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 CB1 receptor,56,P20272,Rat,2-arachidonoylglycerol,729,,5282280,CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)OC(CO)CO,"InChI=1S/C23H38O4/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-23(26)27-22(20-24)21-25/h6-7,9-10,12-13,15-16,22,24-25H,2-5,8,11,14,17-21H2,1H3/b7-6-,10-9-,13-12-,16-15-",RCRCTBLIHCHWDZ-DOFZRALJSA-N,Agonist,Full agonist,,yes,,,pKi,7.2,,6.3,,,,,,,,,7605349|9721036, CB1 receptor,56,P21554,Human,CP55940,730,,104895,CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C,"InChI=1S/C24H40O3/c1-4-5-6-7-14-24(2,3)19-11-13-21(23(27)16-19)22-17-20(26)12-10-18(22)9-8-15-25/h11,13,16,18,20,22,25-27H,4-10,12,14-15,17H2,1-3H3/t18-,20-,22-/m1/s1",YNZFFALZMRAPHQ-SYYKKAFVSA-N,Agonist,Full agonist,,,,,pKi,9.2,,8.3,,,,,=,,,,7565624|8819477|10188977, CB1 receptor,56,P21554,Human,HU-210,731,,9821569,CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)CO)(C)C)(C)C,"InChI=1S/C25H38O3/c1-6-7-8-9-12-24(2,3)18-14-21(27)23-19-13-17(16-26)10-11-20(19)25(4,5)28-22(23)15-18/h10,14-15,19-20,26-27H,6-9,11-13,16H2,1-5H3/t19-,20-/m1/s1",SSQJFGMEZBFMNV-WOJBJXKFSA-N,Agonist,Full agonist,,,,,pKi,10.2,,9.1,,,,,=,,,,7565624|8819477, CB1 receptor,56,P20272,Rat,O-1812,732,,9823107,OC[C@H](NC(=O)CCC/C=C\C/C=C\C/C=C\C/C=C\C(CCCCC#N)(C)C)C,"InChI=1S/C26H42N2O2/c1-24(23-29)28-25(30)19-15-12-10-8-6-4-5-7-9-11-13-16-20-26(2,3)21-17-14-18-22-27/h4-5,8-11,16,20,24,29H,6-7,12-15,17-19,21,23H2,1-3H3,(H,28,30)/b5-4-,10-8-,11-9-,20-16-/t24-/m1/s1",WZQHSBKOWZOASP-QLZKPENWSA-N,Agonist,Full agonist,,,,,pKi,,8.5,,Ki,,3.16,,=,,,,11181068, CB1 receptor,56,P21554,Human,WIN55212-2,733,,5311501,O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2,"InChI=1S/C27H26N2O3/c1-18-25(27(30)22-9-4-7-19-6-2-3-8-21(19)22)23-10-5-11-24-26(23)29(18)20(17-32-24)16-28-12-14-31-15-13-28/h2-11,20H,12-17H2,1H3/t20-/m1/s1",HQVHOQAKMCMIIM-HXUWFJFHSA-N,Agonist,Full agonist,,,,,pKi,8.7,,6.9,,,,,=,,,,7565624|8819477|8679694, CB1 receptor,56,P21554,Human,[3H]CP55940,734,,104895,CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C,"InChI=1S/C24H40O3/c1-4-5-6-7-14-24(2,3)19-11-13-21(23(27)16-19)22-17-20(26)12-10-18(22)9-8-15-25/h11,13,16,18,20,22,25-27H,4-10,12,14-15,17H2,1-3H3/t18-,20-,22-/m1/s1",YNZFFALZMRAPHQ-SYYKKAFVSA-N,Agonist,Full agonist,,,,,pKd,9.4,,8.5,,,,,,,,,7775459|8819477|8526880|1718258|1331766|8636122, CB1 receptor,56,P20272,Rat,[3H]HU-243,735,,3081854,CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2C[C@]([3H])(CO)C(C1)[3H])(C)C)(C)C,"InChI=1S/C25H40O3/c1-6-7-8-9-12-24(2,3)18-14-21(27)23-19-13-17(16-26)10-11-20(19)25(4,5)28-22(23)15-18/h14-15,17,19-20,26-27H,6-13,16H2,1-5H3/t17-,19-,20-/m1/s1/i10T,17T/t10?,17-,19-,20-",MVEVPDCVOXJVBD-AENGYHINSA-N,Agonist,Full agonist,,,,,pKd,,10.4,,,,,,,,,,1317925, CB1 receptor,56,P21554,Human,[3H]WIN55212-2,736,,5689,O=C(c1c(C)n2c3c1cccc3OCC2CN1CCOCC1)c1cccc2c1cccc2,"InChI=1S/C27H26N2O3/c1-18-25(27(30)22-9-4-7-19-6-2-3-8-21(19)22)23-10-5-11-24-26(23)29(18)20(17-32-24)16-28-12-14-31-15-13-28/h2-11,20H,12-17H2,1H3",HQVHOQAKMCMIIM-UHFFFAOYSA-N,Agonist,Full agonist,,,,,pKd,7.9,,7.8,,,,,,,,,8622639|9422383, CB1 