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 β1-adrenoceptor,28,P08588,Human,(-)-propranolol,63,,91536,O[C@H](COc1cccc2c1cccc2)CNC(C)C,"InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3/t14-/m0/s1",AQHHHDLHHXJYJD-AWEZNQCLSA-N,Antagonist,Antagonist,,,yes,,pKi,8.9,,7.9,,,,,=,,,,15060759|10079020|15655528|27588207, β1-adrenoceptor,28,P08588,Human,pindolol,91,,4828,OC(COc1cccc2c1cc[nH]2)CNC(C)C,"InChI=1S/C14H20N2O2/c1-10(2)16-8-11(17)9-18-14-5-3-4-13-12(14)6-7-15-13/h3-7,10-11,15-17H,8-9H2,1-2H3",JZQKKSLKJUAGIC-UHFFFAOYSA-N,Agonist,Partial agonist,,,yes,,pKi,9.3,,8.6,,,,,=,,,,20590599|17804228, β1-adrenoceptor,28,P08588,Human,pindolol,91,,4828,OC(COc1cccc2c1cc[nH]2)CNC(C)C,"InChI=1S/C14H20N2O2/c1-10(2)16-8-11(17)9-18-14-5-3-4-13-12(14)6-7-15-13/h3-7,10-11,15-17H,8-9H2,1-2H3",JZQKKSLKJUAGIC-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,9.7,,8.6,,,,,=,,,,15060759|14645666|20590599, β1-adrenoceptor,28,P08588,Human,cyanopindolol,132,,155346,N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2,"InChI=1S/C16H21N3O2/c1-16(2,3)18-9-12(20)10-21-15-6-4-5-14-13(15)7-11(8-17)19-14/h4-7,12,18-20H,9-10H2,1-3H3",QXIUMMLTJVHILT-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKd,10.5,,10.4,,,,,=,,,,20590599|26385885, β1-adrenoceptor,28,P08588,Human,(-)-adrenaline,479,,5816,CNC[C@@H](c1ccc(c(c1)O)O)O,"InChI=1S/C9H13NO3/c1-10-5-9(13)6-2-3-7(11)8(12)4-6/h2-4,9-13H,5H2,1H3/t9-/m0/s1",UCTWMZQNUQWSLP-VIFPVBQESA-N,Agonist,Agonist,,,,,pEC50,,7.6,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,(-)-adrenaline,479,,5816,CNC[C@@H](c1ccc(c(c1)O)O)O,"InChI=1S/C9H13NO3/c1-10-5-9(13)6-2-3-7(11)8(12)4-6/h2-4,9-13H,5H2,1H3/t9-/m0/s1",UCTWMZQNUQWSLP-VIFPVBQESA-N,Agonist,Agonist,,yes,,,pKi,6.0,,5.2,,,,,=,,,,2849109|14730417|20590599, β1-adrenoceptor,28,P08588,Human,noradrenaline,484,,951,NCC(c1ccc(c(c1)O)O)O,"InChI=1S/C8H11NO3/c9-4-8(12)5-1-2-6(10)7(11)3-5/h1-3,8,10-12H,4,9H2",SFLSHLFXELFNJZ-UHFFFAOYSA-N,Agonist,Full agonist,,yes,,,pKi,,6.0,,,,,,=,,,,2849109, β1-adrenoceptor,28,P08588,Human,(-)-noradrenaline,505,,439260,NC[C@@H](c1ccc(c(c1)O)O)O,"InChI=1S/C8H11NO3/c9-4-8(12)5-1-2-6(10)7(11)3-5/h1-3,8,10-12H,4,9H2/t8-/m0/s1",SFLSHLFXELFNJZ-QMMMGPOBSA-N,Agonist,Agonist,,,,,pEC50,,7.9,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,(-)-noradrenaline,505,,439260,NC[C@@H](c1ccc(c(c1)O)O)O,"InChI=1S/C8H11NO3/c9-4-8(12)5-1-2-6(10)7(11)3-5/h1-3,8,10-12H,4,9H2/t8-/m0/s1",SFLSHLFXELFNJZ-QMMMGPOBSA-N,Agonist,Agonist,,yes,,,pKi,6.0,,5.5,,,,,=,,,,2849109|14730417|20590599, β1-adrenoceptor,28,P08588,Human,(±)-adrenaline,509,,838,CNCC(c1ccc(c(c1)O)O)O,"InChI=1S/C9H13NO3/c1-10-5-9(13)6-2-3-7(11)8(12)4-6/h2-4,9-13H,5H2,1H3",UCTWMZQNUQWSLP-UHFFFAOYSA-N,Agonist,Full agonist,,,,,pKi,,6.0,,,,,,=,,,,2849109, β1-adrenoceptor,28,P08588,Human,[3H](-)CGP 12177,531,,6603756,O[C@H](COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C,"InChI=1S/C14H21N3O3/c1-14(2,3)15-7-9(18)8-20-11-6-4-5-10-12(11)17-13(19)16-10/h4-6,9,15,18H,7-8H2,1-3H3,(H2,16,17,19)/t9-/m0/s1",UMQUQWCJKFOUGV-VIFPVBQESA-N,Agonist,Partial agonist,,,,,pKd,9.9,,6.6,,,,,=,,,,15060759|15655528|20590599, β1-adrenoceptor,28,P08588,Human,[3H](-)CGP 