WIN55212-2 [Ligand Id: 733] 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: CHEMBL188 (WIN-55212-2) |
|---|
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 towards cloned human Cannabinoid receptor 1 | B | 0.28 | pKi | 0.28 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells | B | 5.42 | pKi | 3802 | nM | Ki | J Med Chem (2005) 48: 2509-2517 [PMID:15801840] |
| ChEMBL | Displacement of [3H]SR141716A from human CB1 receptor | B | 5.42 | pKi | 3802 | nM | Ki | J Med Chem (2006) 49: 872-882 [PMID:16451053] |
| ChEMBL | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells | B | 5.42 | pKi | 3800 | nM | Ki | J Med Chem (2005) 48: 7486-7490 [PMID:16279809] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W5 43(280)A mutant Cannabinoid receptor 1 at 5 uM | B | 6.7 | pKi | 199 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes | B | 6.82 | pKi | 152.2 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2233-2236 [PMID:10465552] |
| ChEMBL | Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins | B | 6.82 | pKi | 150 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor | B | 6.85 | pKi | 140 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3695-3700 [PMID:18522867] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.36 (201)A mutant Cannabinoid receptor 1 | B | 6.97 | pKi | 107 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 7.02 | pKi | 94.5 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting | B | 7.1 | pKi | 79.43 | nM | Ki | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in CHO cells membrane by scintillation counting | B | 7.28 | pKi | 52.4 | nM | Ki | J Med Chem (2012) 55: 8948-8952 [PMID:23017078] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by scintillation counting | B | 7.28 | pKi | 52.4 | nM | Ki | Eur J Med Chem (2012) 58: 396-404 [PMID:23151320] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor after 1 hr by scintillation counting analysis | B | 7.28 | pKi | 52.4 | nM | Ki | ACS Med Chem Lett (2015) 6: 198-203 [PMID:25699149] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells | B | 7.34 | pKi | 46 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation counting method | B | 7.34 | pKi | 45.6 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting | B | 7.34 | pKi | 45.6 | nM | Ki | Eur J Med Chem (2013) 70: 111-119 [PMID:24141201] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer | B | 7.34 | pKi | 45.6 | nM | Ki | J Med Chem (2016) 59: 1840-1853 [PMID:26789378] |
| ChEMBL | Displacement of [3H]-CP55940 from CB1 receptor after 90 mins by liquid scintillation counting | B | 7.34 | pKi | 45.6 | nM | Ki | ACS Med Chem Lett (2011) 2: 793-797 [PMID:24936232] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor after 90 mins by liquid scintillation spectrophotometer analysis | B | 7.34 | pKi | 45.59 | nM | Ki | Bioorg Med Chem (2013) 21: 1708-1716 [PMID:23434135] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W6 48(357)A mutant Cannabinoid receptor 1 | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Binding affinity to human CB1 receptor | B | 7.39 | pKi | 40.9 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6183-6187 [PMID:17884494] |
| ChEMBL | Binding affinity against human Cannabinoid receptor 1 expressed in CHO cells by using CP-55940 as Radioactive tracer | B | 7.4 | pKi | 40 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2399-2402 [PMID:12161142] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis | B | 7.44 | pKi | 36.2 | nM | Ki | Eur J Med Chem (2014) 73: 56-72 [PMID:24378710] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis | B | 7.44 | pKi | 36.2 | nM | Ki | Eur J Med Chem (2015) 101: 651-667 [PMID:26209834] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1R transfected in HEK293EBNA cell membranes incubated for 90 mins by Microbeta TriLux based luminescence analysis | B | 7.44 | pKi | 36.2 | nM | Ki | Bioorg Med Chem (2020) 28: 115672-115672 [PMID:32912440] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation and luminescence counting method | B | 7.54 | pKi | 28.8 | nM | Ki | Eur J Med Chem (2017) 127: 398-412 [PMID:28088085] |
