rimonabant [Ligand Id: 743] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL111 (Acomplia, Rimonabant, SR-14171, SR-141716, SR141716, SR-141716A, Zimulti) |
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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 | Antagonist activity at human brain CB1 receptor by calcium mobilization assay | F | 8.59 | pKd | 2.57 | nM | Kd | J Med Chem (2010) 53: 7048-7060 [PMID:20845959] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated [35S]GTPgammaS binding | F | 8.59 | pKd | 2.57 | nM | Kd | J Med Chem (2008) 51: 3526-3539 [PMID:18512901] |
| ChEMBL | In vitro cannabinoid receptor 1 antagonism of [3H]arachidonic acid release by CHO cells | F | 8.6 | pKd | 2.51 | nM | Kd | J Med Chem (2005) 48: 1823-1838 [PMID:15771428] |
| ChEMBL | Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells | F | 8.6 | pKd | 2.51 | nM | Kd | Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010] |
| ChEMBL | Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells | F | 8.6 | pKd | 2.51 | nM | Kd | J Med Chem (2004) 47: 627-643 [PMID:14736243] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release | F | 8.6 | pKd | 2.51 | nM | Kd | Bioorg Med Chem Lett (2010) 20: 2770-2775 [PMID:20363132] |
| ChEMBL | Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cells | B | 8.74 | pKd | 1.8 | nM | Kd | J Med Chem (2006) 49: 5969-5987 [PMID:17004712] |
| ChEMBL | Binding affinity towards cloned human Cannabinoid receptor 1 | B | 1.09 | pKi | 1.09 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay | B | 6.84 | pKi | 143 | nM | Ki | J Med Chem (2019) 62: 9078-9102 [PMID:31609608] |
| ChEMBL | Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method | B | 6.84 | pKi | 143 | nM | Ki | J Med Chem (2018) 61: 1646-1663 [PMID:29400965] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 7.33 | pKi | 47 | nM | Ki | J Med Chem (2007) 50: 5951-5966 [PMID:17979261] |
| ChEMBL | Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting | B | 7.4 | pKi | 40 | nM | Ki | Eur J Med Chem (2009) 44: 593-608 [PMID:18511157] |
| 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 | 7.48 | pKi | 33 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1 | B | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells | B | 7.6 | pKi | 25 | nM | Ki | Eur J Med Chem (2008) 43: 2627-2638 [PMID:18342403] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells | B | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2770-2775 [PMID:20363132] |
| ChEMBL | Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (2004) 47: 627-643 [PMID:14736243] |
| ChEMBL | In vitro displacement of CP-55940 binding to human CB1 receptor expressed in CHO cells | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (2005) 48: 1823-1838 [PMID:15771428] |
| ChEMBL | Antagonist activity at human CB1R expressed in CHO-K1 cell membranes assessed as stimulation of [35S]-GTPgammaS binding by liquid scintillation counting method | F | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2022) 65: 2374-2387 [PMID:35084860] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB1 receptor expressed in HEK293 cells | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2006) 49: 5969-5987 [PMID:17004712] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307] |
| 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 | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 7.9 | pKi | 12.6 | 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 | 7.9 | pKi | 12.6 | nM | Ki | J Med Chem (2012) 55: 7967-7977 [PMID:22916707] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2008) 51: 5075-5084 [PMID:18680276] |
| ChEMBL | Displacement of [3H]CP55940 from human recombinant CB1 receptor transfected in HEK cell membrane | B | 7.92 | pKi | 12 | nM | Ki | Eur J Med Chem (2012) 58: 30-43 [PMID:23085772] |
| ChEMBL | Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells | B | 7.92 | pKi | 12 | nM | Ki | Eur J Med Chem (2010) 45: 5878-5886 [PMID:20943290] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2010) 53: 5915-5928 [PMID:20718492] |