12177,531,,6603756,O[C@H](COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C,"InChI=1S/C14H21N3O3/c1-14(2,3)15-7-9(18)8-20-11-6-4-5-10-12(11)17-13(19)16-10/h4-6,9,15,18H,7-8H2,1-3H3,(H2,16,17,19)/t9-/m0/s1",UMQUQWCJKFOUGV-VIFPVBQESA-N,Antagonist,Antagonist,3H-CGP12177 (high affinity non-selective antagonist of orthosteric site) is excellent for membrane and whole cell binding with little non-specific binding.,,,,pKd,9.4,,9.2,,,,,=,,,,15060759|15655528|20590599, β1-adrenoceptor,28,P08588,Human,CGP 12177,532,,2687,OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C,"InChI=1S/C14H21N3O3/c1-14(2,3)15-7-9(18)8-20-11-6-4-5-10-12(11)17-13(19)16-10/h4-6,9,15,18H,7-8H2,1-3H3,(H2,16,17,19)",UMQUQWCJKFOUGV-UHFFFAOYSA-N,Agonist,Partial agonist,,,,,pKi,,9.4,,,,,,=,,,,10079020|15655528|20590599, β1-adrenoceptor,28,P08588,Human,CGP 12177,532,,2687,OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C,"InChI=1S/C14H21N3O3/c1-14(2,3)15-7-9(18)8-20-11-6-4-5-10-12(11)17-13(19)16-10/h4-6,9,15,18H,7-8H2,1-3H3,(H2,16,17,19)",UMQUQWCJKFOUGV-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,9.3,,8.8,,,,,=,,,,15060759|15655528|27588207, β1-adrenoceptor,28,P08588,Human,T-0509,533,,173382,COc1cc(CCNCC(c2ccc(c(c2)O)O)O)ccc1OC,"InChI=1S/C18H23NO5/c1-23-17-6-3-12(9-18(17)24-2)7-8-19-11-16(22)13-4-5-14(20)15(21)10-13/h3-6,9-10,16,19-22H,7-8,11H2,1-2H3",DIPGFXJERHNAQQ-UHFFFAOYSA-N,Agonist,Full agonist,,,,,pKi,,6.6,,,,,,,,,,8982677, β1-adrenoceptor,28,P08588,Human,denopamine,534,,5311064,COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC,"InChI=1S/C18H23NO4/c1-22-17-8-3-13(11-18(17)23-2)9-10-19-12-16(21)14-4-6-15(20)7-5-14/h3-8,11,16,19-21H,9-10,12H2,1-2H3/t16-/m0/s1",VHSBBVZJABQOSG-INIZCTEOSA-N,Agonist,Partial agonist,,,,,pEC50,,7.7,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,denopamine,534,,5311064,COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC,"InChI=1S/C18H23NO4/c1-22-17-8-3-13(11-18(17)23-2)9-10-19-12-16(21)14-4-6-15(20)7-5-14/h3-8,11,16,19-21H,9-10,12H2,1-2H3/t16-/m0/s1",VHSBBVZJABQOSG-INIZCTEOSA-N,Agonist,Partial agonist,,,,,pKi,6.1,,5.8,,,,,=,,,,10531390|7902433|20590599, β1-adrenoceptor,28,P08588,Human,dobutamine,535,,36811,CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O,"InChI=1S/C18H23NO3/c1-13(2-3-14-4-7-16(20)8-5-14)19-11-10-15-6-9-17(21)18(22)12-15/h4-9,12-13,19-22H,2-3,10-11H2,1H3",JRWZLRBJNMZMFE-UHFFFAOYSA-N,Agonist,Partial agonist,,,,,pEC50,,6.8,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,dobutamine,535,,36811,CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O,"InChI=1S/C18H23NO3/c1-13(2-3-14-4-7-16(20)8-5-14)19-11-10-15-6-9-17(21)18(22)12-15/h4-9,12-13,19-22H,2-3,10-11H2,1H3",JRWZLRBJNMZMFE-UHFFFAOYSA-N,Agonist,Partial agonist,,,yes,,pKi,5.5,,5.2,,,,,=,,,,10531390|20590599, β1-adrenoceptor,28,P08588,Human,isoprenaline,536,,3779,CC(NCC(c1ccc(c(c1)O)O)O)C,"InChI=1S/C11H17NO3/c1-7(2)12-6-11(15)8-3-4-9(13)10(14)5-8/h3-5,7,11-15H,6H2,1-2H3",JWZZKOKVBUJMES-UHFFFAOYSA-N,Agonist,Full agonist,,,,,pEC50,,8.6,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,isoprenaline,536,,3779,CC(NCC(c1ccc(c(c1)O)O)O)C,"InChI=1S/C11H17NO3/c1-7(2)12-6-11(15)8-3-4-9(13)10(14)5-8/h3-5,7,11-15H,6H2,1-2H3",JWZZKOKVBUJMES-UHFFFAOYSA-N,Agonist,Full