| ChEMBL | Displacement of [3H]CP,55-940 from recombinant human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method | B | 7.54 | pKi | 28.8 | nM | Ki | Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 7.64 | pKi | 23 | nM | Ki | J Nat Prod (2001) 64: 1322-1325 [PMID:11678659] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS cells | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2005) 48: 7343-7350 [PMID:16279794] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307] |
| ChEMBL | Binding affinity to human recombinant CB1 receptor expressed in african green monkey COS cells by radioligand binding assay | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2009) 52: 2506-2514 [PMID:19331413] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK cell membrane | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2020) 28: 115513-115513 [PMID:32340793] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2014) 22: 4770-4783 [PMID:25065940] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2007) 15: 5406-5416 [PMID:17561406] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 138-141 [PMID:16213718] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in human HEK293 cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2011) 54: 8278-8288 [PMID:22044209] |
| ChEMBL | Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | B | 7.72 | pKi | 19 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Binding affinity to human CB1 receptor | B | 7.79 | pKi | 16.1 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 1322-1326 [PMID:24508127] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.25 (190)A mutant Cannabinoid receptor 1 | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 7.88 | pKi | 13.3 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB1 receptor in cell free system | B | 7.88 | pKi | 13.3 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 7.88 | pKi | 13.3 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 7.88 | pKi | 13.18 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 7.88 | pKi | 13.18 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]-CP55940 from human cannabinoid CB1 receptor expressed in Sf9 insect cells after 70 mins by scintillation counting | B | 7.9 | pKi | 12.59 | nM | Ki | Medchemcomm (2010) 1: 54-60 |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 expressed in insect Sf9 membranes | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7327-7330 [PMID:21074434] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in insect Sf9 cells | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1748-1753 [PMID:21316962] |
| ChEMBL | Displacement of [3H]CP-55,940 from human CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis | B | 7.9 | pKi | 12.5 | nM | Ki | Eur J Med Chem (2016) 113: 11-27 [PMID:26922225] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cell membranes incubated for 90 mins by scintillation counting | B | 7.91 | pKi | 12.4 | nM | Ki | J Med Chem (2012) 55: 6608-6623 [PMID:22738271] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with wild type Cannabinoid receptor 1 | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis | B | 7.95 | pKi | 11.3 | nM | Ki | J Med Chem (2013) 56: 1098-1112 [PMID:23350768] |
| ChEMBL | Displacement of [3H]-CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cells membrane incubated for 90 mins | B | 8.04 | pKi | 9.2 | nM | Ki | J Nat Prod (2011) 74: 2019-2022 [PMID:21902175] |
| ChEMBL | Displacement of [3H]CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins | B | 8.04 | pKi | 9.2 | nM | Ki | J Nat Prod (2011) 74: 2313-2317 [PMID:21999614] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins | B | 8.04 | pKi | 9.2 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1210-1213 [PMID:20022504] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by scintillation counting analysis | B | 8.06 | pKi | 8.8 | nM | Ki | J Nat Prod (2015) 78: 1671-1682 [PMID:26149623] |
| ChEMBL | Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB1 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis | B | 8.06 | pKi | 8.72 | nM | Ki | Medchemcomm (2017) 8: 1697-1705 [PMID:30108881] |
| ChEMBL | Binding affinity to human cannabinoid CB1 receptor | B | 8.22 | pKi | 6.06 | nM | Ki | Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cell membranes after 90 mins | B | 8.6 | pKi | 2.5 | nM | Ki | Eur J Med Chem (2018) 154: 155-171 [PMID:29793210] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in CHO-K1 cells by liquid scintillation counting | B | 8.6 | pKi | 2.5 | nM | Ki | Eur J Med Chem (2014) 85: 77-86 [PMID:25072877] |