| ChEMBL | Evaluated for binding affinity towards human Cannabinoid receptor 1 | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1151-1154 [PMID:14980654] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2008) 51: 1560-1576 [PMID:18293908] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2011) 54: 5444-5453 [PMID:21702498] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem (2009) 17: 5549-5564 [PMID:19595596] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor transfected in HEK cells | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2012) 55: 5391-5402 [PMID:22548457] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis | B | 7.96 | pKi | 11 | nM | Ki | ACS Med Chem Lett (2013) 4: 387-392 [PMID:24729834] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cells incubated for 1 hr | B | 7.97 | pKi | 10.6 | nM | Ki | J Med Chem (2012) 55: 9973-9987 [PMID:23072339] |
| ChEMBL | Displacement of [3H]CP-55,940 from CB1 receptor (unknown origin) after 1 hr by scintillation counting analysis | B | 7.97 | pKi | 10.6 | nM | Ki | J Med Chem (2013) 56: 2045-2058 [PMID:23406429] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 cell membrane assessed as inhibition constant incubated for 60 mins by radioligand competition binding assay | B | 8.01 | pKi | 9.8 | nM | Ki | Eur J Med Chem (2023) 248: 115109-115109 [PMID:36657299] |
| 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 | 8.02 | pKi | 9.6 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Compound was evaluated for affinity towards human Cannabinoid receptor 1 using [3H]- SR-141716A as radioligand | B | 8.05 | pKi | 8.9 | 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 | 8.05 | pKi | 8.9 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2233-2236 [PMID:10465552] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem (2008) 16: 7510-7515 [PMID:18579386] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation counting method | B | 8.14 | pKi | 7.3 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor after 90 mins by liquid scintillation spectrophotometer analysis | B | 8.14 | pKi | 7.3 | nM | Ki | Bioorg Med Chem (2013) 21: 1708-1716 [PMID:23434135] |
| ChEMBL | Displacement of [3H]-CP55940 from CB1 receptor after 90 mins by liquid scintillation counting | B | 8.14 | pKi | 7.3 | nM | Ki | ACS Med Chem Lett (2011) 2: 793-797 [PMID:24936232] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 8.15 | pKi | 7.1 | nM | Ki | J Med Chem (2006) 49: 5969-5987 [PMID:17004712] |
| ChEMBL | Displacement of [3H]- CP55940 from human CB1R expressed in CHO-K1 cells membrane by Cheng-Prusoff equation analysis | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (2022) 65: 2374-2387 [PMID:35084860] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cell membranes | B | 8.21 | pKi | 6.2 | nM | Ki | Bioorg Med Chem (2016) 24: 1063-1070 [PMID:26827137] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cells | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (2012) 55: 2820-2834 [PMID:22372835] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 8.21 | pKi | 6.18 | nM | Ki | J Med Chem (2008) 51: 3526-3539 [PMID:18512901] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells | B | 8.21 | pKi | 6.18 | nM | Ki | J Med Chem (2010) 53: 7048-7060 [PMID:20845959] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2008) 51: 2115-2127 [PMID:18335976] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHOK1 cells after 1 hr by liquid scintillation counting analysis | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2013) 56: 9874-9896 [PMID:24175572] |
| ChEMBL | Binding affinity to human CB1 receptor | B | 8.25 | pKi | 5.6 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1022-1025 [PMID:19095444] |
| ChEMBL | Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells | B | 8.27 | pKi | 5.4 | nM | Ki | J Med Chem (2005) 48: 2509-2517 [PMID:15801840] |
| ChEMBL | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells | B | 8.27 | pKi | 5.4 | nM | Ki | J Med Chem (2005) 48: 7486-7490 [PMID:16279809] |
| ChEMBL | Displacement of [3H]SR-141716A from human CB1 receptor | B | 8.27 | pKi | 5.37 | nM | Ki | J Med Chem (2006) 49: 70-79 [PMID:16392793] |
| ChEMBL | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with wild type Cannabinoid receptor 1 | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (2003) 46: 5139-5152 [PMID:14613317] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2008) 51: 2439-2446 [PMID:18363352] |
| ChEMBL | Binding affinity to human CB1 receptor | B | 8.62 | pKi | 2.4 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1278-1283 [PMID:20018510] |
| ChEMBL | Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 731-736 [PMID:16263283] |
| GtoPdb | - | - | 8.7 | pKi | 1.99 | nM | Ki |
Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477]; J Pharmacol Exp Ther (1998) 284: 291-7 [PMID:9435190]; FEBS Lett (1994) 350: 240-4 [PMID:8070571]; J Pharmacol Exp Ther (2003) 306: 363-70 [PMID:12663689] |
| ChEMBL | Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2009) 52: 1975-1982 [PMID:19338356] |
| ChEMBL | Antagonist activity at CB1 receptor (unknown origin) | B | 8.7 | pKi | 1.98 | nM | Ki | Eur J Med Chem (2014) 74: 73-84 [PMID:24445310] |
| ChEMBL | Binding affinity to CB1 receptor | B | 8.7 | pKi | 1.98 | nM | Ki | J Med Chem (2008) 51: 2439-2446 [PMID:18363352] |
| ChEMBL | Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572] |
| ChEMBL | Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting | B | 8.74 | pKi | 1.8 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
| ChEMBL | Binding affinity to CB1 receptor | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Displacement of radioligand from human CB1 receptor expressed in HEK293 cells | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1199-1206 [PMID:18083560] |
| ChEMBL | Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assay | F | 8.8 | pKi | 1.6 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 5351-5354 [PMID:19683918] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting | F | 8.8 | pKi | 1.6 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay | F | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Displacement of [3H]CP55940 from CB1 receptor | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2011) 54: 2961-2970 [PMID:21428406] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor by scintillation counting | B | 8.86 | pKi | 1.38 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6209-6212 [PMID:19767206] |
| ChEMBL | Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells | B | 8.93 | pKi | 1.18 | nM | Ki | J Med Chem (2008) 51: 3526-3539 [PMID:18512901] |
| ChEMBL | Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cells | B | 8.93 | pKi | 1.18 | nM | Ki | J Med Chem (2010) 53: 7048-7060 [PMID:20845959] |
| ChEMBL | Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2706-2711 [PMID:17383180] |
| ChEMBL | Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay | F | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 731-736 [PMID:16263283] |
| ChEMBL | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells | B | 9.03 | pKi | 0.93 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 2034-2039 [PMID:21334892] |
| ChEMBL | Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2009) 52: 234-237 [PMID:19102698] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting | B | 9.13 | pKi | 0.74 | nM | Ki | Eur J Med Chem (2010) 45: 1133-1139 [PMID:20047779] |
| ChEMBL | Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting | B | 9.14 | pKi | 0.73 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6856-6860 [PMID:21962575] |
| ChEMBL | Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation spectrometry | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem (2018) 26: 4518-4531 [PMID:30077609] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding | F | 9.37 | pKi | 0.43 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3376-3381 [PMID:18448340] |
| ChEMBL | Binding affinity to human CB1 receptor by [35S]GTPgammaS binding assay | F | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2008) 51: 5608-5616 [PMID:18754613] |
| ChEMBL | Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay | F | 9.72 | pKi | 0.19 | nM | Ki | J Med Chem (2009) 52: 234-237 [PMID:19102698] |
| ChEMBL | Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method | B | 6.8 | pIC50 | 158.49 | nM | IC50 | J Med Chem (2018) 61: 1646-1663 [PMID:29400965] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay | F | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2008) 16: 4035-4051 [PMID:18243711] |
| ChEMBL | Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay | F | 6.97 | pIC50 | 108 | nM | IC50 | Bioorg Med Chem (2010) 18: 1149-1162 [PMID:20045337] |
| ChEMBL | Inverse agonist activity at CB1 receptor assessed as repression of basal receptor activity by mammalian cell-based receptor selection and amplification technology method | F | 7.2 | pIC50 | 63.1 | nM | IC50 | J Med Chem (2009) 52: 1975-1982 [PMID:19338356] |
| ChEMBL | Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level | F | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6173-6180 [PMID:22959249] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2008) 51: 5397-5412 [PMID:18712856] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1022-1025 [PMID:19095444] |