receptor,56,P20272,Rat,arachidonyl-2-chloroethylamide,738,,5311006,CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCCCl,"InChI=1S/C22H36ClNO/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-22(25)24-21-20-23/h6-7,9-10,12-13,15-16H,2-5,8,11,14,17-21H2,1H3,(H,24,25)/b7-6-,10-9-,13-12-,16-15-",SCJNCDSAIRBRIA-DOFZRALJSA-N,Agonist,Full agonist,,,,,pKi,,8.9,,,,,,=,,,,10336536, CB1 receptor,56,P20272,Rat,arachidonylcyclopropylamide,739,,5311007,CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1,"InChI=1S/C23H37NO/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-23(25)24-22-20-21-22/h6-7,9-10,12-13,15-16,22H,2-5,8,11,14,17-21H2,1H3,(H,24,25)/b7-6-,10-9-,13-12-,16-15-",GLGAUBPACOBAMV-DOFZRALJSA-N,Agonist,Full agonist,,,,,pKi,,8.7,,,,,,=,,,,10336536, CB1 receptor,56,P21554,Human,cannabinol,740,,2543,CCCCCc1cc(O)c2c(c1)OC(c1c2cc(C)cc1)(C)C,"InChI=1S/C21H26O2/c1-5-6-7-8-15-12-18(22)20-16-11-14(2)9-10-17(16)21(3,4)23-19(20)13-15/h9-13,22H,5-8H2,1-4H3",VBGLYOIFKLUMQG-UHFFFAOYSA-N,Agonist,Partial agonist,,,,,pKi,6.5,,6.0,,,,,=,,,,7565624|8819477, CB1 receptor,56,P20272,Rat,AM281,741,,4302962,Ic1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCOCC1,"InChI=1S/C21H19Cl2IN4O2/c1-13-19(21(29)26-27-8-10-30-11-9-27)25-28(18-7-4-15(22)12-17(18)23)20(13)14-2-5-16(24)6-3-14/h2-7,12H,8-11H2,1H3,(H,26,29)",AJFFBPZYXRNAIC-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,7.9,,Ki,,12.6,,=,,,,11741201, CB1 receptor,56,P21554,Human,LY320135,742,,5311257,COc1ccc2c(c1)oc(c2C(=O)c1ccc(cc1)C#N)c1ccc(cc1)OC,"InChI=1S/C24H17NO4/c1-27-18-9-7-17(8-10-18)24-22(20-12-11-19(28-2)13-21(20)29-24)23(26)16-5-3-15(14-25)4-6-16/h3-13H,1-2H3",RYNSGDFWBJWWSZ-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,6.9,,Ki,,126.0,,=,,,,9435190, CB1 receptor,56,P21554,Human,rimonabant,743,,104850,Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1,"InChI=1S/C22H21Cl3N4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-9-17(24)13-18(19)25)21(14)15-5-7-16(23)8-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30)",JZCPYUJPEARBJL-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,8.7,,7.9,Ki,12.6,,1.99,=,,,,7565624|8819477|9435190|8070571|12663689, CB1 receptor,56,P47746,Mouse,[123I]AM251,744,,10506880,[123I]c1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1,"InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30)/i25-4",BUZAJRPLUGXRAB-VEFBWTBNSA-N,Antagonist,Antagonist,,,,,pKd,,9.6,,,,,,,,,,9335234, CB1 receptor,56,P20272,Rat,[3H]rimonabant,745,,54585418,Clc1ccc(cc1)c1n(nc(c1C([3H])([3H])[3H])C(=O)NN1CCCCC1)c1ccc(cc1Cl)Cl,"InChI=1S/C22H21Cl3N4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-9-17(24)13-18(19)25)21(14)15-5-7-16(23)8-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30)/i1T3",JZCPYUJPEARBJL-RLXJOQACSA-N,Antagonist,Antagonist,,,,,pKd,10.0,,8.92,Kd,1.2,,0.1,=,,,,9316881|8981483|8978752|8733746|8614277|8987831|9536023, CB1 receptor,56,P21554,Human,anandamide,2364,,5281969,CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCCO,"InChI=1S/C22H37NO2/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-22(25)23-20-21-24/h6-7,9-10,12-13,15-16,24H,2-5,8,11,14,17-21H2,1H3,(H,23,25)/b7-6-,10-9-,13-12-,16-15-",LGEQQWMQCRIYKG-DOFZRALJSA-N,Agonist,Partial