WIN55212-2 [Ligand Id: 733] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL188 (WIN-55212-2)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Mouse [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
  • CB2 receptor/Cannabinoid CB2 receptor in Rat [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
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  • glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
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  • glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Binding affinity towards cloned human Cannabinoid receptor 1 B 0.28 pKi 0.28 nM Log Ki J. Med. Chem. (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells B 5.42 pKi 3802 nM Ki J. Med. Chem. (2005) 48: 2509-2517 [PMID:15801840]
ChEMBL Displacement of [3H]SR141716A from human CB1 receptor B 5.42 pKi 3802 nM Ki J. Med. Chem. (2006) 49: 872-882 [PMID:16451053]
ChEMBL Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells B 5.42 pKi 3800 nM Ki J. Med. Chem. (2005) 48: 7486-7490 [PMID:16279809]
ChEMBL Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W5 43(280)A mutant Cannabinoid receptor 1 at 5 uM B 6.7 pKi 199 nM Ki J. Med. Chem. (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes B 6.82 pKi 152.2 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 2233-2236 [PMID:10465552]
ChEMBL Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins B 6.82 pKi 150 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor B 6.85 pKi 140 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 3695-3700 [PMID:18522867]
ChEMBL Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.36 (201)A mutant Cannabinoid receptor 1 B 6.97 pKi 107 nM Ki J. Med. Chem. (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells B 7.02 pKi 94.5 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting B 7.1 pKi 79.43 nM Ki Eur. J. Med. Chem. (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in CHO cells membrane by scintillation counting B 7.28 pKi 52.4 nM Ki J. Med. Chem. (2012) 55: 8948-8952 [PMID:23017078]
ChEMBL Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by scintillation counting B 7.28 pKi 52.4 nM Ki Eur. J. Med. Chem. (2012) 58: 396-404 [PMID:23151320]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor after 1 hr by scintillation counting analysis B 7.28 pKi 52.4 nM Ki ACS Med. Chem. Lett. (2015) 6: 198-203 [PMID:25699149]
ChEMBL Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells B 7.34 pKi 46 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 3884-3889 [PMID:22607668]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation counting method B 7.34 pKi 45.6 nM Ki J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting B 7.34 pKi 45.6 nM Ki Eur. J. Med. Chem. (2013) 70: 111-119 [PMID:24141201]
ChEMBL Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer B 7.34 pKi 45.6 nM Ki J. Med. Chem. (2016) 59: 1840-1853 [PMID:26789378]
ChEMBL Displacement of [3H]-CP55940 from CB1 receptor after 90 mins by liquid scintillation counting B 7.34 pKi 45.6 nM Ki ACS Med. Chem. Lett. (2011) 2: 793-797 [PMID:24936232]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor after 90 mins by liquid scintillation spectrophotometer analysis B 7.34 pKi 45.59 nM Ki Bioorg. Med. Chem. (2013) 21: 1708-1716 [PMID:23434135]
ChEMBL Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W6 48(357)A mutant Cannabinoid receptor 1 B 7.35 pKi 45 nM Ki J. Med. Chem. (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL Binding affinity to human CB1 receptor B 7.39 pKi 40.9 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6183-6187 [PMID:17884494]
ChEMBL Binding affinity against human Cannabinoid receptor 1 expressed in CHO cells by using CP-55940 as Radioactive tracer B 7.4 pKi 40 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 2399-2402 [PMID:12161142]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis B 7.44 pKi 36.2 nM Ki Eur. J. Med. Chem. (2014) 73: 56-72 [PMID:24378710]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis B 7.44 pKi 36.2 nM Ki Eur. J. Med. Chem. (2015) 101: 651-667 [PMID:26209834]
ChEMBL Displacement of [3H]CP55940 from human CB1R transfected in HEK293EBNA cell membranes incubated for 90 mins by Microbeta TriLux based luminescence analysis B 7.44 pKi 36.2 nM Ki Bioorg Med Chem (2020) 28: 115672-115672 [PMID:32912440]
ChEMBL Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation and luminescence counting method B 7.54 pKi 28.8 nM Ki Eur J Med Chem (2017) 127: 398-412 [PMID:28088085]
