[3H]CP55940 [Ligand Id: 734] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL559612 (CP-55940) |
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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]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 | Displacement of [3H]-CP55,940 from human CB1R expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 2 hrs by liquid scintillation spectrometry analysis | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2022) 65: 9918-9938 [PMID:35849804] |
| 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 | Displacement of [3H]-CP55940 from human CB1 receptor expressed in human HEK293-EBNA cells incubated for 60 mins by radioligand competitive binding assay based liquid scintillation counter | B | 8.78 | pKi | 1.66 | nM | Ki | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in human HEK293-EBNA cells incubated for 60 mins by radioligand competitive binding assay based liquid scintillation counter | B | 8.78 | pKi | 1.66 | nM | Ki | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 | 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 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]-CP55940 from recombinant human CB1 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by radioligand binding assay | B | 9.3 | pKi | 0.5 | nM | Ki | Eur J Med Chem (2021) 226: 113878-113878 [PMID:34634742] |
| 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 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 | 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 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 | 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 recombinant human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin stimulation and measured after 15 mins by HTRF assay | F | 7.14 | pEC50 | 71.89 | nM | EC50 | Eur J Med Chem (2021) 226: 113878-113878 [PMID:34634742] |
| 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 expressed in CHO-K1 cells assessed as assessed as induction of beta-arrestin 2 recruitment measured for 90 mins by PathHunter assay | F | 7.6 | pEC50 | 25 | nM | EC50 | Eur J Med Chem (2022) 230: 114027-114027 [PMID:35051750] |
| 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 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 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 human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay | F | 8.2 | pEC50 | 6.31 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay | F | 8.22 | pEC50 | 6 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay | F | 8.63 | pEC50 | 2.36 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay | F | 8.63 | pEC50 | 2.34 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay | F | 8.82 | pEC50 | 1.5 | nM | EC50 | Eur J Med Chem (2022) 230: 114027-114027 [PMID:35051750] |
| 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]-CP55,940 from human CB2R expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 2 hrs by liquid scintillation spectrometry | B | 7.47 | pKi | 34 | nM | Ki | J Med Chem (2022) 65: 9918-9938 [PMID:35849804] |
| 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]-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]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]-CP55940 from human CB2 receptor expressed in CHO cell membranes assessed as inhibition constant incubated for 1 hr by TopCount liquid scintillation counting analysis | B | 7.96 | pKi | 11 | nM | Ki | J Nat Prod (2023) 86: 1786-1792 [PMID:37450763] |
| 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]-CP55940 from N-terminal 3HA-tagged human CB2 receptor expressed in human HEK293-EBNA cells incubated for 60 mins by radioligand competitive binding assay based liquid scintillation counter | B | 8.7 | pKi | 2 | nM | Ki | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Displacement of [3H]-CP55940 from N-terminal 3HA-tagged human CB2 receptor expressed in human HEK293-EBNA cells incubated for 60 mins by radioligand competitive binding assay based liquid scintillation counter | B | 8.7 | pKi | 1.99 | nM | Ki | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 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]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]-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 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 | 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 | 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 CHO-K1 cells assessed as enhancement of beta arrestin-2 recruitment incubated for 90 mins by HitHunter chemiluminescence based assay | F | 6.25 | pEC50 | 560 | nM | EC50 | J Med Chem (2022) 65: 9918-9938 [PMID:35849804] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in PathHunter CHO-K1 CNR2 beta-arrestin cells assessed as beta-arrestin recruitment incubated for 3 hrs by plate reader analysis | F | 6.79 | pEC50 | 163.5 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1837-1838 [PMID:36518701] |
| 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 receptor expressed in CHO cells assessed as inhibition of accumulation of forskolin-stimulated cAMP level incubated for 35 mins by chemiluminescence based assay | F | 7.24 | pEC50 | 57.92 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1837-1838 [PMID:36518701] |
| 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 recombinant human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin stimulation and measured after 15 mins by HTRF assay | F | 7.35 | pEC50 | 44.33 | nM | EC50 | Eur J Med Chem (2021) 226: 113878-113878 [PMID:34634742] |
| 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 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 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 mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay | F | 7.62 | pEC50 | 24 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay | F | 7.62 | pEC50 | 23.99 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 | Agonist activity at human CB2 receptor expressed in CHO-K1 cells assessed as inhibition of froskolin-stimulated cAMP accumulation incubated for 90 mins by HitHunter chemiluminescence based assay | F | 8.03 | pEC50 | 9.4 | nM | EC50 | J Med Chem (2022) 65: 9918-9938 [PMID:35849804] |
| 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 | 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 | 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 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 CB2 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay | F | 8.92 | pEC50 | 1.2 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at CB2 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay | F | 8.92 | pEC50 | 1.19 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 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 | 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
