[3H]CP55940 [Ligand Id: 734] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL559612 (CP-55940)
  • 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]
1 CHEMBL559612_lig_chart_1 Cannabinoid CB1 receptor HumanMouseRat
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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]
2 CHEMBL559612_lig_chart_2 Cannabinoid CB2 receptor HumanMouseRat
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  • GPR55/G-protein coupled receptor 55 in Human [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6]
  • This target only has 0 pki data point
3 CHEMBL559612_lig_chart_3 G-protein coupled receptor 55 Human
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  • GPR18/N-arachidonyl glycine receptor in Human [ChEMBL: CHEMBL2384898] [GtoPdb: 89] [UniProtKB: Q14330]
  • This target only has 0 pki data point
4 CHEMBL559612_lig_chart_4 N-arachidonyl glycine receptor Human
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
5 CHEMBL559612_lig_chart_5 Plasmodium falciparum Plasmodium falciparum
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  • TRPV1/Vanilloid receptor in Human [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
  • This target only has 0 pki data point
6 CHEMBL559612_lig_chart_6 Vanilloid receptor Human
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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 to human CB1 receptor expressed in CHOK1 cells B 9.3 pKd 0.5 nM Kd Bioorg Med Chem (2017) 25: 6102-6114 [PMID:28284861]
GtoPdb - - 9.4 pKd - - - J. Biol. Chem. (1995) 270: 13973-80 [PMID:7775459];
J. Pharmacol. Exp. Ther. (1996) 278: 989-99 [PMID:8819477];
Biochem. J. (1995) 312 ( Pt 2): 637-41 [PMID:8526880];
Biochem. J. (1991) 279 ( Pt 1): 129-34 [PMID:1718258];
Mol. Pharmacol. (1992) 42: 838-45 [PMID:1331766];
J. Biol. Chem. (1996) 271: 6941-6 [PMID:8636122]
ChEMBL Binding affinity towards cloned human Cannabinoid receptor 1 B 0.19 pKi -0.19 nM Log Ki J. Med. Chem. (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor B 7.89 pKi 13 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 138-141 [PMID:16213718]
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 8.03 pKi 9.26 nM Ki MedChemComm (2017) 8: 1697-1705
ChEMBL Compound was evaluated for affinity towards human Cannabinoid receptor 1 using [3H]- SR-141716A as radioligand B 8.28 pKi 5.2 nM Ki J. Med. Chem. (2002) 45: 1748-1756 [PMID:11960486]
ChEMBL Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes B 8.28 pKi 5.2 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 2233-2236 [PMID:10465552]
ChEMBL Binding affinity to human cannabinoid CB1 receptor B 8.86 pKi 1.37 nM Ki Bioorg. Med. Chem. (2009) 17: 2842-2851 [PMID:19278853]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells B 8.87 pKi 1.36 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting B 8.89 pKi 1.28 nM Ki ACS Med. Chem. Lett. (2013) 4: 41-45 [PMID:24900561]
ChEMBL Displacement of [3H]CP55,940 from human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter B 8.89 pKi 1.28 nM Ki J. Med. Chem. (2012) 55: 7967-7977 [PMID:22916707]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting B 8.9 pKi 1.26 nM Ki Eur. J. Med. Chem. (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL Displacement of radiolabeled CP-55940 from human CB1 receptor B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Agonist activity at recombinant human full length CB1 receptor expressed in HEK293 cell membranes after 2 hrs by [35S]GTP-gammaS binding assay F 9.15 pKi 0.7 nM Ki Eur J Med Chem (2018) 143: 983-996 [PMID:29232588]
ChEMBL Displacement of [3H]CP 55940 from human CB1 receptor in cell free system B 9.22 pKi 0.6 nM Ki Eur. J. Med. Chem. (2011) 46: 547-555 [PMID:21183257]
ChEMBL Binding affinity to human CB1 receptor B 9.24 pKi 0.58 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Binding affinity to cannabinoid CB1 receptor B 9.24 pKi 0.58 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in CHO-K1 cells by liquid scintillation counting B 9.28 pKi 0.52 nM Ki Eur. J. Med. Chem. (2014) 85: 77-86 [PMID:25072877]