| ChEMBL | Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay | F | 7.87 | pIC50 | 13.5 | nM | IC50 | J Med Chem (2015) 58: 5751-5769 [PMID:26151231] |
| ChEMBL | Inhibition of CB1 receptor (unknown origin) | B | 7.87 | pIC50 | 13.5 | nM | IC50 | RSC Med Chem (2022) 13: 1300-1321 [PMID:36439976] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells | B | 7.88 | pIC50 | 13.2 | nM | IC50 | J Med Chem (2009) 52: 4496-4510 [PMID:19530697] |
| ChEMBL | Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay | F | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2014) 74: 73-84 [PMID:24445310] |
| ChEMBL | Antagonist activity against human CB1 receptor | F | 7.95 | pIC50 | 11.22 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2034-2039 [PMID:21334892] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHO cell membranes assessed as reduction in GTPgammaS binding after 30 mins by microbeta counting method | F | 8.01 | pIC50 | 9.7 | nM | IC50 | Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226] |
| ChEMBL | Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO-K1 cell membranes | B | 8.16 | pIC50 | 6.9 | nM | IC50 | J Med Chem (2018) 61: 10276-10298 [PMID:30339387] |
| ChEMBL | Inhibitory concentration tested against human Cannabinoid receptor 1 (hCB1) | B | 8.21 | pIC50 | 6.2 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 645-651 [PMID:15664830] |
| ChEMBL | Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells | B | 8.21 | pIC50 | 6.1 | nM | IC50 | J Med Chem (2006) 49: 7584-7587 [PMID:17181138] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 8.21 | pIC50 | 6.1 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2184-2187 [PMID:17293109] |
| ChEMBL | Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1441-1446 [PMID:15713403] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells | B | 8.29 | pIC50 | 5.1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 453-457 [PMID:20015647] |
| ChEMBL | Displacement of [3H]-rimonabant from human CB1 receptor expressed in CHO cell membranes after 60 mins by TopCount method | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2018) 61: 10276-10298 [PMID:30339387] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding | F | 8.35 | pIC50 | 4.5 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 453-457 [PMID:20015647] |
| ChEMBL | Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding | F | 8.35 | pIC50 | 4.5 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 26-30 [PMID:19954978] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHO-K1 cell membrane in presence of CP55940 by GTP-gamma-S assay | F | 8.35 | pIC50 | 4.5 | nM | IC50 | Bioorg Med Chem Lett (2024) 98: 129572-129572 [PMID:38043690] |
| ChEMBL | Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1962-1964 [PMID:21376588] |
| ChEMBL | Inverse agonist activity at human CB1 receptor expressed in African green monkey COS7 cells co-expressing G-protein in presence of CP55940 by IP3 assay | F | 8.49 | pIC50 | 3.2 | nM | IC50 | Bioorg Med Chem Lett (2024) 98: 129572-129572 [PMID:38043690] |
| ChEMBL | Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader | F | 8.49 | pIC50 | 3.2 | nM | IC50 | Eur J Med Chem (2010) 45: 1133-1139 [PMID:20047779] |
| ChEMBL | Antagonist activity at CB1 receptor by [35S]GTP-gamma-S binding assay | F | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2007) 15: 4077-4084 [PMID:17433696] |
| ChEMBL | Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay | F | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 453-457 [PMID:20015647] |
| ChEMBL | Binding affinity to human CB1 receptor by [35S]GTPgammaS binding assay | F | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2008) 51: 5608-5616 [PMID:18754613] |
| ChEMBL | Agonist activity at human CB1 receptor assessed as stimulation of [35S]GTPgammaS binding | F | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 479-482 [PMID:20005704] |
| ChEMBL | Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cell membrane by GTP-gamma-S assay | F | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2024) 98: 129572-129572 [PMID:38043690] |
| ChEMBL | Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level | F | 8.87 | pIC50 | 1.35 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3376-3381 [PMID:18448340] |
| ChEMBL | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after 90 secs by calcein-4 AAM dye-based FLIPR assay | F | 6.23 | pEC50 | 586 | nM | EC50 | Bioorg Med Chem (2018) 26: 4518-4531 [PMID:30077609] |