agonist,,yes,,,pKi,7.0,,6.3,,,,,,,,,7565624|8819477, CB1 receptor,56,P21554,Human,Δ9-tetrahydrocannabinol,2424,,16078,CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C,"InChI=1S/C21H30O2/c1-5-6-7-8-15-12-18(22)20-16-11-14(2)9-10-17(16)21(3,4)23-19(20)13-15/h11-13,16-17,22H,5-10H2,1-4H3/t16-,17-/m1/s1",CYQFCXCEBYINGO-IAGOWNOFSA-N,Agonist,Partial agonist,,,yes,,pKi,7.4,,7.3,,,,,=,,,,7565624|8819477, CB1 receptor,56,P20272,Rat,R-(+)-methanandamide,2506,,6321351,CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)N[C@@H](CO)C,"InChI=1S/C23H39NO2/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-20-23(26)24-22(2)21-25/h7-8,10-11,13-14,16-17,22,25H,3-6,9,12,15,18-21H2,1-2H3,(H,24,26)/b8-7-,11-10-,14-13-,17-16-/t22-/m1/s1",SQKRUBZPTNJQEM-FQPARAGTSA-N,Agonist,Agonist,,,,,pKi,,7.7,,Ki,,20.0,,=,,,,8893848, CB1 receptor,56,P20272,Rat,AM251,3317,,2125,Ic1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1,"InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30)",BUZAJRPLUGXRAB-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,8.1,,Ki,,7.94,,=,,,,10052983, CB1 receptor,56,P21554,Human,cannabidiol,4150,,644019,CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C,"InChI=1S/C21H30O2/c1-5-6-7-8-16-12-19(22)21(20(23)13-16)18-11-15(4)9-10-17(18)14(2)3/h11-13,17-18,22-23H,2,5-10H2,1,3-4H3/t17-,18+/m0/s1",QHMBSVQNZZTUGM-ZWKOTPCHSA-N,Allosteric modulator,Negative,,,,,,,,,,,,,=,,,,26218440, CB1 receptor,56,P21554,Human,Org27569,7851,,44828492,CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1,"InChI=1S/C24H28ClN3O/c1-2-20-21-16-18(25)8-11-22(21)27-23(20)24(29)26-13-12-17-6-9-19(10-7-17)28-14-4-3-5-15-28/h6-11,16,27H,2-5,12-15H2,1H3,(H,26,29)",AHFZDNYNXFMRFQ-UHFFFAOYSA-N,Allosteric modulator,Positive,,,yes,,pEC50,,6.85,,EC50,,140.0,,=,Measured as increased binding of radiolabelled orthosteric agonist CP55940,,,22571451, CB1 receptor,56,P21554,Human,TM38837,8705,,66772777,C[C@@H](NC(=O)C1=NN(C(=C1CC2=NNN=N2)C3=CC=C(Cl)C=C3)C4=CC=CC=C4Cl)C5=CC=C(C=C5)C(F)(F)F,"InChI=1S/C27H20Cl2F3N7O/c1-15(16-6-10-18(11-7-16)27(30,31)32)33-26(40)24-20(14-23-34-37-38-35-23)25(17-8-12-19(28)13-9-17)39(36-24)22-5-3-2-4-21(22)29/h2-13,15H,14H2,1H3,(H,33,40)(H,34,35,37,38)/t15-/m1/s1",DANBLBWVACCFGQ-OAHLLOKOSA-N,Antagonist,Antagonist,,,yes,,pIC50,,8.07,,IC50,,6.7,,=,Determined as antagonism in a GTPγS assay.,,,20652930|38043690, CB1 receptor,56,P21554,Human,TM38837,8705,,66772777,C[C@@H](NC(=O)C1=NN(C(=C1CC2=NNN=N2)C3=CC=C(Cl)C=C3)C4=CC=CC=C4Cl)C5=CC=C(C=C5)C(F)(F)F,"InChI=1S/C27H20Cl2F3N7O/c1-15(16-6-10-18(11-7-16)27(30,31)32)33-26(40)24-20(14-23-34-37-38-35-23)25(17-8-12-19(28)13-9-17)39(36-24)22-5-3-2-4-21(22)29/h2-13,15H,14H2,1H3,(H,33,40)(H,34,35,37,38)/t15-/m1/s1",DANBLBWVACCFGQ-OAHLLOKOSA-N,Antagonist,Inverse agonist,,,,,pIC50,,7.62,,IC50,,24.0,,=,Determined in a GTPγS assay,,,38043690, CB1 receptor,56,P21554,Human,compound 70 [PMID: 26161824],8706,,46894021,N#CCCC#Cc1ccc(cc1)c1c(CO)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCOCC1,"InChI=1S/C26H23Cl2N5O3/c27-20-9-10-23(22(28)16-20)33-25(19-7-5-18(6-8-19)4-2-1-3-11-29)21(17-34)24(30-33)26(35)31-32-12-14-36-15-13-32/h5-10,16,34H,1,3,12-15,17H2,(H,31,35)",VQXIVPLXEIZJTH-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,,8.15,,Ki,,7.0,,=,,,,26161824, CB1 