,407,P48169,Human,[3H]Ro154513,4365,,5081,CCOC(=O)c1ncn2c1CN(C)C(=O)c1c2ccc(c1)N=[N+]=[N-],"InChI=1S/C15H14N6O3/c1-3-24-15(23)13-12-7-20(2)14(22)10-6-9(18-19-16)4-5-11(10)21(12)8-17-13/h4-6,8H,3,7H2,1-2H3",CFSOJZTUTOQNIA-UHFFFAOYSA-N,Allosteric modulator,Full agonist,,,,,,,,,,,,,=,,benzodiazepine site,,, GABAA receptor α4 subunit,407,P48169,Human,[3H]CGS8216,4366,,104916,O=c1n([nH]c2c1cnc1c2cccc1)c1ccccc1,"InChI=1S/C16H11N3O/c20-16-13-10-17-14-9-5-4-8-12(14)15(13)18-19(16)11-6-2-1-3-7-11/h1-10,18H",XTYGFVVANLMBHE-UHFFFAOYSA-N,Allosteric modulator,Mixed,agonist and antagonist,,,,,,,,,,,,=,,benzodiazepine site,,, GABAA receptor α4 subunit,407,P48169,Human,[11C]flumazenil,4367,,3373,CCOC(=O)c1ncn2c1CN(C)C(=O)c1c2ccc(c1)F,"InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3",OFBIFZUFASYYRE-UHFFFAOYSA-N,Allosteric modulator,Partial agonist,low affinity,,,,,,,,,,,,=,,benzodiazepine site,,, GABAA receptor α4 subunit,407,P48169,Human,[18F]fluoroethylflumazenil,4368,,126761,[18F]CCN1Cc2c(ncn2c2c(C1=O)cc(F)cc2)C(=O)OCC,"InChI=1S/C16H15F2N3O3/c1-2-24-16(23)14-13-8-20(6-5-17)15(22)11-7-10(18)3-4-12(11)21(13)9-19-14/h3-4,7,9H,2,5-6,8H2,1H3/i17-1",NRBIGDVWCXXFLI-SJPDSGJFSA-N,Allosteric modulator,None,,,,,,,,,,,,,=,,benzodiazepine site,,, GABAA receptor α4 subunit,407,P48169,Human,[35S]TBPS,4369,,59896759,CC(C12COP(=[35S])(OC1)OC2)(C)C,"InChI=1S/C8H15O3PS/c1-7(2,3)8-4-9-12(13,10-5-8)11-6-8/h4-6H2,1-3H3/i13+3",VTBHBNXGFPTBJL-DLSVHHIMSA-N,Channel blocker,None,,,,,,,,,,,,,=,,anion channel,,, GABAA receptor α4 subunit,407,P48169,Human,cenobamate,10773,,11962412,NC(=O)O[C@H](c1ccccc1Cl)Cn1nncn1,"InChI=1S/C10H10ClN5O2/c11-8-4-2-1-3-7(8)9(18-10(12)17)5-16-14-6-13-15-16/h1-4,6,9H,5H2,(H2,12,17)/t9-/m0/s1",GFHAXPJGXSQLPT-VIFPVBQESA-N,Allosteric modulator,Positive,,,,,pEC50,,4.38,,EC50,,42000.0,,=,Allosteric modulation of GABA-activated human α4β3γ2 GABAA channels expressed in HEK cells.,,,32325146,