agonist,,,yes,,pKi,7.0,,6.1,,,,,=,,,,8982677|2849109|20590599, β1-adrenoceptor,28,P08588,Human,prenalterol,537,,42396,O[C@H](COc1ccc(cc1)O)CNC(C)C,"InChI=1S/C12H19NO3/c1-9(2)13-7-11(15)8-16-12-5-3-10(14)4-6-12/h3-6,9,11,13-15H,7-8H2,1-2H3/t11-/m0/s1",ADUKCCWBEDSMEB-NSHDSACASA-N,Agonist,Partial agonist,,,,,pKi,,6.6,,,,,,=,,,,10531390|2564629, β1-adrenoceptor,28,P08588,Human,xamoterol,538,,155774,OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1,"InChI=1S/C16H25N3O5/c20-13-1-3-15(4-2-13)24-12-14(21)11-17-5-6-18-16(22)19-7-9-23-10-8-19/h1-4,14,17,20-21H,5-12H2,(H,18,22)",DXPOSRCHIDYWHW-UHFFFAOYSA-N,Agonist,Partial agonist,,,,,pKi,7.2,,7.0,,,,,=,,,,10531390|15655528, β1-adrenoceptor,28,P08588,Human,CGP 20712A,541,,2685,OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O,"InChI=1S/C23H25F3N4O5/c1-30-12-20(23(24,25)26)29-22(30)14-2-4-16(5-3-14)35-13-15(31)11-28-8-9-34-17-6-7-19(32)18(10-17)21(27)33/h2-7,10,12,15,28,31-32H,8-9,11,13H2,1H3,(H2,27,33)",GKJZEKSHCJELPL-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,9.2,,7.8,,,,,=,,,,10079020|15655528|10411574|27588207|26385885, β1-adrenoceptor,28,P08588,Human,H87/07,542,,193122,COCCOc1ccc(cc1)OCC(CNC(C)C)O,"InChI=1S/C15H25NO4/c1-12(2)16-10-13(17)11-20-15-6-4-14(5-7-15)19-9-8-18-3/h4-7,12-13,16-17H,8-11H2,1-3H3",FGAPARDHTDKREN-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,7.0,,,,,,,,,,10079020, β1-adrenoceptor,28,P08588,Human,LK 204-545,544,,5311116,N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O,"InChI=1S/C25H32N4O6/c26-14-19-13-23(34-12-11-33-16-18-1-2-18)7-8-24(19)35-17-22(31)15-27-9-10-28-25(32)29-20-3-5-21(30)6-4-20/h3-8,13,18,22,27,30-31H,1-2,9-12,15-17H2,(H2,28,29,32)",VAWYRUMIUGPAEX-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,8.5,,8.2,,,,,=,,,,10079020|28400472, β1-adrenoceptor,28,P08588,Human,NIHP,545,,10587912,OCCCc1ccc(cc1)OCC(CNC(C)C)O,"InChI=1S/C15H25NO3/c1-12(2)16-10-14(18)11-19-15-7-5-13(6-8-15)4-3-9-17/h5-8,12,14,16-18H,3-4,9-11H2,1-2H3",RUZBBQNQBDCLPE-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,7.1,,,,,,,,,,10079020, β1-adrenoceptor,28,P08588,Human,NIP,546,,3123920,OC(COc1ccccc1)CNC(C)C,"InChI=1S/C12H19NO2/c1-10(2)13-8-11(14)9-15-12-6-4-3-5-7-12/h3-7,10-11,13-14H,8-9H2,1-2H3",ONXLHKFGTDDVLQ-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,8.4,,,,,,,,,,10079020, β1-adrenoceptor,28,P08588,Human,SR59230A,547,,5311452,CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O,"InChI=1S/C21H27NO2/c1-2-16-8-4-6-13-21(16)24-15-18(23)14-22-20-12-7-10-17-9-3-5-11-19(17)20/h3-6,8-9,11,13,18,20,22-23H,2,7,10,12,14-15H2,1H3/t18-,20-/m0/s1",VFDHMSXXELYMRW-ICSRJNTNSA-N,Antagonist,Antagonist,,,,,pKi,8.6,,7.5,,,,,=,,,,15655528|10411574|20590599, β1-adrenoceptor,28,P18090,Rat,atenolol,548,,2249,OC(COc1ccc(cc1)CC(=O)N)CNC(C)C,"InChI=1S/C14H22N2O3/c1-10(2)16-8-12(17)9-19-13-5-3-11(4-6-13)7-14(15)18/h3-6,10,12,16-17H,7-9H2,1-2H3,(H2,15,18)",METKIMKYRPQLGS-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pA2,,6.8,,,,,,=,,,,31837330, β1-adrenoceptor,28,P08588,Human,atenolol,548,,2249,OC(COc1ccc(cc1)CC(=O)N)CNC(C)C,"InChI=1S/C14H22N2O3/c1-10(2)16-8-12(17)9-19-13-5-3-11(4-6-13)7-14(15)18/h3-6,10,12,16-17H,7-9H2,1-2H3,(H2,15,18)",METKIMKYRPQLGS-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,7.6,,6.7,,,,,=,,,,15060759|10079020|15655528, β1-adrenoceptor,28,P08588,Human,betaxolol,549,,2369,OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C,"InChI=1S/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3",NWIUTZDMDHAVTP-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,9.12,,8.2,,,,,=,,,,10079020|15655528|11572462, β1-adrenoceptor,28,P18090,Rat,bupranolol,550,,2475,OC(COc1cc(C)ccc1Cl)CNC(C)(C)C,"InChI=1S/C14H22ClNO2/c1-10-5-6-12(15)13(7-10)18-9-11(17)8-16-14(2,3)4/h5-7,11,16-17H,8-9H2,1-4H3",HQIRNZOQPUAHHV-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pA2,,9.0,,,,,,=,,,,31837330, β1-adrenoceptor,28,P08588,Human,bupranolol,550,,2475,OC(COc1cc(C)ccc1Cl)CNC(C)(C)C,"InChI=1S/C14H22ClNO2/c1-10-5-6-12(15)13(7-10)18-9-11(17)8-16-14(2,3)4/h5-7,11,16-17H,8-9H2,1-4H3",HQIRNZOQPUAHHV-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,9.0,,7.3,,,,,=,,,,10079020|15655528|10411574, β1-adrenoceptor,28,P08588,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,Antagonist,Antagonist,,,yes,,pKi,9.5,,8.8,,,,,=,,,,15655528|10411574, β1-adrenoceptor,28,P08588,Human,cicloprolol,552,,146294,OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C,"InChI=1S/C18H29NO4/c1-14(2)19-11-16(20)13-23-18-7-5-17(6-8-18)22-10-9-21-12-15-3-4-15/h5-8,14-16,19-20H,3-4,9-13H2,1-2H3",JNDJPKHYZWRRIS-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,8.0,,,,,,,,,,10079020, β1-adrenoceptor,28,P08588,Human,metoprolol,553,,4171,COCCc1ccc(cc1)OCC(CNC(C)C)O,"InChI=1S/C15H25NO3/c1-12(2)16-10-14(17)11-19-15-6-4-13(5-7-15)8-9-18-3/h4-7,12,14,16-17H,8-11H2,1-3H3",IUBSYMUCCVWXPE-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,7.9,,7.0,,,,,=,,,,10079020|15655528|10411574|14730417|14645666, β1-adrenoceptor,28,P08588,Human,nadolol,554,,39147,OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C,"InChI=1S/C17H27NO4/c1-17(2,3)18-9-12(19)10-22-16-6-4-5-11-7-14(20)15(21)8-13(11)16/h4-6,12,14-15,18-21H,7-10H2,1-3H3/t12?,14-,15+/m1/s1",VWPOSFSPZNDTMJ-UCWKZMIHSA-N,Antagonist,Antagonist,,,yes,,pKi,,6.9,,,,,,=,,,,10411574, β1-adrenoceptor,28,P08588,Human,practolol,555,,4883,OC(COc1ccc(cc1)NC(=O)C)CNC(C)C,"InChI=1S/C14H22N2O3/c1-10(2)15-8-13(18)9-19-14-6-4-12(5-7-14)16-11(3)17/h4-7,10,13,15,18H,8-9H2,1-3H3,(H,16,17)",DURULFYMVIFBIR-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,6.8,,6.1,,,,,=,,,,10079020|15655528, β1-adrenoceptor,28,P08588,Human,fenoterol,557,,3343,CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O,"InChI=1S/C17H21NO4/c1-11(6-12-2-4-14(19)5-3-12)18-10-17(22)13-7-15(20)9-16(21)8-13/h2-5,7-9,11,17-22H,6,10H2,1H3",LSLYOANBFKQKPT-UHFFFAOYSA-N,Agonist,Agonist,,,,,pEC50,,7.5,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,fenoterol,557,,3343,CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O,"InChI=1S/C17H21NO4/c1-11(6-12-2-4-14(19)5-3-12)18-10-17(22)13-7-15(20)9-16(21)8-13/h2-5,7-9,11,17-22H,6,10H2,1H3",LSLYOANBFKQKPT-UHFFFAOYSA-N,Agonist,Agonist,,,,,pKi,,5.0,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,terbutaline,560,,5403,OC(c1cc(O)cc(c1)O)CNC(C)(C)C,"InChI=1S/C12H19NO3/c1-12(2,3)13-7-11(16)8-4-9(14)6-10(15)5-8/h4-6,11,13-16H,7H2,1-3H3",XWTYSIMOBUGWOL-UHFFFAOYSA-N,Agonist,Partial agonist,,,,,pEC50,,5.8,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,terbutaline,560,,5403,OC(c1cc(O)cc(c1)O)CNC(C)(C)C,"InChI=1S/C12H19NO3/c1-12(2,3)13-7-11(16)8-4-9(14)6-10(15)5-8/h4-6,11,13-16H,7H2,1-3H3",XWTYSIMOBUGWOL-UHFFFAOYSA-N,Agonist,Partial