receptor,56,P21554,Human,nabilone,9071,,39860,CCCCCCC(c1cc(O)c2c(c1)OC(C1C2CC(=O)CC1)(C)C)(C)C,"InChI=1S/C24H36O3/c1-6-7-8-9-12-23(2,3)16-13-20(26)22-18-15-17(25)10-11-19(18)24(4,5)27-21(22)14-16/h13-14,18-19,26H,6-12,15H2,1-5H3",GECBBEABIDMGGL-UHFFFAOYSA-N,Agonist,Agonist,,,,,pKi,,8.4,,Ki,,3.98,,=,,,,21885167, CB1 receptor,56,P21554,Human,pepcan-12,9188,,90488874,CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](N)CCCN=C(N)N)C(C)C)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)O,"InChI=1S/C65H105N19O17/c1-33(2)24-41(55(91)76-42(25-34(3)4)56(92)81-47(31-85)59(95)80-46(64(100)101)27-38-30-71-32-73-38)75-54(90)40(19-12-13-21-66)74-57(93)43(26-37-16-10-9-11-17-37)77-58(94)44(28-49(68)86)78-61(97)52(36(7)8)83-60(96)48-20-15-23-84(48)63(99)45(29-50(87)88)79-62(98)51(35(5)6)82-53(89)39(67)18-14-22-72-65(69)70/h9-11,16-17,30,32-36,39-48,51-52,85H,12-15,18-29,31,66-67H2,1-8H3,(H2,68,86)(H,71,73)(H,74,93)(H,75,90)(H,76,91)(H,77,94)(H,78,97)(H,79,98)(H,80,95)(H,81,92)(H,82,89)(H,83,96)(H,87,88)(H,100,101)(H4,69,70,72)/t39-,40-,41-,42-,43-,44-,45-,46-,47-,48-,51-,52-/m0/s1",CSDQEWILNKOWRN-WSDCEOHFSA-N,Allosteric modulator,Negative,,,,,pKB,8.33,,8.09,,,,,=,,,,22952224, CB1 receptor,56,P21554,Human,taranabant,9231,,11226090,N#Cc1cccc(c1)[C@@H]([C@@H](NC(=O)C(Oc1ccc(cn1)C(F)(F)F)(C)C)C)Cc1ccc(cc1)Cl,"InChI=1S/C27H25ClF3N3O2/c1-17(34-25(35)26(2,3)36-24-12-9-21(16-33-24)27(29,30)31)23(14-18-7-10-22(28)11-8-18)20-6-4-5-19(13-20)15-32/h4-13,16-17,23H,14H2,1-3H3,(H,34,35)/t17-,23+/m0/s1",QLYKJCMUNUWAGO-GAJHUEQPSA-N,Antagonist,Inverse agonist,,,yes,,pKi,,9.52,,Ki,,0.3,,=,Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting.,,,19520572, CB1 receptor,56,P21554,Human,otenabant,9232,,10052040,CCNC1(CCN(CC1)c1ncnc2c1nc(n2c1ccc(cc1)Cl)c1ccccc1Cl)C(=O)N,"InChI=1S/C25H25Cl2N7O/c1-2-31-25(24(28)35)11-13-33(14-12-25)22-20-23(30-15-29-22)34(17-9-7-16(26)8-10-17)21(32-20)18-5-3-4-6-19(18)27/h3-10,15,31H,2,11-14H2,1H3,(H2,28,35)",UNAZAADNBYXMIV-UHFFFAOYSA-N,Antagonist,Inverse agonist,,,yes,,pKi,,9.15,,Ki,,0.7,,=,Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells,,,19102698, CB1 receptor,56,P20272,Rat,otenabant,9232,,10052040,CCNC1(CCN(CC1)c1ncnc2c1nc(n2c1ccc(cc1)Cl)c1ccccc1Cl)C(=O)N,"InChI=1S/C25H25Cl2N7O/c1-2-31-25(24(28)35)11-13-33(14-12-25)22-20-23(30-15-29-22)34(17-9-7-16(26)8-10-17)21(32-20)18-5-3-4-6-19(18)27/h3-10,15,31H,2,11-14H2,1H3,(H2,28,35)",UNAZAADNBYXMIV-UHFFFAOYSA-N,Antagonist,Inverse agonist,,,,,pKi,,8.55,,Ki,,2.8,,=,Displacement of [3H]SR141716A from CB1 receptor in rat brain,,,19102698, CB1 receptor,56,P21554,Human,surinabant,9233,,9849616,CCc1c(nn(c1c1ccc(cc1)Br)c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1,"InChI=1S/C23H23BrCl2N4O/c1-2-18-21(23(31)28-29-12-4-3-5-13-29)27-30(20-11-10-17(25)14-19(20)26)22(18)15-6-8-16(24)9-7-15/h6-11,14H,2-5,12-13H2,1H3,(H,28,31)",HMXDWDSNPRNUKI-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,,8.46,,Ki,,3.5,,=,Inhibition of [3H]CP-55940 binding to human cannabinoid receptor 1 expressed in CHO cells,,,15131245, CB1 