WIN55212-2 [Ligand Id: 733] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL188 (WIN-55212-2) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Binding affinity towards cloned human Cannabinoid receptor 1 | B | 0.28 | pKi | 0.28 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells | B | 5.42 | pKi | 3802 | nM | Ki | J Med Chem (2005) 48: 2509-2517 [PMID:15801840] |
| ChEMBL | Displacement of [3H]SR141716A from human CB1 receptor | B | 5.42 | pKi | 3802 | nM | Ki | J Med Chem (2006) 49: 872-882 [PMID:16451053] |
| ChEMBL | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells | B | 5.42 | pKi | 3800 | nM | Ki | J Med Chem (2005) 48: 7486-7490 [PMID:16279809] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W5 43(280)A mutant Cannabinoid receptor 1 at 5 uM | B | 6.7 | pKi | 199 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes | B | 6.82 | pKi | 152.2 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2233-2236 [PMID:10465552] |
| ChEMBL | Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins | B | 6.82 | pKi | 150 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor | B | 6.85 | pKi | 140 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3695-3700 [PMID:18522867] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.36 (201)A mutant Cannabinoid receptor 1 | B | 6.97 | pKi | 107 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 7.02 | pKi | 94.5 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting | B | 7.1 | pKi | 79.43 | nM | Ki | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in CHO cells membrane by scintillation counting | B | 7.28 | pKi | 52.4 | nM | Ki | J Med Chem (2012) 55: 8948-8952 [PMID:23017078] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by scintillation counting | B | 7.28 | pKi | 52.4 | nM | Ki | Eur J Med Chem (2012) 58: 396-404 [PMID:23151320] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor after 1 hr by scintillation counting analysis | B | 7.28 | pKi | 52.4 | nM | Ki | ACS Med Chem Lett (2015) 6: 198-203 [PMID:25699149] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells | B | 7.34 | pKi | 46 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation counting method | B | 7.34 | pKi | 45.6 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting | B | 7.34 | pKi | 45.6 | nM | Ki | Eur J Med Chem (2013) 70: 111-119 [PMID:24141201] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer | B | 7.34 | pKi | 45.6 | nM | Ki | J Med Chem (2016) 59: 1840-1853 [PMID:26789378] |
| ChEMBL | Displacement of [3H]-CP55940 from CB1 receptor after 90 mins by liquid scintillation counting | B | 7.34 | pKi | 45.6 | nM | Ki | ACS Med Chem Lett (2011) 2: 793-797 [PMID:24936232] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor after 90 mins by liquid scintillation spectrophotometer analysis | B | 7.34 | pKi | 45.59 | nM | Ki | Bioorg Med Chem (2013) 21: 1708-1716 [PMID:23434135] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W6 48(357)A mutant Cannabinoid receptor 1 | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Binding affinity to human CB1 receptor | B | 7.39 | pKi | 40.9 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6183-6187 [PMID:17884494] |
| ChEMBL | Binding affinity against human Cannabinoid receptor 1 expressed in CHO cells by using CP-55940 as Radioactive tracer | B | 7.4 | pKi | 40 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2399-2402 [PMID:12161142] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis | B | 7.44 | pKi | 36.2 | nM | Ki | Eur J Med Chem (2014) 73: 56-72 [PMID:24378710] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis | B | 7.44 | pKi | 36.2 | nM | Ki | Eur J Med Chem (2015) 101: 651-667 [PMID:26209834] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1R transfected in HEK293EBNA cell membranes incubated for 90 mins by Microbeta TriLux based luminescence analysis | B | 7.44 | pKi | 36.2 | nM | Ki | Bioorg Med Chem (2020) 28: 115672-115672 [PMID:32912440] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation and luminescence counting method | B | 7.54 | pKi | 28.8 | nM | Ki | Eur J Med Chem (2017) 127: 398-412 [PMID:28088085] |
| ChEMBL | Displacement of [3H]CP,55-940 from recombinant human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method | B | 7.54 | pKi | 28.8 | nM | Ki | Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 7.64 | pKi | 23 | nM | Ki | J Nat Prod (2001) 64: 1322-1325 [PMID:11678659] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS cells | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2005) 48: 7343-7350 [PMID:16279794] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307] |
| ChEMBL | Binding affinity to human recombinant CB1 receptor expressed in african green monkey COS cells by radioligand binding assay | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2009) 52: 2506-2514 [PMID:19331413] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK cell membrane | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2020) 28: 115513-115513 [PMID:32340793] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2014) 22: 4770-4783 [PMID:25065940] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2007) 15: 5406-5416 [PMID:17561406] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 138-141 [PMID:16213718] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in human HEK293 cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2011) 54: 8278-8288 [PMID:22044209] |