| ChEMBL | Displacement of [3H]CP55940 from recombinant human CB1R expressed in CHO cell membranes incubated for 90 mins | B | 8.6 | pKi | 2.5 | nM | Ki | Eur J Med Chem (2020) 208: 112858-112858 [PMID:33002735] |
| ChEMBL | Compound was evaluated for its binding affinity against Cannabinoid receptor 1 in Guinea pig ileum (GPI) using [3H]CP-55940 ligand | B | 8.61 | pKi | 2.48 | nM | Ki | J Med Chem (1998) 41: 5177-5187 [PMID:9857088] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477]; Biochim Biophys Acta (1996) 1307: 132-6 [PMID:8679694] |
| ChEMBL | Binding affinity of compound was determined against to human cannabinoid receptor 1 in chinese hamster ovary cells | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2003) 46: 2110-2116 [PMID:12747783] |
| ChEMBL | Binding affinity to CB1 receptor | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2008) 51: 5019-5034 [PMID:18680277] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
| ChEMBL | Binding affinity to human CB1 receptor by filtration assay | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem (2012) 20: 2067-2081 [PMID:22341572] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2019-2021 [PMID:23466226] |
| ChEMBL | Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| ChEMBL | Binding affinity to human recombinant CB1 receptor | B | 7.2 | pIC50 | 63.1 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 272-277 [PMID:17027269] |
| ChEMBL | Displacement of [3H]-CP55,940 from human CB1 receptor expressed in HEK293S cell membranes by scintillation counting analysis | B | 7.23 | pIC50 | 59 | nM | IC50 | J Med Chem (2013) 56: 220-240 [PMID:23227781] |
| ChEMBL | Agonist activity at human CB1 in CHO cells assessed as inhibition of cAMP production | F | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| ChEMBL | Inhibition of human cannabinoid CB1 receptor | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| ChEMBL | Agonist activity at CB1 receptor | F | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2008) 43: 513-539 [PMID:17582659] |
| ChEMBL | Agonist activity at human CB1 receptor transfected in human U2OS cells assessed as beta-arrestin2-GFP aggregation after 40 mins | B | 5.75 | pEC50 | 1760 | nM | EC50 | J Med Chem (2013) 56: 3904-3921 [PMID:23621789] |
| ChEMBL | Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 6.5 | pEC50 | 316.23 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 272-277 [PMID:17027269] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding | F | 6.95 | pEC50 | 112 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay | B | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2013) 56: 220-240 [PMID:23227781] |
| ChEMBL | Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay | F | 7.3 | pEC50 | 50.12 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7327-7330 [PMID:21074434] |
| ChEMBL | Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay | F | 7.3 | pEC50 | 50.12 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 1748-1753 [PMID:21316962] |
| ChEMBL | Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay | B | 7.3 | pEC50 | 50.12 | nM | EC50 | Medchemcomm (2010) 1: 54-60 |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method | F | 7.36 | pEC50 | 44 | nM | EC50 | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB1 receptor in HEK293 cells | B | 7.42 | pEC50 | 37.6 | nM | EC50 | J Nat Prod (2006) 69: 432-435 [PMID:16562853] |
| ChEMBL | Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release | F | 7.5 | pEC50 | 31.62 | nM | EC50 | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| ChEMBL | Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519] |
| ChEMBL | Agonist activity at CB1 receptor (unknown origin) assessed as increase in cAMP accumulation after 1 hr by FLIPR assay | F | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation | F | 7.91 | pEC50 | 12.3 | nM | EC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| ChEMBL | Agonist activity at CB1 receptor (unknown origin) assessed as increase in beta-arrestin2 recruitment after 20 mins by BRET-based luciferase reporter gene assay | B | 8.14 | pEC50 | 7.2 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] | ||||||||