receptor,56,P21554,Human,ibipinabant,9234,,9826744,CN=C(N1N=C([C@H](C1)c1ccccc1)c1ccc(cc1)Cl)NS(=O)(=O)c1ccc(cc1)Cl,"InChI=1S/C23H20Cl2N4O2S/c1-26-23(28-32(30,31)20-13-11-19(25)12-14-20)29-15-21(16-5-3-2-4-6-16)22(27-29)17-7-9-18(24)10-8-17/h2-14,21H,15H2,1H3,(H,26,28)/t21-/m1/s1",AXJQVVLKUYCICH-OAQYLSRUSA-N,Antagonist,Antagonist,,,yes,,pKi,,8.11,,Ki,,7.8,,=,Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells,,,14736243, CB1 receptor,56,P21554,Human,GAT100,9237,,117923261,N#CSc1ccc2c(c1)c(CC)c([nH]2)C(=O)NCCc1ccc(cc1)N1CCCCC1,"InChI=1S/C25H28N4OS/c1-2-21-22-16-20(31-17-26)10-11-23(22)28-24(21)25(30)27-13-12-18-6-8-19(9-7-18)29-14-4-3-5-15-29/h6-11,16,28H,2-5,12-15H2,1H3,(H,27,30)",OZEQTGDZTPJNAR-UHFFFAOYSA-N,Allosteric modulator,Negative,,,,,pEC50,,7.72,,EC50,,19.2,,=,"Although GAT100 antagonized CP55940-induced stimulation of [35S]GTPγS binding to human CB1 CHO cell membranes, it enhanced the binding of [3H]CP55940 to these membranes. The EC50 and Emax values of GAT100 for this enhancement, with the 95% confidence limits shown in brackets, were 19.6 nM (10.4 & 36.9 nM) and 116.5% (108.3 & 124.6%), respectively. GAT100 (500 nM) was also found to enhance saturation binding of [3H]CP55940 to human CB1 HEK293 cell membranes.",,,26529344, CB1 receptor,56,P21554,Human,GAT100,9237,,117923261,N#CSc1ccc2c(c1)c(CC)c([nH]2)C(=O)NCCc1ccc(cc1)N1CCCCC1,"InChI=1S/C25H28N4OS/c1-2-21-22-16-20(31-17-26)10-11-23(22)28-24(21)25(30)27-13-12-18-6-8-19(9-7-18)29-14-4-3-5-15-29/h6-11,16,28H,2-5,12-15H2,1H3,(H,27,30)",OZEQTGDZTPJNAR-UHFFFAOYSA-N,Allosteric modulator,Negative,,,,,pEC50,,6.39,,EC50,,409.8,,=,"Measuring GAT100's inhibition of [3H]SR141716A binding, in radioligand binding assays",,,27046127, CB1 receptor,56,P47746,Mouse,ZCZ011,9239,,71819307,[O-][N+](=O)CC(c1c([nH]c2c1ccc(c2)C)c1ccccc1)c1cccs1,"InChI=1S/C21H18N2O2S/c1-14-9-10-16-18(12-14)22-21(15-6-3-2-4-7-15)20(16)17(13-23(24)25)19-8-5-11-26-19/h2-12,17,22H,13H2,1H3",RJSPNRDBWHHFMH-UHFFFAOYSA-N,Allosteric modulator,Positive,,,,,pEC50,,6.9,,,,,,=,"Equilibrium binding experiment versus [3H]CP55940, to mouse brain membranes.",,,26052038, CB1 receptor,56,P47746,Mouse,ZCZ011,9239,,71819307,[O-][N+](=O)CC(c1c([nH]c2c1ccc(c2)C)c1ccccc1)c1cccs1,"InChI=1S/C21H18N2O2S/c1-14-9-10-16-18(12-14)22-21(15-6-3-2-4-7-15)20(16)17(13-23(24)25)19-8-5-11-26-19/h2-12,17,22H,13H2,1H3",RJSPNRDBWHHFMH-UHFFFAOYSA-N,Allosteric modulator,Positive,,,,,pEC50,,6.31,,,,,,=,"Equilibrium binding experiment versus [3HWIN55212, to mouse brain membranes.",,,26052038, CB1 receptor,56,P20272,Rat,AM7499,9257,,121231416,CCCCOC(=O)C(c1cc(O)c2c(c1)OC([C@H]1[C@H]2C[C@H](CO)CC1)(C)C)(C)C,"InChI=1S/C24H36O5/c1-6-7-10-28-22(27)23(2,3)16-12-19(26)21-17-11-15(14-25)8-9-18(17)24(4,5)29-20(21)13-16/h12-13,15,17-18,25-26H,6-11,14H2,1-5H3/t15-,17-,18-/m1/s1",OSVHLUXLWQLPIY-KBAYOESNSA-N,Agonist,Agonist,,,,,pKi,,8.62,,Ki,,2.4,,=,,,,27367336, CB1 receptor,56,P21554,Human,AM6538,9338,,46912833,[O-][N+](=O)OCCC#Cc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1,"InChI=1S/C26H25Cl2N5O4/c1-18-24(26(34)30-31-14-4-2-5-15-31)29-32(23-13-12-21(27)17-22(23)28)25(18)20-10-8-19(9-11-20)7-3-6-16-37-33(35)36/h8-13,17H,2,4-6,14-16H2,1H3,(H,30,34)",KXXKUWQMQUYUSE-UHFFFAOYSA-N,Antagonist,Antagonist,,,yes,,pKi,,8.34,,Ki,,4.6,,=,"Competition