ChEMBL Displacement of [3H]CP-55,940 from recombinant human full length CB1 receptor expressed in HEK293 cell membranes after 90 mins by topcount method B 9.3 pKi 0.5 nM Ki Eur J Med Chem (2018) 143: 983-996 [PMID:29232588]
ChEMBL Displacement of [3H]-CP55940 from human cannabinoid CB1 receptor expressed in Sf9 insect cells after 70 mins by scintillation counting B 9.5 pKi 0.32 nM Ki MedChemComm (2010) 1: 54-60
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in insect Sf9 cells B 9.5 pKi 0.32 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1748-1753 [PMID:21316962]
ChEMBL Displacement of [3H]-CP55940 from human CB1 expressed in insect Sf9 membranes B 9.5 pKi 0.32 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7327-7330 [PMID:21074434]
ChEMBL Binding affinity to human CB1 receptor by radioligand displacement assay B 9.57 pKi 0.27 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes in presence of agonist 5'-guanylyimidodiphosphate 50 uM B 7.56 pIC50 27.5 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 2233-2236 [PMID:10465552]
ChEMBL Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes in absence of agonist 5''-guanylyimidodiphosphate B 7.84 pIC50 14.4 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 2233-2236 [PMID:10465552]
ChEMBL Binding affinity to human recombinant CB1 receptor B 8.6 pIC50 2.51 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 272-277 [PMID:17027269]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells B 8.68 pIC50 2.1 nM IC50 Bioorg. Med. Chem. (2008) 16: 1111-1124 [PMID:18006322]
ChEMBL Displacement of [3H]CP-55940 form human CB1 receptor expressed in CHO cells B 8.68 pIC50 2.1 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6299-6304 [PMID:17884496]
ChEMBL Displacement of radiolabeled CP-55940 from human CB1 receptor B 8.85 pIC50 1.4 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]CP 55940 from human recombinant CB1 receptor expressed in CHO cells B 9.05 pIC50 0.9 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [3H]CP 55940 from human recombinant CB1 receptor expressed in CHO cells measured after 120 mins by scintillation counting method B 9.05 pIC50 0.9 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells B 9.11 pIC50 0.77 nM IC50 J. Med. Chem. (2007) 50: 3851-3856 [PMID:17630726]
ChEMBL Binding affinity to human CB1 receptor by radioligand displacement assay B 9.51 pIC50 0.31 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity to human CB1 receptor by radioligand displacement assay B 9.68 pIC50 0.21 nM IC50 Bioorg. Med. Chem. (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins F 9.89 pIC50 0.13 nM IC50 Eur. J. Med. Chem. (2010) 45: 1133-1139 [PMID:20047779]
ChEMBL Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay F 6.8 pEC50 158.49 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 272-277 [PMID:17027269]
ChEMBL Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay F 7.52 pEC50 30.02 nM EC50 Eur J Med Chem (2017) 137: 598-611 [PMID:28651225]
ChEMBL Agonist activity at CB1 receptor F 7.6 pEC50 25.12 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 2932-2937 [PMID:22421020]
ChEMBL Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay F 7.7 pEC50 19.95 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 7327-7330 [PMID:21074434]
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 7.7 pEC50 19.95 nM EC50 MedChemComm (2010) 1: 54-60
ChEMBL Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay F 7.7 pEC50 19.95 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1748-1753 [PMID:21316962]
ChEMBL Agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay B 7.89 pEC50 12.88 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4209-4214 [PMID:25096297]
ChEMBL Agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Galpha i2 assessed as Galpha GTPase activity using [gamma-33P]GTP by scintillation counting B 7.89 pEC50 12.88 nM EC50 Bioorg. Med. Chem. (2014) 22: 3938-3946 [PMID:24984935]