agonist,,,,,pKi,,3.9,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,[125I]ICYP,562,,73754996,OC(COc1cccc2c1c([125I])c([nH]2)C#N)CNC(C)C,"InChI=1S/C15H18IN3O2/c1-9(2)18-7-10(20)8-21-13-5-3-4-11-14(13)15(16)12(6-17)19-11/h3-5,9-10,18-20H,7-8H2,1-2H3/i16-2",WGSPBWSPJOBKNT-RFLHHMENSA-N,Antagonist,Antagonist,It is necessary to use an excess of a β2-AR-selective ligand such as ICI 118551 in combination with this radioligand in order to allow visualisation of β1-AR binding in native tissue.,,,,pKd,11.3,,10.4,Kd,0.039,,0.00499,=,,,,8982677|10079020|10531390|15037517, β1-adrenoceptor,28,P08588,Human,timolol,565,,33624,O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C,"InChI=1S/C13H24N4O3S/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17/h10,14,18H,4-9H2,1-3H3/t10-/m0/s1",BLJRIMJGRPQVNF-JTQLQIEISA-N,Antagonist,Antagonist,,,,,pKi,9.0,,8.3,,,,,=,,,,15060759|15655528|14645666, β1-adrenoceptor,28,P08588,Human,BRL 37344,567,,9841972,C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O,"InChI=1S/C19H22ClNO4/c1-13(21-11-18(22)15-3-2-4-16(20)10-15)9-14-5-7-17(8-6-14)25-12-19(23)24/h2-8,10,13,18,21-22H,9,11-12H2,1H3,(H,23,24)/t13-,18+/m1/s1",ZGGNJJJYUVRADP-ACJLOTCBSA-N,Agonist,Partial agonist,,,,,pEC50,,6.5,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,BRL 37344,567,,9841972,C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O,"InChI=1S/C19H22ClNO4/c1-13(21-11-18(22)15-3-2-4-16(20)10-15)9-14-5-7-17(8-6-14)25-12-19(23)24/h2-8,10,13,18,21-22H,9,11-12H2,1H3,(H,23,24)/t13-,18+/m1/s1",ZGGNJJJYUVRADP-ACJLOTCBSA-N,Agonist,Partial agonist,,,,,pKi,,5.2,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,carazolol,569,,71739,OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C,"InChI=1S/C18H22N2O2/c1-12(2)19-10-13(21)11-22-17-9-5-8-16-18(17)14-6-3-4-7-15(14)20-16/h3-9,12-13,19-21H,10-11H2,1-2H3",BQXQGZPYHWWCEB-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKd,10.2,,9.7,,,,,=,,,,20590599|26385885, β1-adrenoceptor,28,P08588,Human,bunolol,570,,3914,CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O,"InChI=1S/C17H25NO3/c1-17(2,3)18-10-12(19)11-21-16-9-5-6-13-14(16)7-4-8-15(13)20/h5-6,9,12,18-19H,4,7-8,10-11H2,1-3H3",IXHBTMCLRNMKHZ-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,,8.4,,Ki,,3.99,,=,,,,, β1-adrenoceptor,28,P08588,Human,bunolol,570,,3914,CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O,"InChI=1S/C17H25NO3/c1-17(2,3)18-10-12(19)11-21-16-9-5-6-13-14(16)7-4-8-15(13)20/h5-6,9,12,18-19H,4,7-8,10-11H2,1-3H3",IXHBTMCLRNMKHZ-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,8.4,,,,,,=,,,,, β1-adrenoceptor,28,P08588,Human,propafenone,2561,,4932,CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O,"InChI=1S/C21H27NO3/c1-2-14-22-15-18(23)16-25-21-11-7-6-10-19(21)20(24)13-12-17-8-4-3-5-9-17/h3-11,18,22-23H,2,12-16H2,1H3",JWHAUXFOSRPERK-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,,6.7,,Ki,,205.0,,=,,,,, β1-adrenoceptor,28,P08588,Human,formoterol,3465,,3410,O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O,"InChI=1S/C19H24N2O4/c1-13(9-14-3-6-16(25-2)7-4-14)20-11-19(24)15-5-8-18(23)17(10-15)21-12-22/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22)",BPZSYCZIITTYBL-UHFFFAOYSA-N,Agonist,Agonist,,,,,pEC50,,8.3,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,formoterol,3465,,3410,O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O,"InChI=1S/C19H24N2O4/c1-13(9-14-3-6-16(25-2)7-4-14)20-11-19(24)15-5-8-18(23)17(10-15)21-12-22/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22)",BPZSYCZIITTYBL-UHFFFAOYSA-N,Agonist,Agonist,,,,,pKi,6.5,,6.1,,,,,=,,,,20590599|20655218, β1-adrenoceptor,28,P08588,Human,(-)-Ro 