binding assay using [3H]-CP55,940",,,27768894, CB1 receptor,56,P21554,Human,BMS-202,9607,,117951478,COc1nc(OCc2cccc(c2C)c2ccccc2)ccc1CNCCNC(=O)C,"InChI=1S/C25H29N3O3/c1-18-22(10-7-11-23(18)20-8-5-4-6-9-20)17-31-24-13-12-21(25(28-24)30-3)16-26-14-15-27-19(2)29/h4-13,26H,14-17H2,1-3H3,(H,27,29)",JEDPSOYOYVELLZ-UHFFFAOYSA-N,Agonist,Agonist,,,,,pIC50,,6.99,,IC50,,102.0,,=,,,,25921407, CB1 receptor,56,P21554,Human,AM11542,9612,,53318931,BrCCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)C)(C)C)(C)C,"InChI=1S/C25H37BrO2/c1-17-10-11-20-19(14-17)23-21(27)15-18(16-22(23)28-25(20,4)5)24(2,3)12-8-6-7-9-13-26/h10,15-16,19-20,27H,6-9,11-14H2,1-5H3/t19-,20-/m1/s1",SZDVFUZKFPGYEK-WOJBJXKFSA-N,Agonist,Agonist,,,,,pKi,,9.96,,Ki,,0.11,,=,,,,28678776, CB1 receptor,56,P21554,Human,AM841,9613,,102336704,S=C=NCCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2C[C@H](CO)CC1)(C)C)(C)C,"InChI=1S/C26H39NO3S/c1-25(2,11-7-5-6-8-12-27-17-31)19-14-22(29)24-20-13-18(16-28)9-10-21(20)26(3,4)30-23(24)15-19/h14-15,18,20-21,28-29H,5-13,16H2,1-4H3/t18-,20-,21-/m1/s1",JCIYJYHFBBXSBF-HMXCVIKNSA-N,Agonist,Agonist,,,,,pKi,,8.94,,Ki,,1.14,,=,,,,28678776, CB1 receptor,56,P21554,Human,AM2201,9705,,53393997,FCCCCCn1cc(c2c1cccc2)C(=O)c1cccc2c1cccc2,"InChI=1S/C24H22FNO/c25-15-6-1-7-16-26-17-22(20-12-4-5-14-23(20)26)24(27)21-13-8-10-18-9-2-3-11-19(18)21/h2-5,8-14,17H,1,6-7,15-16H2",ALQFAGFPQCBPED-UHFFFAOYSA-N,Agonist,Agonist,,,,,pEC50,,7.42,,EC50,,38.0,,=,,,,25921407, CB1 receptor,56,P20272,Rat,AM2201,9705,,53393997,FCCCCCn1cc(c2c1cccc2)C(=O)c1cccc2c1cccc2,"InChI=1S/C24H22FNO/c25-15-6-1-7-16-26-17-22(20-12-4-5-14-23(20)26)24(27)21-13-8-10-18-9-2-3-11-19(18)21/h2-5,8-14,17H,1,6-7,15-16H2",ALQFAGFPQCBPED-UHFFFAOYSA-N,Agonist,Agonist,,,,,pKi,,9.0,,Ki,,1.0,,=,Binding affinity vs. rat forebrain membranes.,,,, CB1 receptor,56,P21554,Human,JWH-018,9706,,10382701,CCCCCn1cc(c2c1cccc2)C(=O)c1cccc2c1cccc2,"InChI=1S/C24H23NO/c1-2-3-8-16-25-17-22(20-13-6-7-15-23(20)25)24(26)21-14-9-11-18-10-4-5-12-19(18)21/h4-7,9-15,17H,2-3,8,16H2,1H3",JDNLPKCAXICMBW-UHFFFAOYSA-N,Agonist,Full agonist,,,,,pKi,,8.0,,,,,,=,,,,10525107, CB1 receptor,56,P21554,Human,lenabasum,9772,,3083542,CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)C(=O)O)(C)C)(C)C,"InChI=1S/C25H36O4/c1-6-7-8-9-12-24(2,3)17-14-20(26)22-18-13-16(23(27)28)10-11-19(18)25(4,5)29-21(22)15-17/h10,14-15,18-19,26H,6-9,11-13H2,1-5H3,(H,27,28)/t18-,19-/m1/s1",YCHYFHOSGQABSW-RTBURBONSA-N,Agonist,Agonist,,,,,pKi,,7.49,,Ki,,32.3,,=,,,,23865723|9379442, CB1 receptor,56,P21554,Human,Sch.336,9799,,10324989,COc1ccc(c(c1)S(=O)(=O)c1ccc(cc1)OC)S(=O)(=O)c1ccc(cc1)[C@@H](NS(=O)(=O)C)C,"InChI=1S/C23H25NO8S3/c1-16(24-33(4,25)26)17-5-10-20(11-6-17)34(27,28)22-14-9-19(32-3)15-23(22)35(29,30)21-12-7-18(31-2)8-13-21/h5-16,24H,1-4H3/t16-/m0/s1",NXODIUKWAVUFGF-INIZCTEOSA-N,Agonist,Inverse agonist,,,,,pEC50,,6.7,,EC50,,200.0,,=,,,,16258021, CB1 receptor,56,P21554,Human,Sch.336,9799,,10324989,COc1ccc(c(c1)S(=O)(=O)c1ccc(cc1)OC)S(=O)(=O)c1ccc(cc1)[C@@H](NS(=O)(=O)C)C,"InChI=1S/C23H25NO8S3/c1-16(24-33(4,25)26)17-5-10-20(11-6-17)34(27,28)22-14-9-19(32-3)15-23(22)35(29,30)21-12-7-18(31-2)8-13-21/h5-16,24H,1-4H3/t16-/m0/s1",NXODIUKWAVUFGF-INIZCTEOSA-N,Agonist,Inverse