ChEMBL Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assay F 7.99 pEC50 10.3 nM EC50 J. Med. Chem. (2009) 52: 433-444 [PMID:19115816]
ChEMBL Agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay B 8.1 pEC50 8 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4209-4214 [PMID:25096297]
ChEMBL Agonist activity at CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as increase in intracellular calcium level by microplate reader based assay B 8.1 pEC50 7.93 nM EC50 J. Med. Chem. (2015) 58: 5751-5769 [PMID:26151231]
ChEMBL Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells by calcium mobilization assay F 8.15 pEC50 7 nM EC50 Eur. J. Med. Chem. (2015) 93: 16-32 [PMID:25644673]
ChEMBL Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay F 8.26 pEC50 5.5 nM EC50 Eur J Med Chem (2018) 154: 155-171 [PMID:29793210]
ChEMBL Agonist activity at human CB1 receptor expressed in CHO cells by [35S]GTPgammaS assay F 8.3 pEC50 5 nM EC50 J. Med. Chem. (2008) 51: 4932-4947 [PMID:18666769]
ChEMBL Positive allosteric modulator activity at human CB1R expressed in CHO cells assessed as enhanced binding of [3H]CP55,940 after 60 mins by liquid scintillation spectrometric analysis B 8.31 pEC50 4.9 nM EC50 J. Med. Chem. (2016) 59: 44-60 [PMID:26529344]
ChEMBL Partial agonist activity at human cannabinoid CB1 receptor expressed in CHO-K1 cells assessed as [S35]GTPgammaS binding by scintillation counting B 8.41 pEC50 3.9 nM EC50 Eur. J. Med. Chem. (2014) 85: 77-86 [PMID:25072877]
ChEMBL Agonist activity at recombinant human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 5 mins by cAMP-competition binding assay F 8.64 pEC50 2.28 nM EC50 ACS Med. Chem. Lett. (2013) 4: 41-45 [PMID:24900561]
ChEMBL Agonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assay B 8.64 pEC50 2.28 nM EC50 J. Med. Chem. (2008) 51: 5019-5034 [PMID:18680277]
ChEMBL Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation using [3H]-cAMP after 5 mins by liquid scintillation counter F 8.64 pEC50 2.28 nM EC50 J. Med. Chem. (2012) 55: 7967-7977 [PMID:22916707]
ChEMBL Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay F 8.84 pEC50 1.43 nM EC50 Bioorg. Med. Chem. (2014) 22: 4770-4783 [PMID:25065940]
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 8.9 pEC50 1.26 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay F 9.05 pEC50 0.9 nM EC50 J Med Chem (2018) 61: 5569-5579 [PMID:29856219]
ChEMBL Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assay F 9.15 pEC50 0.7 nM EC50 Eur. J. Med. Chem. (2012) 58: 30-43 [PMID:23085772]
ChEMBL Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release F 9.2 pEC50 0.63 nM EC50 Eur. J. Med. Chem. (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation B 9.36 pEC50 0.44 nM EC50 J. Med. Chem. (2015) 58: 5979-5988 [PMID:26203658]
ChEMBL Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation F 9.55 pEC50 0.28 nM EC50 J. Med. Chem. (2007) 50: 3851-3856 [PMID:17630726]
ChEMBL Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level F 9.59 pEC50 0.26 nM EC50 J. Med. Chem. (2008) 51: 5019-5034 [PMID:18680277]
CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
ChEMBL Displacement of [3H]CP-55940 from CD1 mouse brain CB1 receptor B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2006) 49: 7502-7512 [PMID:17149879]
ChEMBL Displacement of [3H]-CP55,940 from CB1 receptor in mouse whole brain membranes after 60 mins by liquid scintillation spectrometry B 9.21 pKi 0.62 nM Ki Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL Agonist activity at MF1 mouse brain CB1 receptor assessed as induction of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting F 7.38 pEC50 42 nM EC50 J. Med. Chem. (2011) 54: 8278-8288 [PMID:22044209]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Displacement of [3H]SR14716 from CB1 receptor in Rattus norvegicus (rat) cerebellum homogenate after 2 hr by scintillation counting B 8.11 pKi 7.7 nM Ki Med Chem Res (2012) 21: 4473-4484
ChEMBL Binding affinity for cannabinoid receptor 1 B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2005) 48: 5059-5087 [PMID:16078824]