363,5571,,156297,COc1cc(CCNCC(COc2ccc(c(c2)O)O)O)ccc1OC,"InChI=1S/C19H25NO6/c1-24-18-6-3-13(9-19(18)25-2)7-8-20-11-14(21)12-26-15-4-5-16(22)17(23)10-15/h3-6,9-10,14,20-23H,7-8,11-12H2,1-2H3",RFNBEBPVKCJZPV-UHFFFAOYSA-N,Agonist,Agonist,,,,,pKi,,8.0,,,,,,=,,,,9117106, β1-adrenoceptor,28,P08588,Human,acebutolol,7107,,1978,CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O,"InChI=1S/C18H28N2O4/c1-5-6-18(23)20-14-7-8-17(16(9-14)13(4)21)24-11-15(22)10-19-12(2)3/h7-9,12,15,19,22H,5-6,10-11H2,1-4H3,(H,20,23)",GOEMGAFJFRBGGG-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,6.5,,6.4,,,,,=,,,,15655528, β1-adrenoceptor,28,P08588,Human,bisoprolol,7129,,2405,OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C,"InChI=1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3",VHYCDWMUTMEGQY-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,7.8,,Ki,,10.0,,=,,,,28400472, β1-adrenoceptor,28,P08588,Human,esmolol,7178,,59768,COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O,"InChI=1S/C16H25NO4/c1-12(2)17-10-14(18)11-21-15-7-4-13(5-8-15)6-9-16(19)20-3/h4-5,7-8,12,14,17-18H,6,9-11H2,1-3H3",AQNDDEOPVVGCPG-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,6.9,,6.7,,,,,=,,,,27451411, β1-adrenoceptor,28,P08588,Human,labetalol,7207,,3869,CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O,"InChI=1S/C19H24N2O3/c1-13(7-8-14-5-3-2-4-6-14)21-12-18(23)15-9-10-17(22)16(11-15)19(20)24/h2-6,9-11,13,18,21-23H,7-8,12H2,1H3,(H2,20,24)",SGUAFYQXFOLMHL-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,8.2,,7.6,,,,,=,,,,15655528|14645666, β1-adrenoceptor,28,,Rabbit,nebivolol,7246,,71301,OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O,"InChI=1S/C22H25F2NO4/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2",KOHIRBRYDXPAMZ-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pIC50,8.7,,8.1,,,,,=,,,,2462161, β1-adrenoceptor,28,P08588,Human,nebivolol,7246,,71301,OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O,"InChI=1S/C22H25F2NO4/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2",KOHIRBRYDXPAMZ-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,9.1,,,,,,=,Radioligand binding,,,20590599, β1-adrenoceptor,28,P08588,Human,sotalol,7297,,5253,CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C,"InChI=1S/C12H20N2O3S/c1-9(2)13-8-12(15)10-4-6-11(7-5-10)14-18(3,16)17/h4-7,9,12-15H,8H2,1-3H3",ZBMZVLHSJCTVON-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,6.1,,5.8,,,,,=,,,,15655528, β1-adrenoceptor,28,P08588,Human,mirabegron,7445,,9865528,O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O,"InChI=1S/C21H24N4O2S/c22-21-25-18(14-28-21)12-20(27)24-17-8-6-15(7-9-17)10-11-23-13-19(26)16-4-2-1-3-5-16/h1-9,14,19,23,26H,10-13H2,(H2,22,25)(H,24,27)/t19-/m0/s1",PBAPPPCECJKMCM-IBGZPJMESA-N,Agonist,Agonist