agonist,,,,,pKi,,6.04,,Ki,,905.0,,=,,,,15664857, CB1 receptor,56,P21554,Human,AM6545,10029,,46912919,N#CCCC#Cc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCS(=O)(=O)CC1,"InChI=1S/C26H23Cl2N5O3S/c1-18-24(26(34)31-32-13-15-37(35,36)16-14-32)30-33(23-11-10-21(27)17-22(23)28)25(18)20-8-6-19(7-9-20)5-3-2-4-12-29/h6-11,17H,2,4,13-16H2,1H3,(H,31,34)",XBHQLFVDGLPBCK-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,8.48,,Ki,,3.3,,=,,,,25535367, CB1 receptor,56,P21554,Human,VCE-004.3,10030,,91972027,CCCCCNC1=C(CCCCC)C(=O)C(=O)C(=C1O)[C@@H]1C=C(C)CC[C@H]1C(=C)C,"InChI=1S/C26H39NO3/c1-6-8-10-12-20-23(27-15-11-9-7-2)25(29)22(26(30)24(20)28)21-16-18(5)13-14-19(21)17(3)4/h16,19,21,27,29H,3,6-15H2,1-2,4-5H3/t19-,21+/m0/s1",CIEWIZBPWBLHSB-PZJWPPBQSA-N,Antagonist,Antagonist,,,,,pKi,,5.61,,Ki,,2454.0,,=,,,,30033591, CB1 receptor,56,P21554,Human,olorinab,10058,,60164925,OC[C@H](C(C)(C)C)NC(=O)c1nn(c2c1C[C@H]1[C@@H]2C1)c1ncc[n+](c1)[O-],"InChI=1S/C18H23N5O3/c1-18(2,3)13(9-24)20-17(25)15-12-7-10-6-11(10)16(12)23(21-15)14-8-22(26)5-4-19-14/h4-5,8,10-11,13,24H,6-7,9H2,1-3H3,(H,20,25)/t10-,11-,13+/m0/s1",ACSQLTBPYZSGBA-GMXVVIOVSA-N,Agonist,Agonist,,,,,pEC50,,5.0,,EC50,,10000.0,,>,In a DiscoverX PathHunter β-arrestin recruitment assay.,,,29259753, CB1 receptor,56,P20272,Rat,olorinab,10058,,60164925,OC[C@H](C(C)(C)C)NC(=O)c1nn(c2c1C[C@H]1[C@@H]2C1)c1ncc[n+](c1)[O-],"InChI=1S/C18H23N5O3/c1-18(2,3)13(9-24)20-17(25)15-12-7-10-6-11(10)16(12)23(21-15)14-8-22(26)5-4-19-14/h4-5,8,10-11,13,24H,6-7,9H2,1-3H3,(H,20,25)/t10-,11-,13+/m0/s1",ACSQLTBPYZSGBA-GMXVVIOVSA-N,Agonist,Agonist,,,,,pEC50,,5.0,,EC50,,10000.0,,>,In a DiscoverX PathHunter β-arrestin recruitment assay.,,,29259753, CB1 receptor,56,P21554,Human,MDMB-Fubinaca,10178,,119025665,COC(=O)[C@H](C(C)(C)C)NC(=O)c1nn(c2c1cccc2)Cc1ccc(cc1)F,"InChI=1S/C22H24FN3O3/c1-22(2,3)19(21(28)29-4)24-20(27)18-16-7-5-6-8-17(16)26(25-18)13-14-9-11-15(23)12-10-14/h5-12,19H,13H2,1-4H3,(H,24,27)/t19-/m1/s1",RFCDVEHNYDVCMU-LJQANCHMSA-N,Agonist,Agonist,,,,,pKi,,10.01,,Ki,,0.098,,=,,,,29963207, CB1 receptor,56,P20272,Rat,AM1710,10202,,11268660,CCCCCCC(c1cc(O)c2c(c1)oc(=O)c1c2cc(OC)cc1)(C)C,"InChI=1S/C23H28O4/c1-5-6-7-8-11-23(2,3)15-12-19(24)21-18-14-16(26-4)9-10-17(18)22(25)27-20(21)13-15/h9-10,12-14,24H,5-8,11H2,1-4H3",ZAIKPEWFCSQNQB-UHFFFAOYSA-N,Agonist,Agonist,,,,,pKi,,6.44,,Ki,,360.0,,=,,,,18038967, CB1 receptor,56,P21554,Human,GAT211,10272,,4402318,[O-][N+](=O)CC(c1c([nH]c2c1cccc2)c1ccccc1)c1ccccc1,"InChI=1S/C22H18N2O2/c25-24(26)15-19(16-9-3-1-4-10-16)21-18-13-7-8-14-20(18)23-22(21)17-11-5-2-6-12-17/h1-14,19,23H,15H2",OHZDCJJHWPHZJD-UHFFFAOYSA-N,Allosteric modulator,Positive,,,,,,,,,,,,,=,,,,28103441, CB1 receptor,56,P21554,Human,BAY-593074,10348,,10479060,N#Cc1c(cccc1C(F)(F)F)Oc1cccc(c1)OS(=O)(=O)CCCC(F)(F)F,"InChI=1S/C18H13F6NO4S/c19-17(20,21)8-3-9-30(26,27)29-13-5-1-4-12(10-13)28-16-7-2-6-15(14(16)11-25)18(22,23)24/h1-2,4-7,10H,3,8-9H2",LWUSZIVDPJPVBW-UHFFFAOYSA-N,Agonist,Partial agonist,,,,,pKi,,7.32,,Ki,,48.3,,=,,,,15140913, CB1 receptor,56,P20272,Rat,BAY-593074,10348,,10479060,N#Cc1c(cccc1C(F)(F)F)Oc1cccc(c1)OS(=O)(=O)CCCC(F)(F)F,"InChI=1S/C18H13F6NO4S/c19-17(20,21)8-3-9-30(26,27)29-13-5-1-4-12(10-13)28-16-7-2-6-15(14(16)11-25)18(22,23)24/h1-2,4-7,10H,3,8-9H2",LWUSZIVDPJPVBW-UHFFFAOYSA-N,Agonist,Partial