ChEMBL Binding affinity to CB1 cannabinoid receptor using [3H]WIN-55212-2 in rat cerebellum membranes B 8.89 pKi 1.3 nM Ki J. Med. Chem. (2001) 44: 4505-4508 [PMID:11741470]
ChEMBL Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain cortical membrane B 8.91 pKi 1.24 nM Ki Bioorg. Med. Chem. (2009) 17: 2842-2851 [PMID:19278853]
ChEMBL Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat brain membrane B 9.24 pKi 0.58 nM Ki Bioorg. Med. Chem. (2008) 16: 322-335 [PMID:17919913]
ChEMBL Displacement of [3H]BMS-725519 from rat brain CB1 receptor after 90 mins by scintillation counting B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6856-6860 [PMID:21962575]
ChEMBL Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor F 7 pEC50 100 nM EC50 J. Med. Chem. (2006) 49: 554-566 [PMID:16420041]
ChEMBL Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels F 8.52 pEC50 3 nM EC50 Bioorg Med Chem (2018) 26: 4963-4970 [PMID:30122284]
ChEMBL Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level F 9.8 pEC50 0.16 nM EC50 J. Med. Chem. (2008) 51: 5019-5034 [PMID:18680277]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Binding affinity to human CB2 receptor expressed in CHOK1 cells B 9.23 pKd 0.59 nM Kd Bioorg Med Chem (2017) 25: 6102-6114 [PMID:28284861]
GtoPdb - - 9.7 pKd - - - 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];
J. Biol. Chem. (1996) 271: 6941-6 [PMID:8636122];
Nature (1993) 365: 61-5 [PMID:7689702];
Eur. J. Biochem. (1996) 237: 704-11 [PMID:8647116]
ChEMBL Binding affinity towards cloned human cannabinoid receptor 2 B 0.01 pKi -0.01 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 7.57 pKi 27 nM Ki Bioorg. Med. Chem. (2013) 21: 7481-7498 [PMID:24139843]
ChEMBL Displacement of [3H]CP-55940 from human CB2 receptor B 7.81 pKi 15.4 nM Ki J. Med. Chem. (2006) 49: 70-79 [PMID:16392793]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells after 1 hr B 7.81 pKi 15.4 nM Ki J. Med. Chem. (2010) 53: 7918-7931 [PMID:20979417]
ChEMBL Displacement of [3H]-CP55,940 from human CB2 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting B 7.81 pKi 15.4 nM Ki Bioorg. Med. Chem. (2013) 21: 5383-5394 [PMID:23849204]
ChEMBL Displacement of [3H]-CP55,940 from human CB2 receptor transfected in CHO cell membranes after 60 mins by liquid scintillation spectrometry B 8.01 pKi 9.73 nM Ki Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
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 8.44 nM Ki MedChemComm (2017) 8: 1697-1705
ChEMBL Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation counting B 8.74 pKi 1.8 nM Ki J. Med. Chem. (2008) 51: 4932-4947 [PMID:18666769]
ChEMBL Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter B 8.85 pKi 1.42 nM Ki J. Med. Chem. (2012) 55: 7967-7977 [PMID:22916707]
ChEMBL Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting B 8.85 pKi 1.42 nM Ki ACS Med. Chem. Lett. (2013) 4: 41-45 [PMID:24900561]
ChEMBL Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. (2013) 21: 5383-5394 [PMID:23849204]
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting B 9.05 pKi 0.89 nM Ki Eur. J. Med. Chem. (2014) 85: 77-86 [PMID:25072877]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor B 9.15 pKi 0.7 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 138-141 [PMID:16213718]
ChEMBL Displacement of [3H]CP-55940 from human cloned CB2 receptor B 9.16 pKi 0.69 nM Ki Bioorg. Med. Chem. (2008) 16: 322-335 [PMID:17919913]
ChEMBL Displacement of [3H]CP-55,940 from recombinant human full length CB2 receptor expressed in HEK293 cell membranes after 90 mins by topcount method B 9.16 pKi 0.69 nM Ki Eur J Med Chem (2018) 143: 983-996 [PMID:29232588]