ChEMBL Displacement of [3H]CP,55-940 from recombinant human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method B 7.54 pKi 28.8 nM Ki Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells B 7.64 pKi 23 nM Ki J. Nat. Prod. (2001) 64: 1322-1325 [PMID:11678659]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS cells B 7.68 pKi 21 nM Ki J. Med. Chem. (2005) 48: 7343-7350 [PMID:16279794]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells B 7.68 pKi 21 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6505-6510 [PMID:17942307]
ChEMBL Binding affinity to human recombinant CB1 receptor expressed in african green monkey COS cells by radioligand binding assay B 7.68 pKi 21 nM Ki J. Med. Chem. (2009) 52: 2506-2514 [PMID:19331413]
ChEMBL Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK cell membrane B 7.68 pKi 21 nM Ki Bioorg Med Chem (2020) 28: 115513-115513 [PMID:32340793]
ChEMBL Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes B 7.68 pKi 21 nM Ki Bioorg. Med. Chem. (2014) 22: 4770-4783 [PMID:25065940]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells B 7.68 pKi 21 nM Ki Bioorg. Med. Chem. (2007) 15: 5406-5416 [PMID:17561406]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor B 7.68 pKi 21 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 138-141 [PMID:16213718]
ChEMBL Displacement of [3H]CP55940 from human CB1 receptor expressed in human HEK293 cells B 7.7 pKi 20 nM Ki J. Med. Chem. (2011) 54: 8278-8288 [PMID:22044209]
ChEMBL Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis B 7.72 pKi 19 nM Ki Eur J Med Chem (2019) 165: 347-362 [PMID:30583970]
ChEMBL Binding affinity to human CB1 receptor B 7.79 pKi 16.1 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 1322-1326 [PMID:24508127]
ChEMBL Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.25 (190)A mutant Cannabinoid receptor 1 B 7.82 pKi 15 nM Ki J. Med. Chem. (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor B 7.85 pKi 14 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4030-4034 [PMID:17521907]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells B 7.88 pKi 13.3 nM Ki J. Med. Chem. (2010) 53: 295-315 [PMID:19921781]
ChEMBL Displacement of [3H]CP 55940 from human CB1 receptor in cell free system B 7.88 pKi 13.3 nM Ki Eur. J. Med. Chem. (2011) 46: 547-555 [PMID:21183257]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells B 7.88 pKi 13.3 nM Ki J. Med. Chem. (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells B 7.88 pKi 13.18 nM Ki J. Med. Chem. (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells B 7.88 pKi 13.18 nM Ki J. Med. Chem. (2010) 53: 295-315 [PMID:19921781]
ChEMBL Displacement of [3H]-CP55940 from human cannabinoid CB1 receptor expressed in Sf9 insect cells after 70 mins by scintillation counting B 7.9 pKi 12.59 nM Ki MedChemComm (2010) 1: 54-60
ChEMBL Displacement of [3H]-CP55940 from human CB1 expressed in insect Sf9 membranes B 7.9 pKi 12.59 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7327-7330 [PMID:21074434]
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in insect Sf9 cells B 7.9 pKi 12.59 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1748-1753 [PMID:21316962]
ChEMBL Displacement of [3H]CP-55,940 from human CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis B 7.9 pKi 12.5 nM Ki Eur. J. Med. Chem. (2016) 113: 11-27 [PMID:26922225]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cell membranes incubated for 90 mins by scintillation counting B 7.91 pKi 12.4 nM Ki J. Med. Chem. (2012) 55: 6608-6623 [PMID:22738271]
ChEMBL Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with wild type Cannabinoid receptor 1 B 7.92 pKi 12 nM Ki J. Med. Chem. (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis B 7.95 pKi 11.3 nM Ki J. Med. Chem. (2013) 56: 1098-1112 [PMID:23350768]
ChEMBL Displacement of [3H]-CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cells membrane incubated for 90 mins B 8.04 pKi 9.2 nM Ki J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
ChEMBL Displacement of [3H]CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins B 8.04 pKi 9.2 nM Ki J. Nat. Prod. (2011) 74: 2313-2317 [PMID:21999614]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins B 8.04 pKi 9.2 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 1210-1213 [PMID:20022504]
ChEMBL Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by scintillation counting analysis B 8.06 pKi 8.8 nM Ki J. Nat. Prod. (2015) 78: 1671-1682 [PMID:26149623]
