[3H]CP55940 [Ligand Id: 734] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL559612 (CP-55940) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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]CP55940 from human CB1 receptor expressed in CHO-K1 cell membranes incubated for 60 mins by liquid scintillation spectrometry analysis | B | 7.89 | pKi | 13 | nM | Ki | Bioorg Med Chem (2021) 50: 116421-116421 [PMID:34634617] |
| 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 [PMID:30108881] |
| 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 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]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]-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 | Displacement of [3H]CP55940 from human CB1 receptor incubated for 30 mins by scintillation counting method | B | 9.03 | pKi | 0.93 | nM | Ki | J Nat Prod (2020) 83: 88-98 [PMID:31891265] |
| 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 cannabinoid CB1 receptor | B | 9.24 | pKi | 0.58 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| 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 | 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 [3H]CP55940 from human CB1 receptor incubated for 30 mins by scintillation counting method | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Nat Prod (2020) 83: 88-98 [PMID:31891265] |
| 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 human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay | F | 7.38 | pEC50 | 42 | nM | EC50 | J Med Chem (2021) 64: 385-403 [PMID:33382613] |
| 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 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 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 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 | 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 | 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 | F | 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 cannabinoid CB1 receptor in human U2OS cells assessed as induction of beta-arrestin recruitment using CCF4/AM as substrate preincubated for 5 hrs followed by substrate addition and measured after 2 hrs by Tango assay | B | 8.24 | pEC50 | 5.75 | nM | EC50 | Bioorg Med Chem (2021) 33: 116035-116035 [PMID:33550084] |
| 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 | F | 8.41 | pEC50 | 3.9 | nM | EC50 | Eur J Med Chem (2014) 85: 77-86 [PMID:25072877] |
| ChEMBL | Agonist activity at GFP-fused human CB1 receptor assessed as increase in beta-arrestin-2 recruitment by BRET-based luciferase reporter gene assay | B | 8.49 | pEC50 | 3.2 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at GFP-fused human CB1 receptor assessed as increase in cAMP accumulation after 1 hr by FRET assay | F | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| 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 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 cell membranes assessed as increase in [35S]GTPgammaS binding incubated for 30 mins by liquid scintillation spectrometry analysis | F | 8.68 | pEC50 | 2.1 | nM | EC50 | Bioorg Med Chem (2021) 50: 116421-116421 [PMID:34634617] |
| ChEMBL | Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assay | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem (2021) 33: 116035-116035 [PMID:33550084] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay | F | 8.78 | pEC50 | 1.66 | nM | EC50 | Bioorg Med Chem (2020) 28: 115513-115513 [PMID:32340793] |
| ChEMBL | Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay | F | 8.82 | pEC50 | 1.51 | nM | EC50 | Eur J Med Chem (2021) 220: 113354-113354 [PMID:33915369] |
| 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 CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis | F | 8.85 | pEC50 | 1.4 | nM | EC50 | J Med Chem (2020) 63: 542-568 [PMID:31756109] |
| 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 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay | F | 8.95 | pEC50 | 1.13 | nM | EC50 | J Med Chem (2021) 64: 3870-3884 [PMID:33761251] |
| 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 | F | 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 after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment method | B | 9.52 | pEC50 | 0.3 | nM | EC50 | J Med Chem (2021) 64: 385-403 [PMID:33382613] |
| 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 rat brain CB1 receptor assessed as inhibition of forskolin-stimulated cAMP level at 500 nM stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins relative to control | F | 7.14 | pEC50 | 73 | nM | EC50 | Bioorg Med Chem Lett (2021) 38: 127882-127882 [PMID:33636308] |
| ChEMBL | Allosteric agonist activity at N-terminal GFP-tagged rat CB1R expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 min by TR-FRET assay | F | 7.74 | pEC50 | 18 | nM | EC50 | J Med Chem (2020) 63: 542-568 [PMID:31756109] |
| ChEMBL | Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins | F | 8.14 | pEC50 | 7.3 | nM | EC50 | Bioorg Med Chem Lett (2021) 38: 127882-127882 [PMID:33636308] |
| 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 [PMID:30108881] |