,,,,,pEC50,5.0,,4.9,,,,,>,,,,17293563|32813332, β1-adrenoceptor,28,P08588,Human,indacaterol,7455,,6918554,CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O,"InChI=1S/C24H28N2O3/c1-3-14-9-16-11-18(12-17(16)10-15(14)4-2)25-13-22(28)19-5-7-21(27)24-20(19)6-8-23(29)26-24/h5-10,18,22,25,27-28H,3-4,11-13H2,1-2H3,(H,26,29)/t22-/m0/s1",QZZUEBNBZAPZLX-QFIPXVFZSA-N,Agonist,Agonist,,,,,pKi,,6.7,,Ki,,180.0,,=,,,,22932315, β1-adrenoceptor,28,P08588,Human,abediterol,9326,,11962616,O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O,"InChI=1S/C25H30F2N2O4/c26-25(27,18-8-4-3-5-9-18)17-33-15-7-2-1-6-14-28-16-22(31)19-10-12-21(30)24-20(19)11-13-23(32)29-24/h3-5,8-13,22,28,30-31H,1-2,6-7,14-17H2,(H,29,32)/t22-/m0/s1",SFYAXIFVXBKRPK-QFIPXVFZSA-N,Agonist,Agonist,,,,,pIC50,,7.44,,IC50,,36.2,,=,Membrane radioligand displacement assay using [3H]CGP12177 as tracer.,,,22588259, β1-adrenoceptor,28,P08588,Human,solabegron,9512,,9887812,Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O,"InChI=1S/C23H23ClN2O3/c24-20-8-2-6-18(13-20)22(27)15-25-10-11-26-21-9-3-5-17(14-21)16-4-1-7-19(12-16)23(28)29/h1-9,12-14,22,25-27H,10-11,15H2,(H,28,29)/t22-/m0/s1",LLDXOPKUNJTIRF-QFIPXVFZSA-N,Agonist,Agonist,,,,,pEC50,,5.4,,,,,,=,,,,16640337, β1-adrenoceptor,28,P08588,Human,levosalbutamol,9816,,123600,OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O,"InChI=1S/C13H21NO3/c1-13(2,3)14-7-12(17)9-4-5-11(16)10(6-9)8-15/h4-6,12,14-17H,7-8H2,1-3H3/t12-/m0/s1",NDAUXUAQIAJITI-LBPRGKRZSA-N,Agonist,Partial agonist,,,,,pEC50,,6.2,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,levosalbutamol,9816,,123600,OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O,"InChI=1S/C13H21NO3/c1-13(2,3)14-7-12(17)9-4-5-11(16)10(6-9)8-15/h4-6,12,14-17H,7-8H2,1-3H3/t12-/m0/s1",NDAUXUAQIAJITI-LBPRGKRZSA-N,Agonist,Partial agonist,,,,,pKi,,4.7,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,BI-167107,12065,,45483813,Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O,"InChI=1S/C21H26N2O4/c1-13-6-4-5-7-14(13)10-21(2,3)22-11-17(25)15-8-9-16(24)19-20(15)27-12-18(26)23-19/h4-9,17,22,24-25H,10-12H2,1-3H3,(H,23,26)",NWQXBEWHTDRJIP-UHFFFAOYSA-N,Agonist,Agonist,,,,,pEC50,,9.22,,EC50,,0.6,,=,Determined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ1-AR,,,19875286|33093660, β1-adrenoceptor,28,P08588,Human,cimaterol,12578,,2755,CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O,"InChI=1S/C12H17N3O/c1-8(2)15-7-12(16)9-3-4-11(14)10(5-9)6-13/h3-5,8,12,15-16H,7,14H2,1-2H3",BUXRLJCGHZZYNE-UHFFFAOYSA-N,Agonist,Agonist,,,,,pEC50,,8.4,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,cimaterol,12578,,2755,CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O,"InChI=1S/C12H17N3O/c1-8(2)15-7-12(16)9-3-4-11(14)10(5-9)6-13/h3-5,8,12,15-16H,7,14H2,1-2H3",BUXRLJCGHZZYNE-UHFFFAOYSA-N,Agonist,Agonist,,,,,pKi,,6.6,,,,,,=,,,,20590599, β1-adrenoceptor,28,P18090,Rat,NDD-713,12579,,167993658,O[C@@H](CNCCOC1=CC=C(C=C1)C(O)=N)COC2=CC3=C(O[C@H](CCCC4CC4)CO3)C=C2,"InChI=1S/C26H34N2O6/c27-26(30)19-6-8-21(9-7-19)31-13-12-28-15-20(29)16-32-22-10-11-24-25(14-22)33-17-23(34-24)3-1-2-18-4-5-18/h6-11,14,18,20,23,28-29H,1-5,12-13,15-17H2,(H2,27,30)/t20-,23+/m0/s1",KCULGNGHWNHUQW-NZQKXSOJSA-N,Antagonist,Antagonist,,,,,pKd,,8.1,,,,,,=,,,,28400472, β1-adrenoceptor,28,P08588,Human,NDD-713,12579,,167993658,O[C@@H](CNCCOC1=CC=C(C=C1)C(O)=N)COC2=CC3=C(O[C@H](CCCC4CC4)CO3)C=C2,"InChI=1S/C26H34N2O6/c27-26(30)19-6-8-21(9-7-19)31-13-12-28-15-20(29)16-32-22-10-11-24-25(14-22)33-17-23(34-24)3-1-2-18-4-5-18/h6-11,14,18,20,23,28-29H,1-5,12-13,15-17H2,(H2,27,30)/t20-,23+/m0/s1",KCULGNGHWNHUQW-NZQKXSOJSA-N,Antagonist,Antagonist,,,,,pKi,8.5,,7.8,,,,,=,,,,28400472, β1-adrenoceptor,28,P18090,Rat,NDD-825,12580,,167993659,O[C@@H](CNCCOC1=CC=C2C(=O)NCC2=C1)COC3=CC4=C(O[C@H](CCCC5CC5)CO4)C=C3,"InChI=1S/C27H34N2O6/c30-20(15-28-10-11-32-21-6-8-24-19(12-21)14-29-27(24)31)16-33-22-7-9-25-26(13-22)34-17-23(35-25)3-1-2-18-4-5-18/h6-9,12-13,18,20,23,28,30H,1-5,10-11,14-17H2,(H,29,31)/t20-,23+/m0/s1",FZVQBHZOAHLLDF-NZQKXSOJSA-N,Antagonist,Antagonist,,,,,pKd,,8.4,,,,,,=,,,,28400472, β1-adrenoceptor,28,P08588,Human,NDD-825,12580,,167993659,O[C@@H](CNCCOC1=CC=C2C(=O)NCC2=C1)COC3=CC4=C(O[C@H](CCCC5CC5)CO4)C=C3,"InChI=1S/C27H34N2O6/c30-20(15-28-10-11-32-21-6-8-24-19(12-21)14-29-27(24)31)16-33-22-7-9-25-26(13-22)34-17-23(35-25)3-1-2-18-4-5-18/h6-9,12-13,18,20,23,28,30H,1-5,10-11,14-17H2,(H,29,31)/t20-,23+/m0/s1",FZVQBHZOAHLLDF-NZQKXSOJSA-N,Antagonist,Antagonist,,,,,pKi,9.0,,8.3,,,,,=,,,,28400472, β1-adrenoceptor,28,P08588,Human,ICI-89406,12581,,123686,C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O,"InChI=1S/C19H22N4O3/c20-12-15-6-4-5-9-18(15)26-14-17(24)13-21-10-11-22-19(25)23-16-7-2-1-3-8-16/h1-9,17,21,24H,10-11,13-14H2,(H2,22,23,25)",HTLWRKRZKFAAAH-UHFFFAOYSA-N,Antagonist,Partial agonist,,,,,pKi,,8.8,,,,,,=,,,,23614528, β1-adrenoceptor,28,P08588,Human,clenbuterol,12582,,2783,CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O,"InChI=1S/C12H18Cl2N2O/c1-12(2,3)16-6-10(17)7-4-8(13)11(15)9(14)5-7/h4-5,10,16-17H,6,15H2,1-3H3",STJMRWALKKWQGH-UHFFFAOYSA-N,Agonist,Full agonist,,,,,pEC50,,9.2,,,,,,=,,,,20590599, β1-adrenoceptor,28,P08588,Human,clenbuterol,12582,,2783,CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O,"InChI=1S/C12H18Cl2N2O/c1-12(2,3)16-6-10(17)7-4-8(13)11(15)9(14)5-7/h4-5,10,16-17H,6,15H2,1-3H3",STJMRWALKKWQGH-UHFFFAOYSA-N,Agonist,Full agonist,,,,,pKi,7.9,,7.4,,,,,=,,,,20590599|25324048, β1-adrenoceptor,28,P08588,Human,7-methylcyanopindolol,13191,,91885640,C(C)(C)(C)NC[C@@H](COC1=C2C=C(NC2=C(C=C1)C)C#N)O,"InChI=1S/C17H23N3O2/c1-11-5-6-15(14-7-12(8-18)20-16(11)14)22-10-13(21)9-19-17(2,3)4/h5-7,13,19-21H,9-10H2,1-4H3/t13-/m0/s1",NDCOGBYMSDLXAU-ZDUSSCGKSA-N,Antagonist,Antagonist,,,,,pKd,,10.4,,,,,,=,,,,26385885, β1-adrenoceptor,28,P08588,Human,landiolol,13192,,114905,CC1(OC[C@H](O1)COC(=O)CCC2=CC=C(C=C2)OC[C@H](CNCCNC(=O)N3CCOCC3)O)C,"InChI=1S/C25H39N3O8/c1-25(2)35-18-22(36-25)17-34-23(30)8-5-19-3-6-21(7-4-19)33-16-20(29)15-26-9-10-27-24(31)28-11-13-32-14-12-28/h3-4,6-7,20,22,26,29H,5,8-18H2,1-2H3,(H,27,31)/t20-,22+/m0/s1",WMDSZGFJQKSLLH-RBBKRZOGSA-N,Antagonist,Antagonist,,,,,pKi,,7.0,,,,,,=,,,,27451411, β1-adrenoceptor,28,P08588,Human,bucindolol,13193,,51045,CC(C)(CC1=CNC2=CC=CC=C21)NCC(COC3=CC=CC=C3C#N)O,"InChI=1S/C22H25N3O2/c1-22(2,11-17-13-24-20-9-5-4-8-19(17)20)25-14-18(26)15-27-21-10-6-3-7-16(21)12-23/h3-10,13,18,24-26H,11,14-15H2,1-2H3",FBMYKMYQHCBIGU-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,9.3,,,,,,=,,,,20590599,