ChEMBL Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB1 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis B 8.06 pKi 8.72 nM Ki MedChemComm (2017) 8: 1697-1705 [PMID:30108881]
ChEMBL Binding affinity to human cannabinoid CB1 receptor B 8.22 pKi 6.06 nM Ki Bioorg. Med. Chem. (2009) 17: 2842-2851 [PMID:19278853]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cell membranes after 90 mins B 8.6 pKi 2.5 nM Ki Eur J Med Chem (2018) 154: 155-171 [PMID:29793210]
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in CHO-K1 cells by liquid scintillation counting B 8.6 pKi 2.5 nM Ki Eur. J. Med. Chem. (2014) 85: 77-86 [PMID:25072877]
ChEMBL Displacement of [3H]CP55940 from recombinant human CB1R expressed in CHO cell membranes incubated for 90 mins B 8.6 pKi 2.5 nM Ki Eur J Med Chem (2020) 208: 112858-112858 [PMID:33002735]
ChEMBL Compound was evaluated for its binding affinity against Cannabinoid receptor 1 in Guinea pig ileum (GPI) using [3H]CP-55940 ligand B 8.61 pKi 2.48 nM Ki J. Med. Chem. (1998) 41: 5177-5187 [PMID:9857088]
GtoPdb - - 8.7 pKi - - - Mol Pharmacol (1995) 48: 443-50 [PMID:7565624];
J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477];
Biochim Biophys Acta (1996) 1307: 132-6 [PMID:8679694]
ChEMBL Binding affinity of compound was determined against to human cannabinoid receptor 1 in chinese hamster ovary cells B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2003) 46: 2110-2116 [PMID:12747783]
ChEMBL Binding affinity to CB1 receptor B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2008) 51: 5019-5034 [PMID:18680277]
ChEMBL Binding affinity to CB1 receptor (unknown origin) B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2013) 56: 7161-7176 [PMID:23672690]
ChEMBL Binding affinity to human CB1 receptor by filtration assay B 8.72 pKi 1.9 nM Ki Bioorg. Med. Chem. (2012) 20: 2067-2081 [PMID:22341572]
ChEMBL Binding affinity to CB1 receptor (unknown origin) B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Binding affinity to CB1 receptor (unknown origin) B 8.72 pKi 1.9 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 2019-2021 [PMID:23466226]
ChEMBL Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins B 6.7 pIC50 200 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells B 6.85 pIC50 140 nM IC50 J. Med. Chem. (2007) 50: 3851-3856 [PMID:17630726]
ChEMBL Binding affinity to human recombinant CB1 receptor B 7.2 pIC50 63.1 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 272-277 [PMID:17027269]
ChEMBL Displacement of [3H]-CP55,940 from human CB1 receptor expressed in HEK293S cell membranes by scintillation counting analysis B 7.23 pIC50 59 nM IC50 J. Med. Chem. (2013) 56: 220-240 [PMID:23227781]
ChEMBL Agonist activity at human CB1 in CHO cells assessed as inhibition of cAMP production F 7.77 pIC50 17 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4030-4034 [PMID:17521907]
ChEMBL Inhibition of human cannabinoid CB1 receptor B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Agonist activity at CB1 receptor F 8.7 pIC50 2 nM IC50 Eur. J. Med. Chem. (2008) 43: 513-539 [PMID:17582659]
ChEMBL Agonist activity at human CB1 receptor transfected in human U2OS cells assessed as beta-arrestin2-GFP aggregation after 40 mins B 5.75 pEC50 1760 nM EC50 J. Med. Chem. (2013) 56: 3904-3921 [PMID:23621789]
ChEMBL Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay F 6.5 pEC50 316.23 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 272-277 [PMID:17027269]
ChEMBL Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding F 6.95 pEC50 112 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 3884-3889 [PMID:22607668]
ChEMBL Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay B 6.96 pEC50 110 nM EC50 J. Med. Chem. (2013) 56: 220-240 [PMID:23227781]
ChEMBL Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay F 7.3 pEC50 50.12 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 7327-7330 [PMID:21074434]
ChEMBL Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay F 7.3 pEC50 50.12 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1748-1753 [PMID:21316962]
ChEMBL Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay B 7.3 pEC50 50.12 nM EC50 MedChemComm (2010) 1: 54-60
ChEMBL Agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method F 7.36 pEC50 44 nM EC50 J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL Displacement of [3H]WIN-55212-2 from human CB1 receptor in HEK293 cells B 7.42 pEC50 37.6 nM EC50 J. Nat. Prod. (2006) 69: 432-435 [PMID:16562853]
