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 RyR2,748,Q92736,Human,caffeine,407,,2519,Cn1cnc2c1c(=O)n(C)c(=O)n2C,"InChI=1S/C8H10N4O2/c1-10-4-9-6-5(10)7(13)12(3)8(14)11(6)2/h4H,1-3H3",RYYVLZVUVIJVGH-UHFFFAOYSA-N,Activator,None,pharmacological; mM range,,,,,,,,,,,,,,,,, RyR2,748,Q92736,Human,carvedilol,551,,2585,COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O,"InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3",OGHNVEJMJSYVRP-UHFFFAOYSA-N,Inhibitor,Inhibition,,,,,pIC50,,4.8,,IC50,,15900.0,,=,Inhibition of R4496C mutant RyR2 (expressed in HEK293 cells)-mediated store-overload induced calcium release after 8 to 10 mins using a fura-2/AM dye-based fluorescence assay.,,,24124794, RyR2,748,Q92736,Human,Ca2+,707,,,,,,Activator,None,endogenous; μM range,yes,,,,,,,,,,,,,,cytosolic,, RyR2,748,Q92736,Human,Ca2+,707,,,,,,Antagonist,Antagonist,,yes,,>1000,,,,,,,,,,,,cytosolic,, RyR2,748,Q92736,Human,Ca2+,707,,,,,,Activator,None,endogenous,yes,,,,,,,,,,,,,,luminal,, RyR2,748,Q92736,Human,Mg2+,708,,888,,,,Antagonist,Antagonist,mM range,yes,,,,,,,,,,,,,,cytosolic,, RyR2,748,Q92736,Human,ATP,1713,,5957,O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N,"InChI=1S/C10H16N5O13P3/c11-8-5-9(13-2-12-8)15(3-14-5)10-7(17)6(16)4(26-10)1-25-30(21,22)28-31(23,24)27-29(18,19)20/h2-4,6-7,10,16-17H,1H2,(H,21,22)(H,23,24)(H2,11,12,13)(H2,18,19,20)/t4-,6-,7-,10-/m1/s1",ZKHQWZAMYRWXGA-KQYNXXCUSA-N,Activator,None,endogenous; mM range,yes,,,,,,,,,,,,,,cytosolic,, RyR2,748,Q92736,Human,suramin,1728,,5361,O=C(Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)Nc1cccc(c1)C(=O)Nc1cc(ccc1C)C(=O)Nc1ccc(c2c1c(cc(c2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O,"InChI=1S/C51H40N6O23S6/c1-25-9-11-29(49(60)54-37-13-15-41(83(69,70)71)35-21-33(81(63,64)65)23-43(45(35)37)85(75,76)77)19-39(25)56-47(58)27-5-3-7-31(17-27)52-51(62)53-32-8-4-6-28(18-32)48(59)57-40-20-30(12-10-26(40)2)50(61)55-38-14-16-42(84(72,73)74)36-22-34(82(66,67)68)24-44(46(36)38)86(78,79)80/h3-24H,1-2H3,(H,54,60)(H,55,61)(H,56,58)(H,57,59)(H2,52,53,62)(H,63,64,65)(H,66,67,68)(H,69,70,71)(H,72,73,74)(H,75,76,77)(H,78,79,80)",FIAFUQMPZJWCLV-UHFFFAOYSA-N,Activator,None,pharmacological; μM range,,,,,,,,,,,,,,,,, RyR2,748,Q92736,Human,ruthenium red,2432,,656819,,,,Channel blocker,None,,,,,,,,,,,,,,,,,, RyR2,748,Q92736,Human,procaine,4291,,4914,CCN(CCOC(=O)c1ccc(cc1)N)CC,"InChI=1S/C13H20N2O2/c1-3-15(4-2)9-10-17-13(16)11-5-7-12(14)8-6-11/h5-8H,3-4,9-10,14H2,1-2H3",MFDFERRIHVXMIY-UHFFFAOYSA-N,Channel blocker,None,,,,,,,,,,,,,,,,,, RyR2,748,Q92736,Human,ryanodine,4303,,11317883,C[C@H]1CC[C@]2([C@@]3([C@@H]1O)O[C@@]1([C@]4([C@@]3(O)[C@@]([C@@]2(C)C1)(O)[C@@H]([C@]4(O)C(C)C)OC(=O)c1[nH]ccc1)C)O)O,"InChI=1S/C25H35NO9/c1-12(2)22(31)17(34-16(28)14-7-6-10-26-14)23(32)18(4)11-21(30)19(22,5)25(23,33)24(35-21)15(27)13(3)8-9-20(18,24)29/h6-7,10,12-13,15,17,26-27,29-33H,8-9,11H2,1-5H3/t13-,15+,17+,18-,19+,20-,21-,22+,23+,24+,25+/m0/s1",JJSYXNQGLHBRRK-SFEDZAPPSA-N,Activator,None,pharmacological; nM - μM range,,,,,,,,,,,,,,,,, RyR2,748,Q92736,Human,ryanodine,4303,,11317883,C[C@H]1CC[C@]2([C@@]3([C@@H]1O)O[C@@]1([C@]4([C@@]3(O)[C@@]([C@@]2(C)C1)(O)[C@@H]([C@]4(O)C(C)C)OC(=O)c1[nH]ccc1)C)O)O,"InChI=1S/C25H35NO9/c1-12(2)22(31)17(34-16(28)14-7-6-10-26-14)23(32)18(4)11-21(30)19(22,5)25(23,33)24(35-21)15(27)13(3)8-9-20(18,24)29/h6-7,10,12-13,15,17,26-27,29-33H,8-9,11H2,1-5H3/t13-,15+,17+,18-,19+,20-,21-,22+,23+,24+,25+/m0/s1",JJSYXNQGLHBRRK-SFEDZAPPSA-N,Channel blocker,None,,,,>100,,,,,,,,,,,,,, RyR2,748,Q92736,Human,VK-II-86,10161,,71158523,COc1ccccc1OCCNCC(CCOc1cccc2c1c1ccccc1[nH]2)O,"InChI=1S/C25H28N2O4/c1-29-22-10-4-5-11-23(22)31-16-14-26-17-18(28)13-15-30-24-12-6-9-21-25(24)19-7-2-3-8-20(19)27-21/h2-12,18,26-28H,13-17H2,1H3",OHYHNEODRHJYSS-UHFFFAOYSA-N,Inhibitor,Inhibition,,,,,pIC50,,4.77,,IC50,,16800.0,,=,Inhibition of R4496C mutant RyR2 (expressed in HEK293 cells)-mediated store-overload induced calcium release after 8 to 10 mins using a fura-2/AM dye-based fluorescence assay.,,,24124794,