agonist,,,,,pKi,,7.26,,Ki,,55.4,,=,,,,15140913, CB1 receptor,56,P21554,Human,MRI-1867,10521,,132937648,Clc1ccc(cc1)C1=NN(C[C@@H]1c1ccccc1)/C(=N/S(=O)(=O)c1ccc(cc1)Cl)/N=C(\N)/C,"InChI=1S/C24H21Cl2N5O2S/c1-16(27)28-24(30-34(32,33)21-13-11-20(26)12-14-21)31-15-22(17-5-3-2-4-6-17)23(29-31)18-7-9-19(25)10-8-18/h2-14,22H,15H2,1H3,(H2,27,28,30)/t22-/m1/s1",GZPQTZIUWCQXCF-JOCHJYFZSA-N,Agonist,Inverse agonist,,,yes,,pKi,,8.64,,Ki,,2.3,,=,Measured in a radioligand displacement assay using [3H]-CP55940 as tracer and membranes from CB1R-expressing CHO-K1 cells.,,,27525312, CB1 receptor,56,P21554,Human,JD5037,10690,,66553204,Clc1ccc(cc1)C1=NN(C[C@@H]1c1ccccc1)/C(=N\[C@H](C(=O)N)C(C)C)/NS(=O)(=O)c1ccc(cc1)Cl,"InChI=1S/C27H27Cl2N5O3S/c1-17(2)24(26(30)35)31-27(33-38(36,37)22-14-12-21(29)13-15-22)34-16-23(18-6-4-3-5-7-18)25(32-34)19-8-10-20(28)11-9-19/h3-15,17,23-24H,16H2,1-2H3,(H2,30,35)(H,31,33)/t23-,24+/m1/s1",GTCSIQFTNPTSLO-RPWUZVMVSA-N,Antagonist,Antagonist,,,,,pKi,,9.46,,Ki,,0.35,,=,,,,22841573, CB1 receptor,56,P21554,Human,PF-514273,11693,,11316919,Clc1c(cccc1)n1nc2C(=O)N(CCOc2c1c1ccc(cc1)Cl)CC(C)(F)F,"InChI=1S/C21H17Cl2F2N3O2/c1-21(24,25)12-27-10-11-30-19-17(20(27)29)26-28(16-5-3-2-4-15(16)23)18(19)13-6-8-14(22)9-7-13/h2-9H,10-12H2,1H3",FJMQJSUOOGOWBD-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,9.09,,Ki,,0.82,,=,Antagonism of CP-55940-induced GTPgamma[35S] binding at CB1 expressed in CHOK1 cells,,,19351113, CB1 receptor,56,P20272,Rat,levonantradol,11818,,5361881,C[C@H]1[C@@H]2CC[C@H](C[C@H]2c2c(N1)cc(cc2OC(=O)C)O[C@H](C)CCCc1ccccc1)O,"InChI=1S/C27H35NO4/c1-17(8-7-11-20-9-5-4-6-10-20)31-22-15-25-27(26(16-22)32-19(3)29)24-14-21(30)12-13-23(24)18(2)28-25/h4-6,9-10,15-18,21,23-24,28,30H,7-8,11-14H2,1-3H3/t17-,18+,21-,23+,24-/m1/s1",FFVXQGMUHIJQAO-BFKQJKLPSA-N,Agonist,Agonist,,,,,pKi,,8.54,,Ki,,2.9,,=,,,,23865723, CB1 receptor,56,P21554,Human,AZD1940,12754,,11675994,C(C)(C)(C)C1=NC2=C(N1CC3CCC(CC3)(F)F)C=CC(=C2)NS(=O)(=O)CC,"InChI=1S/C20H29F2N3O2S/c1-5-28(26,27)24-15-6-7-17-16(12-15)23-18(19(2,3)4)25(17)13-14-8-10-20(21,22)11-9-14/h6-7,12,14,24H,5,8-11,13H2,1-4H3",ZAGGGZCIFUQHOH-UHFFFAOYSA-N,Agonist,Agonist,,,,,pKi,,7.93,,Ki,,11.7,,=,,,,30583970, CB1 receptor,56,P21554,Human,TM39875,13287,,,OC(=O)C1=C(N(N=C1C(=O)N2CCC(CC2)C3=C(F)C=CC=C3)C4=CC=CC=C4Cl)C5=CC=C(Cl)C=C5,"InChI=1S/C28H22Cl2FN3O3/c29-19-11-9-18(10-12-19)26-24(28(36)37)25(32-34(26)23-8-4-2-6-21(23)30)27(35)33-15-13-17(14-16-33)20-5-1-3-7-22(20)31/h1-12,17H,13-16H2,(H,36,37)",KXBFPNIMUCRAAB-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pIC50,,8.32,,IC50,,4.8,,=,Determined as antagonism in a GTPγS assay,,,38043690, CB1 receptor,56,P21554,Human,TM39875,13287,,,OC(=O)C1=C(N(N=C1C(=O)N2CCC(CC2)C3=C(F)C=CC=C3)C4=CC=CC=C4Cl)C5=CC=C(Cl)C=C5,"InChI=1S/C28H22Cl2FN3O3/c29-19-11-9-18(10-12-19)26-24(28(36)37)25(32-34(26)23-8-4-2-6-21(23)30)27(35)33-15-13-17(14-16-33)20-5-1-3-7-22(20)31/h1-12,17H,13-16H2,(H,36,37)",KXBFPNIMUCRAAB-UHFFFAOYSA-N,Antagonist,Inverse agonist,,,,,pIC50,,7.29,,IC50,,51.0,,=,Determined in a GTPγS assay,,,38043690,