| ChEMBL | Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity | F | 6.62 | pEC50 | 240 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2546-2550 [PMID:19328683] |
| ChEMBL | Inverse 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 | 7.3 | pEC50 | 50.12 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4209-4214 [PMID:25096297] |
| ChEMBL | Inverse 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 | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4209-4214 [PMID:25096297] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay | F | 7.44 | pEC50 | 36 | nM | EC50 | Eur J Med Chem (2018) 154: 155-171 [PMID:29793210] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding | B | 7.74 | pEC50 | 18.2 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1022-1025 [PMID:19095444] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding | B | 7.74 | pEC50 | 18.2 | nM | EC50 | J Med Chem (2008) 51: 5397-5412 [PMID:18712856] |
| ChEMBL | Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding | B | 7.8 | pEC50 | 15.7 | nM | EC50 | J Med Chem (2009) 52: 4496-4510 [PMID:19530697] |
| ChEMBL | Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay | F | 8 | pEC50 | 10.1 | nM | EC50 | J Med Chem (2005) 48: 7486-7490 [PMID:16279809] |
| ChEMBL | Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay | F | 8.3 | pEC50 | 5 | nM | EC50 | Bioorg Med Chem (2016) 24: 1063-1070 [PMID:26827137] |
| ChEMBL | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay | F | 8.39 | pEC50 | 4.1 | nM | EC50 | ACS Med Chem Lett (2020) 11: 2504-2509 [PMID:33335674] |
| ChEMBL | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay | F | 8.39 | pEC50 | 4.1 | nM | EC50 | J Med Chem (2018) 61: 10276-10298 [PMID:30339387] |
| ChEMBL | Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572] |
| ChEMBL | Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1199-1206 [PMID:18083560] |
| ChEMBL | Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis | F | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (2013) 56: 9874-9896 [PMID:24175572] |
| 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 | 9.96 | pEC50 | 0.11 | nM | EC50 | Eur J Med Chem (2010) 45: 1133-1139 [PMID:20047779] |
| CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] | ||||||||
| ChEMBL | Antagonist activity at CB1 receptor in ICR mouse vas deferens assessed as reversal of WIN-55212-2-induced effect on electrically-stimulated contraction | F | 6.72 | pKd | 190.55 | nM | Kd | Bioorg Med Chem (2007) 15: 7480-7493 [PMID:17870539] |
| ChEMBL | Displacement of [3H]CP55940 from mouse brain CB1R expressed in CHOK1 cell membranes | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2017) 60: 1126-1141 [PMID:28085283] |
| ChEMBL | Displacement of [3H]CP55490 from CB1 receptor in mouse brain plasma membrane by radioligand displacement analysis | B | 8.35 | pKi | 4.5 | nM | Ki | J Med Chem (2023) 66: 11985-12004 [PMID:37611316] |
| ChEMBL | Displacement of [3H]-CP55,940 from CB1 receptor in mouse whole brain membranes after 60 mins by liquid scintillation spectrometry | B | 8.55 | pKi | 2.82 | nM | Ki | Eur J Med Chem (2016) 121: 194-208 [PMID:27240274] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in CD1 mouse brain | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2005) 48: 7351-7362 [PMID:16279795] |
| ChEMBL | Displacement of [3H]-CP55,940 from CB1 receptor in CD1 mouse brain membranes after 60 mins by liquid scintillation counting method | B | 8.74 | pKi | 1.8 | nM | Ki | Eur J Med Chem (2016) 121: 194-208 [PMID:27240274] |
| ChEMBL | Displacement of [3H]CP55940 from CB1 receptor in CD1 mouse brain membrane without cerebellum by liquid scintillation counting analysis | B | 8.82 | pKi | 1.5 | nM | Ki | Eur J Med Chem (2013) 62: 256-269 [PMID:23357307] |
| ChEMBL | Inverse agonist at mouse brain CB1R expressed in CHOK1 cell membranes assessed as inhibition of CP55940-stimulated [35S]GTP-gammaS binding measured after 60 mins by scintillation spectrometry | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2017) 60: 1126-1141 [PMID:28085283] |
| ChEMBL | Antagonist activity at CB1 receptor in mouse brain membrane assessed as inhibition of CP55490-induced GTPgammaS binding by [35S]GTPgammaS binding analysis | F | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2023) 66: 11985-12004 [PMID:37611316] |