| ChEMBL | Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | B | 7.72 | pKi | 19 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Binding affinity to human CB1 receptor | B | 7.79 | pKi | 16.1 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 1322-1326 [PMID:24508127] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.25 (190)A mutant Cannabinoid receptor 1 | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 7.88 | pKi | 13.3 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB1 receptor in cell free system | B | 7.88 | pKi | 13.3 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 7.88 | pKi | 13.3 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 7.88 | pKi | 13.18 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 7.88 | pKi | 13.18 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]-CP55940 from human cannabinoid CB1 receptor expressed in Sf9 insect cells after 70 mins by scintillation counting | B | 7.9 | pKi | 12.59 | nM | Ki | Medchemcomm (2010) 1: 54-60 |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 expressed in insect Sf9 membranes | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7327-7330 [PMID:21074434] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in insect Sf9 cells | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1748-1753 [PMID:21316962] |
| ChEMBL | Displacement of [3H]CP-55,940 from human CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis | B | 7.9 | pKi | 12.5 | nM | Ki | Eur J Med Chem (2016) 113: 11-27 [PMID:26922225] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cell membranes incubated for 90 mins by scintillation counting | B | 7.91 | pKi | 12.4 | nM | Ki | J Med Chem (2012) 55: 6608-6623 [PMID:22738271] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with wild type Cannabinoid receptor 1 | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis | B | 7.95 | pKi | 11.3 | nM | Ki | J Med Chem (2013) 56: 1098-1112 [PMID:23350768] |
| ChEMBL | Displacement of [3H]-CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cells membrane incubated for 90 mins | B | 8.04 | pKi | 9.2 | nM | Ki | J Nat Prod (2011) 74: 2019-2022 [PMID:21902175] |
| ChEMBL | Displacement of [3H]CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins | B | 8.04 | pKi | 9.2 | nM | Ki | J Nat Prod (2011) 74: 2313-2317 [PMID:21999614] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins | B | 8.04 | pKi | 9.2 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1210-1213 [PMID:20022504] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by scintillation counting analysis | B | 8.06 | pKi | 8.8 | nM | Ki | J Nat Prod (2015) 78: 1671-1682 [PMID:26149623] |
| ChEMBL | Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB1 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis | B | 8.06 | pKi | 8.72 | nM | Ki | Medchemcomm (2017) 8: 1697-1705 [PMID:30108881] |
| ChEMBL | Binding affinity to human cannabinoid CB1 receptor | B | 8.22 | pKi | 6.06 | nM | Ki | Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cell membranes after 90 mins | B | 8.6 | pKi | 2.5 | nM | Ki | Eur J Med Chem (2018) 154: 155-171 [PMID:29793210] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in CHO-K1 cells by liquid scintillation counting | B | 8.6 | pKi | 2.5 | nM | Ki | Eur J Med Chem (2014) 85: 77-86 [PMID:25072877] |
| ChEMBL | Displacement of [3H]CP55940 from recombinant human CB1R expressed in CHO cell membranes incubated for 90 mins | B | 8.6 | pKi | 2.5 | nM | Ki | Eur J Med Chem (2020) 208: 112858-112858 [PMID:33002735] |
| ChEMBL | Compound was evaluated for its binding affinity against Cannabinoid receptor 1 in Guinea pig ileum (GPI) using [3H]CP-55940 ligand | B | 8.61 | pKi | 2.48 | nM | Ki | J Med Chem (1998) 41: 5177-5187 [PMID:9857088] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477]; Biochim Biophys Acta (1996) 1307: 132-6 [PMID:8679694] |
| ChEMBL | Binding affinity of compound was determined against to human cannabinoid receptor 1 in chinese hamster ovary cells | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2003) 46: 2110-2116 [PMID:12747783] |
| ChEMBL | Binding affinity to CB1 receptor | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2008) 51: 5019-5034 [PMID:18680277] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
| ChEMBL | Binding affinity to human CB1 receptor by filtration assay | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem (2012) 20: 2067-2081 [PMID:22341572] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2019-2021 [PMID:23466226] |
| ChEMBL | Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| ChEMBL | Binding affinity to human recombinant CB1 receptor | B | 7.2 | pIC50 | 63.1 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 272-277 [PMID:17027269] |
| ChEMBL | Displacement of [3H]-CP55,940 from human CB1 receptor expressed in HEK293S cell membranes by scintillation counting analysis | B | 7.23 | pIC50 | 59 | nM | IC50 | J Med Chem (2013) 56: 220-240 [PMID:23227781] |
| ChEMBL | Agonist activity at human CB1 in CHO cells assessed as inhibition of cAMP production | F | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| ChEMBL | Inhibition of human cannabinoid CB1 receptor | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| ChEMBL | Agonist activity at CB1 receptor | F | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2008) 43: 513-539 [PMID:17582659] |
| ChEMBL | Agonist activity at human CB1 receptor transfected in human U2OS cells assessed as beta-arrestin2-GFP aggregation after 40 mins | B | 5.75 | pEC50 | 1760 | nM | EC50 | J Med Chem (2013) 56: 3904-3921 [PMID:23621789] |
| ChEMBL | Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 6.5 | pEC50 | 316.23 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 272-277 [PMID:17027269] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding | F | 6.95 | pEC50 | 112 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay | B | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2013) 56: 220-240 [PMID:23227781] |
| ChEMBL | Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay | F | 7.3 | pEC50 | 50.12 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7327-7330 [PMID:21074434] |