ChEMBL Binding affinity to human CB2 receptor B 9.16 pKi 0.69 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Binding affinity to cannabinoid CB2 receptor B 9.17 pKi 0.68 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells B 9.21 pKi 0.62 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL Displacement of [3H]CP 55940 from human CB2 receptor in cell free system B 9.22 pKi 0.6 nM Ki Eur. J. Med. Chem. (2011) 46: 547-555 [PMID:21183257]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells by liquid scintillation counting B 9.3 pKi 0.5 nM Ki Eur. J. Med. Chem. (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in HEK293 cells B 9.36 pKi 0.44 nM Ki Bioorg. Med. Chem. (2009) 17: 2842-2851 [PMID:19278853]
ChEMBL Displacement of [3H]-CP55940 from human cannabinoid CB2 receptor expressed in Sf9 insect cells after 70 mins by scintillation counting B 9.5 pKi 0.32 nM Ki MedChemComm (2010) 1: 54-60
ChEMBL Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in insect Sf9 cells B 9.5 pKi 0.32 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1748-1753 [PMID:21316962]
ChEMBL Displacement of [3H]-CP55940 from human CB2 expressed in insect Sf9 membranes B 9.5 pKi 0.32 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7327-7330 [PMID:21074434]
ChEMBL Agonist activity at recombinant human full length CB2 receptor expressed in HEK293 cell membranes after 2 hrs by [35S]GTP-gammaS binding assay F 9.7 pKi 0.2 nM Ki Eur J Med Chem (2018) 143: 983-996 [PMID:29232588]
ChEMBL Binding affinity to human CB2 cannabinoid receptor using [3H]CP-55940 in HEK293 EBNA transfected cells B 9.82 pKi 0.15 nM Ki J. Med. Chem. (2001) 44: 4505-4508 [PMID:11741470]
ChEMBL Displacement of [3H]CP-55940 human CB2 receptor expressed in CHOK1 cells B 8.89 pIC50 1.3 nM IC50 J. Med. Chem. (2007) 50: 3851-3856 [PMID:17630726]
ChEMBL Displacement of [3H]CP-55940 form human CB2 receptor expressed in CHO cells B 9.09 pIC50 0.82 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6299-6304 [PMID:17884496]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells B 9.09 pIC50 0.82 nM IC50 Bioorg. Med. Chem. (2008) 16: 1111-1124 [PMID:18006322]
ChEMBL Inverse agonist activity at human CB2 receptor expressed in CHO cells assessed as increase in forskolin-induced cAMP production after 45 mins in presence of phosphodiesterase inhibitor RO20-1724 F 7.33 pEC50 47.1 nM EC50 J. Med. Chem. (2013) 56: 2045-2058 [PMID:23406429]
ChEMBL Agonist activity at human CB2 receptor expressed in Sf9 cells coexpressing Galpha i2 assessed as Galpha GTPase activity using [gamma-33P]GTP by scintillation counting B 7.39 pEC50 40.74 nM EC50 Bioorg. Med. Chem. (2014) 22: 3938-3946 [PMID:24984935]
ChEMBL Agonist activity at CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as increase in intracellular calcium level by microplate reader based assay B 7.51 pEC50 30.7 nM EC50 J. Med. Chem. (2015) 58: 5751-5769 [PMID:26151231]
ChEMBL Agonist activity at CB2 receptor (unknown origin) expressed in CHO cells co-expressing G-alpha16 incubated for 24 hrs by fluo-4 AM dye based whole-cell calcium mobilization assay B 7.54 pEC50 28.62 nM EC50 ACS Med Chem Lett (2017) 8: 678-681 [PMID:28626532]
ChEMBL Agonist activity at CB2 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay F 7.54 pEC50 28.62 nM EC50 Eur J Med Chem (2017) 137: 598-611 [PMID:28651225]
ChEMBL Agonist activity at CB2 receptor (unknown origin) expressed in CHO cells by calcium mobilization assay F 7.59 pEC50 26 nM EC50 Eur. J. Med. Chem. (2015) 93: 16-32 [PMID:25644673]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cell membranes assessed as increase in forskolin-stimulated cAMP production after 45 mins by TR-FRET assay F 7.96 pEC50 11 nM EC50 ACS Med. Chem. Lett. (2013) 4: 387-392 [PMID:24729834]
ChEMBL Partial agonist activity at human cannabinoid CB2 receptor expressed in CHO-K1 cells assessed as [S35]GTPgammaS binding by scintillation counting B 8.03 pEC50 9.3 nM EC50 Eur. J. Med. Chem. (2014) 85: 77-86 [PMID:25072877]
ChEMBL Inverse agonist activity at human recombinant CB2 receptor expressed CHO cells membrane by [35S]GTPgamma binding assay F 8.06 pEC50 8.66 nM EC50 J. Med. Chem. (2009) 52: 433-444 [PMID:19115816]
ChEMBL Agonist activity at human CB2 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assay F 8.13 pEC50 7.4 nM EC50 Eur. J. Med. Chem. (2012) 58: 30-43 [PMID:23085772]