ChEMBL Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production F 7.43 pEC50 37 nM EC50 J. Med. Chem. (2010) 53: 295-315 [PMID:19921781]
ChEMBL Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release F 7.5 pEC50 31.62 nM EC50 Eur. J. Med. Chem. (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay F 7.5 pEC50 31.62 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL Agonist activity at CB1 receptor (unknown origin) assessed as increase in cAMP accumulation after 1 hr by FLIPR assay F 7.8 pEC50 16 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation F 7.91 pEC50 12.3 nM EC50 J. Med. Chem. (2007) 50: 3851-3856 [PMID:17630726]
ChEMBL Agonist activity at CB1 receptor (unknown origin) assessed as increase in beta-arrestin2 recruitment after 20 mins by BRET-based luciferase reporter gene assay B 8.14 pEC50 7.2 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
ChEMBL Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [3H]SR-141,716A B 7.7 pKi 20 nM Ki J. Med. Chem. (2005) 48: 6386-6392 [PMID:16190764]
ChEMBL Displacement of [3H]CP-55940 from mouse CB1 receptor B 8.15 pKi 7 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4030-4034 [PMID:17521907]
ChEMBL Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [131I]-(R)-8 B 8.8 pKi 1.6 nM Ki J. Med. Chem. (2005) 48: 6386-6392 [PMID:16190764]
ChEMBL Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction F 5.84 pEC50 1450 nM EC50 Bioorg. Med. Chem. (2007) 15: 7480-7493 [PMID:17870539]
ChEMBL Activity at CB1 receptor assessed as stimulation of [35S]GTP-gamma-S binding in DBA/J2 mouse brain F 6.69 pEC50 204 nM EC50 J. Med. Chem. (2006) 49: 5947-5957 [PMID:17004710]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Displacement of [3H]-CP55940 from CB1 receptor in rat brain homogenate after 1.5 hrs by microbeta liquid scintillation counting analysis B 7.44 pKi 36 nM Ki Eur. J. Med. Chem. (2013) 69: 881-907 [PMID:24125850]
ChEMBL Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat brain by scintillation counting B 7.81 pKi 15.6 nM Ki J. Med. Chem. (2012) 55: 6608-6623 [PMID:22738271]
ChEMBL Displacement of [3H]CP-55,940 from Sprague-Dawley rat brain CB1 receptor by scintillation counting analysis B 7.84 pKi 14.4 nM Ki J. Med. Chem. (2013) 56: 1098-1112 [PMID:23350768]
ChEMBL Binding affinity for cannabinoid receptor 1 B 8 pKi 9.9 nM Ki J. Med. Chem. (2005) 48: 5059-5087 [PMID:16078824]
ChEMBL Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain cortical membrane B 8.22 pKi 6.06 nM Ki Bioorg. Med. Chem. (2009) 17: 2842-2851 [PMID:19278853]
ChEMBL Binding affinity to CB1 cannabinoid receptor using [3H]WIN-55212-2 in rat cerebellum membranes B 8.35 pKi 4.5 nM Ki J. Med. Chem. (2001) 44: 4505-4508 [PMID:11741470]
ChEMBL Binding affinity to displace [3H]CP-55940 from CB1 receptor of rat brain B 8.72 pKi 1.9 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4110-4113 [PMID:16005223]
ChEMBL Displacement of [3H]SR141716A from CB1 receptor in Sprague-Dawley rat cerebellum membrane B 6.37 pIC50 430 nM IC50 Eur. J. Med. Chem. (2008) 43: 513-539 [PMID:17582659]
ChEMBL Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay F 8 pEC50 10 nM EC50 J. Med. Chem. (2010) 53: 295-315 [PMID:19921781]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Binding affinity towards cloned human cannabinoid receptor 2 B 0.55 pKi 0.55 nM Log Ki J. Med. Chem. (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL Displacement of [3H]CP-55,940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells B 7.15 pKi 70 nM Ki Bioorg. Med. Chem. (2013) 21: 7481-7498 [PMID:24139843]
ChEMBL Displacement of [3H]CP-55940 from human CB2 receptor B 7.7 pKi 20 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 3695-3700 [PMID:18522867]
ChEMBL Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting B 7.79 pKi 16.1 nM Ki Bioorg. Med. Chem. (2013) 21: 5383-5394 [PMID:23849204]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cells after 1.5 hrs by microbeta liquid scintillation counting analysis B 7.89 pKi 13 nM Ki Eur. J. Med. Chem. (2013) 69: 881-907 [PMID:24125850]
ChEMBL Displacement of [3H]CP-55940 from human CB2 receptor B 8.04 pKi 9.1 nM Ki J. Med. Chem. (2006) 49: 70-79 [PMID:16392793]
ChEMBL Binding affinity to human CB2 receptor B 8.04 pKi 9.1 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 1322-1326 [PMID:24508127]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells after 1 hr B 8.04 pKi 9.1 nM Ki J. Med. Chem. (2010) 53: 7918-7931 [PMID:20979417]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells B 8.04 pKi 9.1 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL Displacement of [3H]-CP55,940 from human CB2 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting B 8.04 pKi 9.1 nM Ki Bioorg. Med. Chem. (2013) 21: 5383-5394 [PMID:23849204]