| ChEMBL | Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay | F | 7.3 | pEC50 | 50.12 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 1748-1753 [PMID:21316962] |
| ChEMBL | Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay | B | 7.3 | pEC50 | 50.12 | nM | EC50 | Medchemcomm (2010) 1: 54-60 |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method | F | 7.36 | pEC50 | 44 | nM | EC50 | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB1 receptor in HEK293 cells | B | 7.42 | pEC50 | 37.6 | nM | EC50 | J Nat Prod (2006) 69: 432-435 [PMID:16562853] |
| ChEMBL | Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release | F | 7.5 | pEC50 | 31.62 | nM | EC50 | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| ChEMBL | Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519] |
| ChEMBL | Agonist activity at CB1 receptor (unknown origin) assessed as increase in cAMP accumulation after 1 hr by FLIPR assay | F | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation | F | 7.91 | pEC50 | 12.3 | nM | EC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| ChEMBL | Agonist activity at CB1 receptor (unknown origin) assessed as increase in beta-arrestin2 recruitment after 20 mins by BRET-based luciferase reporter gene assay | B | 8.14 | pEC50 | 7.2 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] | ||||||||
| ChEMBL | Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [3H]SR-141,716A | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2005) 48: 6386-6392 [PMID:16190764] |
| ChEMBL | Displacement of [3H]CP-55940 from mouse CB1 receptor | B | 8.15 | pKi | 7 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907] |
| ChEMBL | Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [131I]-(R)-8 | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2005) 48: 6386-6392 [PMID:16190764] |
| ChEMBL | Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction | F | 5.84 | pEC50 | 1450 | nM | EC50 | Bioorg Med Chem (2007) 15: 7480-7493 [PMID:17870539] |
| ChEMBL | Activity at CB1 receptor assessed as stimulation of [35S]GTP-gamma-S binding in DBA/J2 mouse brain | F | 6.69 | pEC50 | 204 | nM | EC50 | J Med Chem (2006) 49: 5947-5957 [PMID:17004710] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from CB1 receptor in rat brain homogenate after 1.5 hrs by microbeta liquid scintillation counting analysis | B | 7.44 | pKi | 36 | nM | Ki | Eur J Med Chem (2013) 69: 881-907 [PMID:24125850] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat brain by scintillation counting | B | 7.81 | pKi | 15.6 | nM | Ki | J Med Chem (2012) 55: 6608-6623 [PMID:22738271] |
| ChEMBL | Displacement of [3H]CP-55,940 from Sprague-Dawley rat brain CB1 receptor by scintillation counting analysis | B | 7.84 | pKi | 14.4 | nM | Ki | J Med Chem (2013) 56: 1098-1112 [PMID:23350768] |
| ChEMBL | Displacement of [3H]-WIN55212-2 from CB1R in rat brain membranes incubated for 60 mins by radioligand competitive binding assay | B | 7.96 | pKi | 11 | nM | Ki | ACS Med Chem Lett (2023) 14: 479-486 [PMID:37077391] |
| 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 brain membrane CB1 receptor assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins | B | 6.84 | pEC50 | 143 | nM | EC50 | ACS Med Chem Lett (2023) 14: 479-486 [PMID:37077391] |
| 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]-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 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]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 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 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]-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 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 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 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]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 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 recombinant human CB2 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by radioligand binding assay | B | 8.45 | pKi | 3.55 | nM | Ki | Eur J Med Chem (2021) 226: 113878-113878 [PMID:34634742] |
| 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 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 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 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-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 | 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-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]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 | 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]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-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]-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]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]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]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 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]-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]-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 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 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 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 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: 8224-8256 [PMID:23865723] |
| 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 | 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: 7161-7176 [PMID:23672690] |
| 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 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 | 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] |
| 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] |
| 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 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]