ChEMBL Effect on [35S]GTP-gamma-S binding to human CB2 receptor F 8.21 pEC50 6.1 nM EC50 J. Med. Chem. (2006) 49: 70-79 [PMID:16392793]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding F 8.21 pEC50 6.1 nM EC50 J. Med. Chem. (2010) 53: 7918-7931 [PMID:20979417]
ChEMBL Agonist activity at N-terminal HA-tagged human CB2 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as decrease in forskolin-stimulated cAMP level by BRET assay F 8.25 pEC50 5.6 nM EC50 Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay F 8.26 pEC50 5.5 nM EC50 Eur J Med Chem (2018) 154: 155-171 [PMID:29793210]
ChEMBL Agonist activity at CB2 receptor in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation F 8.38 pEC50 4.21 nM EC50 J. Med. Chem. (2013) 56: 6593-6612 [PMID:23855811]
ChEMBL Agonist activity at human recombinant CB2 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay F 8.38 pEC50 4.13 nM EC50 Eur. J. Med. Chem. (2013) 69: 881-907 [PMID:24125850]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cells by [35S]GTPgammaS assay F 8.57 pEC50 2.7 nM EC50 J. Med. Chem. (2008) 51: 4932-4947 [PMID:18666769]
ChEMBL Agonist activity at human recombinant CB2 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay F 8.63 pEC50 2.37 nM EC50 Bioorg. Med. Chem. (2014) 22: 4770-4783 [PMID:25065940]
ChEMBL Agonist activity at recombinant human Cb2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels F 8.7 pEC50 2 nM EC50 Bioorg Med Chem (2018) 26: 4963-4970 [PMID:30122284]
ChEMBL Agonist activity at N-terminal FLAG-tagged human CB2 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay F 8.76 pEC50 1.73 nM EC50 J Med Chem (2018) 61: 5569-5579 [PMID:29856219]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation using [3H]-cAMP after 5 mins by liquid scintillation counter F 9 pEC50 1 nM EC50 J. Med. Chem. (2012) 55: 7967-7977 [PMID:22916707]
ChEMBL Agonist activity at recombinant human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 5 mins by cAMP-competition binding assay F 9 pEC50 1 nM EC50 ACS Med. Chem. Lett. (2013) 4: 41-45 [PMID:24900561]
ChEMBL Agonist activity at human recombinant CB2 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level F 9.06 pEC50 0.88 nM EC50 J. Med. Chem. (2008) 51: 5019-5034 [PMID:18680277]
ChEMBL Agonist activity at human recombinant CB2 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay F 9.07 pEC50 0.86 nM EC50 Bioorg. Med. Chem. (2008) 16: 1111-1124 [PMID:18006322]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay F 9.07 pEC50 0.86 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 6299-6304 [PMID:17884496]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cells assessed as increase of forskolin-stimulated cAMP accumulation after 20 mins F 9.1 pEC50 0.79 nM EC50 Eur. J. Med. Chem. (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay F 9.16 pEC50 0.69 nM EC50 Bioorg. Med. Chem. (2008) 16: 322-335 [PMID:17919913]
ChEMBL Agonist activity at human CB2 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation B 9.24 pEC50 0.58 nM EC50 J. Med. Chem. (2015) 58: 5979-5988 [PMID:26203658]
ChEMBL Agonist activity at human recombinant CB2 receptor expressed in Sf9 cells by GTP-europium binding assay B 9.37 pEC50 0.43 nM EC50 J. Med. Chem. (2008) 51: 5019-5034 [PMID:18680277]
ChEMBL Agonist activity at human CB2 receptor expressed in CHOK1 cells assessed as reversal of forskolin-evoked cAMP accumulation F 9.46 pEC50 0.35 nM EC50 J. Med. Chem. (2007) 50: 3851-3856 [PMID:17630726]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Displacement of [3H]CP-55940 from CD1 mouse spleen CB2 receptor B 8.95 pKi 1.11 nM Ki J. Med. Chem. (2006) 49: 7502-7512 [PMID:17149879]
CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
ChEMBL Agonist activity at rat recombinant CB2 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level F 9.47 pEC50 0.34 nM EC50 J. Med. Chem. (2008) 51: 5019-5034 [PMID:18680277]
GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6]
ChEMBL