| ChEMBL | Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction | F | 5.05 | pEC50 | 8990 | nM | EC50 | Bioorg Med Chem (2007) 15: 7480-7493 [PMID:17870539] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [3H]-WIN55212-2 from CB1R in rat brain membranes incubated for 60 mins by radioligand competitive binding assay | B | 7.74 | pKi | 18 | nM | Ki | ACS Med Chem Lett (2023) 14: 479-486 [PMID:37077391] |
| ChEMBL | Binding affinity against Cannabinoid receptor 1 in rat forebrain | B | 7.94 | pKi | 11.5 | nM | Ki | J Med Chem (1999) 42: 769-776 [PMID:10052983] |
| ChEMBL | Antagonist activity at rat forebrain CB1R assessed as inhibition constant | B | 7.94 | pKi | 11.5 | nM | Ki | RSC Med Chem (2022) 13: 497-510 [PMID:35694688] |
| ChEMBL | Displacement of [3H]SR141716A from CB1 receptor in rat cerebellum membrane | B | 8.19 | pKi | 6.5 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 3471-3475 [PMID:19457667] |
| ChEMBL | Binding affinity in a competition assay by displacement of [3H]CP-55940 from Cannabinoid receptor 1 in rat whole brain membrane preparation | B | 8.21 | pKi | 6.18 | nM | Ki | J Med Chem (2002) 45: 2708-2719 [PMID:12061874] |
| ChEMBL | Displacement of [3H]SR141716A from CB1 receptor in rat cerebellum by scintillation spectrometry | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2009) 52: 4329-4337 [PMID:19527048] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from CB1 receptor in rat cerebellar membrane by liquid scintillation counting | B | 8.7 | pKi | 1.98 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 639-643 [PMID:19128970] |
| ChEMBL | Binding affinity was determined by using a competition assay with [125 I]- AM251 against rat cannabinoid receptor 1 | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2003) 46: 642-645 [PMID:12570386] |
| ChEMBL | Inhibition of [3H]CP-55940 binding to cannabinoid receptor 1 in rat brain membranes. | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2002) 45: 1447-1459 [PMID:11906286] |
| ChEMBL | Binding affinity in a competition assay by displacement of [3H]- SR-141716 from Cannabinoid receptor 1 in rat whole brain membrane preparation | B | 8.93 | pKi | 1.18 | nM | Ki | J Med Chem (2002) 45: 2708-2719 [PMID:12061874] |
| ChEMBL | Displacement of [3H]SR141716A from rat brain CB1 receptor | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 5351-5354 [PMID:19683918] |
| ChEMBL | Displacement of [3H]SR141716A from CB1 receptor in rat brain | B | 9.19 | pKi | 0.65 | nM | Ki | J Med Chem (2009) 52: 234-237 [PMID:19102698] |
| ChEMBL | Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding | F | 9.51 | pKi | 0.31 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3376-3381 [PMID:18448340] |
| ChEMBL | Displacement of [3H]SR141716A from CB1 receptor in Sprague-Dawley rat cerebellum membrane | B | 5.41 | pIC50 | 3920 | nM | IC50 | Eur J Med Chem (2008) 43: 513-539 [PMID:17582659] |
| ChEMBL | Displacement of [3H]CP55940 from rat brain membrane CB1 receptor incubated for 3 hrs by scintillation counter analysis | B | 7.2 | pIC50 | 63.1 | nM | IC50 | J Med Chem (2023) 66: 6414-6435 [PMID:37127287] |
| ChEMBL | Displacement of [3H]CP55940 from rat brain membrane CB1 receptor incubated for 3 hrs by scintillation counter analysis | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2023) 66: 6414-6435 [PMID:37127287] |
| ChEMBL | Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation counting | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4913-4918 [PMID:21741835] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from CB1 receptor in rat cerebellar membrane by liquid scintillation counting | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 639-643 [PMID:19128970] |
| ChEMBL | Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in Sprague-Dawley rat cerebellar membrane by liquid scintillation spectrometry | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4692-4697 [PMID:19596576] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellar membrane | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 142-145 [PMID:19022666] |