| ChEMBL | Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [3H]SR-141,716A | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2005) 48: 6386-6392 [PMID:16190764] |
| ChEMBL | Displacement of [3H]CP-55940 from mouse CB1 receptor | B | 8.15 | pKi | 7 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| ChEMBL | Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [131I]-(R)-8 | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2005) 48: 6386-6392 [PMID:16190764] |
| ChEMBL | Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction | F | 5.84 | pEC50 | 1450 | nM | EC50 | Bioorg Med Chem (2007) 15: 7480-7493 [PMID:17870539] |
| ChEMBL | Activity at CB1 receptor assessed as stimulation of [35S]GTP-gamma-S binding in DBA/J2 mouse brain | F | 6.69 | pEC50 | 204 | nM | EC50 | J Med Chem (2006) 49: 5947-5957 [PMID:17004710] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from CB1 receptor in rat brain homogenate after 1.5 hrs by microbeta liquid scintillation counting analysis | B | 7.44 | pKi | 36 | nM | Ki | Eur J Med Chem (2013) 69: 881-907 [PMID:24125850] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat brain by scintillation counting | B | 7.81 | pKi | 15.6 | nM | Ki | J Med Chem (2012) 55: 6608-6623 [PMID:22738271] |
| ChEMBL | Displacement of [3H]CP-55,940 from Sprague-Dawley rat brain CB1 receptor by scintillation counting analysis | B | 7.84 | pKi | 14.4 | nM | Ki | J Med Chem (2013) 56: 1098-1112 [PMID:23350768] |
| ChEMBL | Binding affinity for cannabinoid receptor 1 | B | 8 | pKi | 9.9 | nM | Ki | J Med Chem (2005) 48: 5059-5087 [PMID:16078824] |
| ChEMBL | Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain cortical membrane | B | 8.22 | pKi | 6.06 | nM | Ki | Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853] |
| ChEMBL | Binding affinity to CB1 cannabinoid receptor using [3H]WIN-55212-2 in rat cerebellum membranes | B | 8.35 | pKi | 4.5 | nM | Ki | J Med Chem (2001) 44: 4505-4508 [PMID:11741470] |
| ChEMBL | Binding affinity to displace [3H]CP-55940 from CB1 receptor of rat brain | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4110-4113 [PMID:16005223] |
| ChEMBL | Displacement of [3H]SR141716A from CB1 receptor in Sprague-Dawley rat cerebellum membrane | B | 6.37 | pIC50 | 430 | nM | IC50 | Eur J Med Chem (2008) 43: 513-539 [PMID:17582659] |
| ChEMBL | Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Binding affinity towards cloned human cannabinoid receptor 2 | B | 0.55 | pKi | 0.55 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells | B | 7.15 | pKi | 70 | nM | Ki | Bioorg Med Chem (2013) 21: 7481-7498 [PMID:24139843] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3695-3700 [PMID:18522867] |
| ChEMBL | Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting | B | 7.79 | pKi | 16.1 | nM | Ki | Bioorg Med Chem (2013) 21: 5383-5394 [PMID:23849204] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cells after 1.5 hrs by microbeta liquid scintillation counting analysis | B | 7.89 | pKi | 13 | nM | Ki | Eur J Med Chem (2013) 69: 881-907 [PMID:24125850] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor | B | 8.04 | pKi | 9.1 | nM | Ki | J Med Chem (2006) 49: 70-79 [PMID:16392793] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 8.04 | pKi | 9.1 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 1322-1326 [PMID:24508127] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells after 1 hr | B | 8.04 | pKi | 9.1 | nM | Ki | J Med Chem (2010) 53: 7918-7931 [PMID:20979417] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells | B | 8.04 | pKi | 9.1 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519] |
| ChEMBL | Displacement of [3H]-CP55,940 from human CB2 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting | B | 8.04 | pKi | 9.1 | nM | Ki | Bioorg Med Chem (2013) 21: 5383-5394 [PMID:23849204] |
| ChEMBL | Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB2 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis | B | 8.07 | pKi | 8.57 | nM | Ki | Medchemcomm (2017) 8: 1697-1705 [PMID:30108881] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells by liquid scintillation counting | B | 8.2 | pKi | 6.31 | nM | Ki | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting analysis | B | 8.31 | pKi | 4.95 | nM | Ki | J Med Chem (2013) 56: 1098-1112 [PMID:23350768] |