| 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 | Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins by HTRF assay | F | 8.08 | pIC50 | 8.3 | nM | IC50 | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| 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 | Agonist activity at human CB2 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assay | B | 7.2 | pEC50 | 63.1 | nM | EC50 | Eur J Med Chem (2019) 180: 291-309 [PMID:31319265] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assay | B | 7.2 | pEC50 | 63 | nM | EC50 | Eur J Med Chem (2019) 180: 291-309 [PMID:31319265] |
| ChEMBL | Agonist activity at human CB2 expressed in mouse AtT20 cells assessed as activation of G-protein gated inwardly rectifying K+ channels measured every 2 sec for 2 mins by FLIPR membrane potential assay | B | 7.25 | pEC50 | 56.23 | nM | EC50 | Eur J Med Chem (2021) 210: 113087-113087 [PMID:33321261] |
| ChEMBL | Agonist activity at human CB2 expressed in mouse AtT20 cells assessed as activation of G-protein gated inwardly rectifying K+ channels measured every 2 sec for 2 mins by FLIPR membrane potential assay | B | 7.25 | pEC50 | 56 | nM | EC50 | Eur J Med Chem (2021) 210: 113087-113087 [PMID:33321261] |
| ChEMBL | Agonist activity at human CB2-receptor expressed in CHO-K1 cells coexpressing G-alpha16 by Fluo-4-AM dye based calcium mobilization assay | F | 7.26 | pEC50 | 55 | nM | EC50 | Medchemcomm (2019) 10: 2131-2139 [PMID:32904145] |
| 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 cannabinoid CB2 receptor in human U2OS cells assessed as induction of beta-arrestin recruitment using CCF4/AM as substrate preincubated for 5 hrs followed by substrate addition and measured after 2 hrs by Tango assay | B | 7.43 | pEC50 | 37.15 | nM | EC50 | Bioorg Med Chem (2021) 33: 116035-116035 [PMID:33550084] |
| ChEMBL | Agonist activity at human CB2 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay | F | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2021) 64: 385-403 [PMID:33382613] |
| ChEMBL | Agonist activity at CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as increase in intracellular calcium level by microplate reader based assay | F | 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 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 co-expressing G-alpha16 incubated for 24 hrs by fluo-4 AM dye based whole-cell calcium mobilization assay | F | 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 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 HEK293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 15 mins by cAMP HTRF assay | F | 7.79 | pEC50 | 16.3 | nM | EC50 | J Med Chem (2021) 64: 385-403 [PMID:33382613] |
| 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 | Agonist activity at human CB2 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment method | B | 8.01 | pEC50 | 9.8 | nM | EC50 | J Med Chem (2021) 64: 385-403 [PMID:33382613] |
| ChEMBL | Partial agonist activity at human cannabinoid CB2 receptor expressed in CHO-K1 cells assessed as [S35]GTPgammaS binding by scintillation counting | F | 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 | Agonist activity at human recombinant cannabinoid CB2 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assay | F | 8.2 | pEC50 | 6.31 | nM | EC50 | Bioorg Med Chem (2021) 33: 116035-116035 [PMID:33550084] |
| 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 HEK293 cells assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins | F | 8.85 | pEC50 | 1.4 | nM | EC50 | Bioorg Med Chem Lett (2021) 38: 127882-127882 [PMID:33636308] |
| ChEMBL | Agonist activity at 3xHA tagged human CB2 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay | F | 8.99 | pEC50 | 1.03 | nM | EC50 | J Med Chem (2021) 64: 3870-3884 [PMID:33761251] |
| 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 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 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 | F | 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 CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay | F | 9.27 | pEC50 | 0.54 | nM | EC50 | Eur J Med Chem (2021) 220: 113354-113354 [PMID:33915369] |
| 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 | Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | B | 5.79 | pEC50 | 1610 | nM | EC50 | Medchemcomm (2014) 5: 632-649 |
| GPR18/N-arachidonyl glycine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2384898] [GtoPdb: 89] [UniProtKB: Q14330] | ||||||||
| ChEMBL | Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay | B | 5.22 | pIC50 | 5990 | nM | IC50 | J Med Chem (2013) 56: 4798-4810 [PMID:23679955] |
| ChEMBL | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | B | 5.22 | pEC50 | 5990 | nM | EC50 | Medchemcomm (2014) 5: 632-649 |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5.6 | pIC50 | 2511.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.6 | pIC50 | 2511.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.7 | pIC50 | 1995.26 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.7 | pIC50 | 1995.26 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| ChEMBL | Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2009) 52: 3001-3009 [PMID:19361197] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