ChEMBL Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB2 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis B 8.07 pKi 8.57 nM Ki MedChemComm (2017) 8: 1697-1705 [PMID:30108881]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells by liquid scintillation counting B 8.2 pKi 6.31 nM Ki Eur. J. Med. Chem. (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL Displacement of [3H]CP-55,940 from human recombinant CB2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting analysis B 8.31 pKi 4.95 nM Ki J. Med. Chem. (2013) 56: 1098-1112 [PMID:23350768]
ChEMBL Displacement of [3H]CP-55,940 from human CB2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting analysis B 8.34 pKi 4.6 nM Ki Eur. J. Med. Chem. (2016) 113: 11-27 [PMID:26922225]
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ChEMBL Binding affinity against human Cannabinoid receptor 2 expressed in CHO cells by using WIN-55212-2 Mesylate [573H] as Radioactive tracer B 8.4 pKi 4 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 2399-2402 [PMID:12161142]
ChEMBL Binding affinity to human CB2 cannabinoid receptor using [3H]CP-55940 in HEK293 EBNA transfected cells B 8.41 pKi 3.9 nM Ki J. Med. Chem. (2001) 44: 4505-4508 [PMID:11741470]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor after 90 mins by liquid scintillation spectrophotometer analysis B 8.43 pKi 3.73 nM Ki Bioorg. Med. Chem. (2013) 21: 1708-1716 [PMID:23434135]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis B 8.43 pKi 3.7 nM Ki Eur. J. Med. Chem. (2015) 101: 651-667 [PMID:26209834]
ChEMBL Displacement of [3H]CP55940 from human CB2R transfected in HEK293EBNA cell membrane incubated for 90 mins by Microbeta TriLux based luminescence analysis B 8.43 pKi 3.7 nM Ki Bioorg Med Chem (2020) 28: 115672-115672 [PMID:32912440]
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ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis B 8.43 pKi 3.7 nM Ki Eur. J. Med. Chem. (2014) 73: 56-72 [PMID:24378710]
ChEMBL Displacement of [3H]CP55940 from human CB2 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer B 8.43 pKi 3.7 nM Ki J. Med. Chem. (2016) 59: 1840-1853 [PMID:26789378]
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting B 8.43 pKi 3.7 nM Ki Eur. J. Med. Chem. (2013) 70: 111-119 [PMID:24141201]
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ChEMBL Displacement of [3H]CP,55-940 from recombinant human CB2 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method B 8.43 pKi 3.7 nM Ki Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor after 1 hr by scintillation counting analysis B 8.51 pKi 3.1 nM Ki ACS Med. Chem. Lett. (2015) 6: 198-203 [PMID:25699149]
ChEMBL Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by scintillation counting B 8.51 pKi 3.1 nM Ki Eur. J. Med. Chem. (2012) 58: 396-404 [PMID:23151320]
ChEMBL Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in CHO cells membrane by scintillation counting B 8.51 pKi 3.1 nM Ki J. Med. Chem. (2012) 55: 8948-8952 [PMID:23017078]
ChEMBL Displacement of [3H]-CP-55940 from human CB2 expressed in CHO cells after 90 mins by TopCount scintillation counting method B 8.52 pKi 3.01 nM Ki Eur J Med Chem (2018) 146: 68-78 [PMID:29360044]
ChEMBL Binding affinity to human CB2 receptor B 8.54 pKi 2.9 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6183-6187 [PMID:17884494]
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in insect Sf9 cells B 8.6 pKi 2.51 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1748-1753 [PMID:21316962]
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ChEMBL Displacement of [3H]-CP55940 from human cannabinoid CB2 receptor expressed in Sf9 insect cells after 70 mins by scintillation counting B 8.6 pKi 2.51 nM Ki MedChemComm (2010) 1: 54-60
ChEMBL Displacement of [3H]CP-55940 from human CB2 receptor B 8.66 pKi 2.2 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4030-4034 [PMID:17521907]
ChEMBL Displacement of [3H]CP-55940 from human CB2 receptor expressed in COS cells B 8.68 pKi 2.1 nM Ki J. Med. Chem. (2005) 48: 7343-7350 [PMID:16279794]
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ChEMBL Displacement of [3H]-CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cells membrane incubated for 90 mins B 8.68 pKi 2.1 nM