| ChEMBL | Displacement of [3H]CP-55,940 from human CB2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting analysis | B | 8.34 | pKi | 4.6 | nM | Ki | Eur J Med Chem (2016) 113: 11-27 [PMID:26922225] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cell membranes incubated for 60 mins by scintillation counting | B | 8.34 | pKi | 4.53 | nM | Ki | J Med Chem (2012) 55: 6608-6623 [PMID:22738271] |
| ChEMBL | Binding affinity against human Cannabinoid receptor 2 expressed in CHO cells by using WIN-55212-2 Mesylate [573H] as Radioactive tracer | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2399-2402 [PMID:12161142] |
| ChEMBL | Binding affinity to human CB2 cannabinoid receptor using [3H]CP-55940 in HEK293 EBNA transfected cells | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2001) 44: 4505-4508 [PMID:11741470] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor after 90 mins by liquid scintillation spectrophotometer analysis | B | 8.43 | pKi | 3.73 | nM | Ki | Bioorg Med Chem (2013) 21: 1708-1716 [PMID:23434135] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis | B | 8.43 | pKi | 3.7 | nM | Ki | Eur J Med Chem (2015) 101: 651-667 [PMID:26209834] |
| ChEMBL | Displacement of [3H]CP55940 from human CB2R transfected in HEK293EBNA cell membrane incubated for 90 mins by Microbeta TriLux based luminescence analysis | B | 8.43 | pKi | 3.7 | nM | Ki | Bioorg Med Chem (2020) 28: 115672-115672 [PMID:32912440] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis | B | 8.43 | pKi | 3.7 | nM | Ki | Eur J Med Chem (2014) 73: 56-72 [PMID:24378710] |
| ChEMBL | Displacement of [3H]CP55940 from human CB2 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2016) 59: 1840-1853 [PMID:26789378] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting | B | 8.43 | pKi | 3.7 | nM | Ki | Eur J Med Chem (2013) 70: 111-119 [PMID:24141201] |
| ChEMBL | Displacement of [3H]CP55940 from human CB2 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation and luminescence counting method | B | 8.43 | pKi | 3.7 | nM | Ki | Eur J Med Chem (2017) 127: 398-412 [PMID:28088085] |
| ChEMBL | Displacement of [3H]CP,55-940 from recombinant human CB2 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method | B | 8.43 | pKi | 3.7 | nM | Ki | Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor after 1 hr by scintillation counting analysis | B | 8.51 | pKi | 3.1 | nM | Ki | ACS Med Chem Lett (2015) 6: 198-203 [PMID:25699149] |
| ChEMBL | Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by scintillation counting | B | 8.51 | pKi | 3.1 | nM | Ki | Eur J Med Chem (2012) 58: 396-404 [PMID:23151320] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in CHO cells membrane by scintillation counting | B | 8.51 | pKi | 3.1 | nM | Ki | J Med Chem (2012) 55: 8948-8952 [PMID:23017078] |
| ChEMBL | Displacement of [3H]-CP-55940 from human CB2 expressed in CHO cells after 90 mins by TopCount scintillation counting method | B | 8.52 | pKi | 3.01 | nM | Ki | Eur J Med Chem (2018) 146: 68-78 [PMID:29360044] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 8.54 | pKi | 2.9 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6183-6187 [PMID:17884494] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in insect Sf9 cells | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1748-1753 [PMID:21316962] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 expressed in insect Sf9 membranes | B | 8.6 | pKi | 2.51 | 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 | 8.6 | pKi | 2.51 | nM | Ki | Medchemcomm (2010) 1: 54-60 |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in COS cells | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2005) 48: 7343-7350 [PMID:16279794] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem (2014) 22: 4770-4783 [PMID:25065940] |
| ChEMBL | Displacement of [3H]-CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cells membrane incubated for 90 mins | B | 8.68 | pKi | 2.1 | nM | Ki | J Nat Prod (2011) 74: 2019-2022 [PMID:21902175] |
| ChEMBL | Binding affinity to human recombinant CB2 receptor expressed in african green monkey COS cells by radioligand binding assay | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2009) 52: 2506-2514 [PMID:19331413] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1210-1213 [PMID:20022504] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307] |
| ChEMBL | Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins | B | 8.68 | pKi | 2.1 | nM | Ki | J Nat Prod (2011) 74: 2313-2317 [PMID:21999614] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem (2007) 15: 5406-5416 [PMID:17561406] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in HEK cell membrane | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem (2020) 28: 115513-115513 [PMID:32340793] |
| ChEMBL | Displacement of [3H]CP55940 from human CB2 receptor expressed in human HEK293 cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2011) 54: 8278-8288 [PMID:22044209] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 138-141 [PMID:16213718] |
| ChEMBL | Displacement of [3H]WIN 55212-2 from human CB2 receptor incubated for 120 mins by scintillation counting method | B | 8.77 | pKi | 1.7 | nM | Ki | J Nat Prod (2020) 83: 88-98 [PMID:31891265] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cell membranes after 90 mins | B | 8.8 | pKi | 1.6 | nM | Ki | Eur J Med Chem (2018) 154: 155-171 [PMID:29793210] |
| ChEMBL | Displacement of [3H]CP55940 from recombinant human CB2R expressed in CHO cell membranes incubated for 90 mins | B | 8.8 | pKi | 1.6 | nM | Ki | Eur J Med Chem (2020) 208: 112858-112858 [PMID:33002735] |
| ChEMBL | Displacement of [3H]-CP-55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | B | 8.8 | pKi | 1.57 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | B | 8.89 | pKi | 1.3 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 8.89 | pKi | 1.29 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 8.89 | pKi | 1.29 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in HEK293 cells | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by scintillation counting analysis | B | 9.05 | pKi | 0.9 | nM | Ki | J Nat Prod (2015) 78: 1671-1682 [PMID:26149623] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting | B | 9.35 | pKi | 0.45 | nM | Ki | Eur J Med Chem (2014) 85: 77-86 [PMID:25072877] |
| ChEMBL | Binding affinity of compound was determined against to human cannabinoid receptor 2 in chinese hamster ovary cells | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2003) 46: 2110-2116 [PMID:12747783] |
| ChEMBL | Binding affinity to CB2 receptor (unknown origin) | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2019-2021 [PMID:23466226] |
| ChEMBL | Binding affinity to CB2 receptor (unknown origin) | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
| ChEMBL | Binding affinity to CB2 receptor | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2008) 51: 5019-5034 [PMID:18680277] |
| ChEMBL | Binding affinity to CB2 receptor (unknown origin) | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Binding affinity to displace [3H]CP-55940 from cloned human CB2 receptor | B | 9.55 | pKi | 0.28 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4110-4113 [PMID:16005223] |
| ChEMBL | Agonist activity at CB2 receptor (unknown origin) | B | 9.55 | pKi | 0.28 | nM | Ki | Eur J Med Chem (2016) 124: 17-35 [PMID:27560280] |
| ChEMBL | Compound was evaluated for its binding affinity against Cannabinoid receptor 2 in Guinea pig ileum (GPI) using [3H]CP-55940 ligand | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (1998) 41: 5177-5187 [PMID:9857088] |
| ChEMBL | Binding affinity to human CB2 receptor by filtration assay | B | 9.55 | pKi | 0.28 | nM | Ki | Bioorg Med Chem (2012) 20: 2067-2081 [PMID:22341572] |
| GtoPdb | - | - | 9.6 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477]; Biochim Biophys Acta (1996) 1307: 132-6 [PMID:8679694] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation | F | 7.8 | pIC50 | 15.7 | nM | IC50 | J Med Chem (2012) 55: 6608-6623 [PMID:22738271] |
| ChEMBL | Displacement of [3H]CP-55940 human CB2 receptor expressed in CHOK1 cells | B | 8.05 | pIC50 | 8.9 | nM | IC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| ChEMBL | Displacement of [3H]-CP55,940 from human CB2 receptor expressed in Sf9 cell membranes by scintillation counting analysis | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2013) 56: 220-240 [PMID:23227781] |
| ChEMBL | Displacement of [3H]WIN 55212-2 from human CB2 receptor incubated for 120 mins by scintillation counting method | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Nat Prod (2020) 83: 88-98 [PMID:31891265] |
| ChEMBL | Agonist activity at human CB2 in CHO cells assessed as inhibition of cAMP production | F | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in CHO cells membrane by [35S]-GTPgammaS assay | F | 7.05 | pEC50 | 89.6 | nM | EC50 | J Med Chem (2012) 55: 8948-8952 [PMID:23017078] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay | F | 7.05 | pEC50 | 89.6 | nM | EC50 | Eur J Med Chem (2012) 58: 396-404 [PMID:23151320] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR | F | 7.07 | pEC50 | 86 | nM | EC50 | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells coexpressing Galphaq/o5 assessed as calcium mobilization by FLIPR assay | F | 7.07 | pEC50 | 86 | nM | EC50 | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding | F | 7.61 | pEC50 | 24.6 | nM | EC50 | J Med Chem (2010) 53: 7918-7931 [PMID:20979417] |
| ChEMBL | Effect on [35S]GTP-gamma-S binding to human CB2 receptor | F | 7.61 | pEC50 | 24.6 | nM | EC50 | J Med Chem (2006) 49: 70-79 [PMID:16392793] |
| ChEMBL | Agonist activity at human CB2 receptor after 1 hr by [35S]-GTPgammaS binding assay | F | 7.61 | pEC50 | 24.5 | nM | EC50 | ACS Med Chem Lett (2015) 6: 198-203 [PMID:25699149] |
| ChEMBL | Inverse agonist activity at human CB2 receptor transfected in CHO cells assessed as increase in forksolin stimulated cAMP production by scintillation counting analysis | F | 7.81 | pEC50 | 15.6 | nM | EC50 | Eur J Med Chem (2016) 113: 11-27 [PMID:26922225] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as forskolin-stimulated [3H]cyclic-AMP accumulation by scintillation counting analysis | F | 7.83 | pEC50 | 14.8 | nM | EC50 | J Med Chem (2013) 56: 1098-1112 [PMID:23350768] |
| ChEMBL | Agonist activity at cloned human CB2 receptor in Sf9 cells assessed as stimulation of [35S]GTPgammaS binding assay | F | 7.85 | pEC50 | 14 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3695-3700 [PMID:18522867] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cell membranes assessed as [35S]GTPgammaS binding after 1 hr by beta-counting analysis | F | 7.94 | pEC50 | 11.5 | nM | EC50 | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO membranes assessed as [35S]-GTPgammaS binding after 1 hr | F | 8.69 | pEC50 | 2.04 | nM | EC50 | Bioorg Med Chem (2013) 21: 5383-5394 [PMID:23849204] |
| ChEMBL | Agonist activity at human CB2 receptor by [35S]-GTPgammaS binding assay | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 1322-1326 [PMID:24508127] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as increase of forskolin-stimulated cAMP accumulation after 20 mins | F | 8.8 | pEC50 | 1.58 | nM | EC50 | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| ChEMBL | Agonist activity at human CB2 receptor by GTPgamma[35S] assay | F | 8.82 | pEC50 | 1.5 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6183-6187 [PMID:17884494] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHOK1 cells assessed as reversal of forskolin-evoked cAMP accumulation | F | 9.33 | pEC50 | 0.47 | nM | EC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production | F | 9.41 | pEC50 | 0.39 | nM | EC50 | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] | ||||||||
| ChEMBL | Displacement of [3H]CP-55940 from mouse CB2 receptor | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] | ||||||||
| ChEMBL | Displacement of [3H]CP-55,940 from Sprague-Dawley rat spleen CB2 receptor by scintillation counting analysis | B | 8.11 | pKi | 7.73 | nM | Ki | J Med Chem (2013) 56: 1098-1112 [PMID:23350768] |
| ChEMBL | Displacement of [3H]CP-55940 from CB2 receptor in Sprague-Dawley rat spleen by scintillation counting | B | 8.12 | pKi | 7.58 | nM | Ki | J Med Chem (2012) 55: 6608-6623 [PMID:22738271] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from CB2 receptor in Sprague-Dawley rat spleen membrane | B | 5.66 | pIC50 | 2200 | nM | IC50 | Eur J Med Chem (2008) 43: 513-539 [PMID:17582659] |
| ChEMBL | Agonist activity at rat CB2 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay | F | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416] | ||||||||
| GtoPdb | - | - | 6.7 | pIC50 | 220 | nM | IC50 | |
| glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311] | ||||||||
| GtoPdb | - | - | 7 | pIC50 | 97 | nM | IC50 | |
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]