| ChEMBL | Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in Sprague-Dawley rat cerebellar membrane by liquid scintillation spectrometry | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1899-1902 [PMID:19269817] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1R in Sprague-Dawley rat cerebellar membrane | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2009) 17: 3080-3092 [PMID:19328001] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellar membrane | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6632-6636 [PMID:19850473] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellar membrane | B | 8.34 | pIC50 | 4.53 | nM | IC50 | Bioorg Med Chem (2010) 18: 1149-1162 [PMID:20045337] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellum after 1 hr by liquid scintillation counting | B | 8.34 | pIC50 | 4.53 | nM | IC50 | Bioorg Med Chem (2010) 18: 6377-6388 [PMID:20673729] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellum by liquid scintillation spectrometry | B | 8.34 | pIC50 | 4.53 | nM | IC50 | J Med Chem (2008) 51: 7216-7233 [PMID:18954042] |
| ChEMBL | Inhibition of cannabinoid CB1 receptor in Sprague-Dawley rat brain | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2385-2389 [PMID:18337096] |
| ChEMBL | Binding affinity to CB1 receptor in rat brain synaptosomal membranes | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4573-4577 [PMID:20584609] |
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebella membrane | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem (2008) 16: 4035-4051 [PMID:18243711] |
| ChEMBL | Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding | F | 4.25 | pEC50 | 56305 | nM | EC50 | J Med Chem (2010) 53: 7048-7060 [PMID:20845959] |
| ChEMBL | Agonist activity at rat brain membrane CB1 receptor assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins | B | 5.51 | pEC50 | 3086 | nM | EC50 | ACS Med Chem Lett (2023) 14: 479-486 [PMID:37077391] |
| ChEMBL | Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptor | B | 9.77 | pEC50 | 0.17 | nM | EC50 | Proc Natl Acad Sci U S A (2007) 104: 20588-20593 [PMID:18077343] |
| 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 | 2.85 | pKi | 2.85 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method | B | 4.4 | pKi | >40000 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation spectrometry | B | 5.11 | pKi | 7700 | nM | Ki | Bioorg Med Chem (2018) 26: 4518-4531 [PMID:30077609] |
| ChEMBL | Displacement of [3H]WIN-552122 from human recombinant CB2 receptor expressed in CHOK1 cells | B | 5.7 | pKi | 1990 | nM | Ki | J Med Chem (2007) 50: 5951-5966 [PMID:17979261] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 5.79 | pKi | 1640 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307] |
| ChEMBL | In vitro displacement of CP-55940 binding to human CB2 receptor expressed in CHO cells | B | 5.8 | pKi | 1580 | nM | Ki | J Med Chem (2005) 48: 1823-1838 [PMID:15771428] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells | B | 5.8 | pKi | 1580 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2770-2775 [PMID:20363132] |
| ChEMBL | Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells | B | 5.8 | pKi | 1580 | nM | Ki | J Med Chem (2004) 47: 627-643 [PMID:14736243] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells | B | 5.8 | pKi | 1580 | nM | Ki | Eur J Med Chem (2008) 43: 2627-2638 [PMID:18342403] |
| ChEMBL | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2 | B | 5.8 | pKi | 1580 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010] |
| ChEMBL | Binding affinity to CB2 receptor | B | 5.8 | pKi | 1569 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Displacement of [3H]-CP55,940 from human CB2 receptor transfected in CHO cell membranes after 60 mins by liquid scintillation spectrometry | B | 5.85 | pKi | 1400 | nM | Ki | Eur J Med Chem (2016) 121: 194-208 [PMID:27240274] |
| ChEMBL | Binding affinity to CB2 receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 2439-2446 [PMID:18363352] |
| ChEMBL | Displacement of [3H]rimonabant from human CB2 receptor expressed in HEK293 cells by liquid scintillation counting | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572] |
| ChEMBL | Displacement of [3H]- CP55940 from human CB2R expressed in CHO-K1 cells membrane by Cheng-Prusoff equation analysis | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2022) 65: 2374-2387 [PMID:35084860] |
| ChEMBL | Displacement of [3H]CP-55940 from CB2 receptor by scintillation counting | B | 6.03 | pKi | 927 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6209-6212 [PMID:19767206] |
| ChEMBL | Displacement of [3H]CP55940 from CB2 receptor | B | 6.03 | pKi | 927 | nM | Ki | J Med Chem (2011) 54: 2961-2970 [PMID:21428406] |
| ChEMBL | Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter | B | 6.05 | pKi | 900 | nM | Ki | J Med Chem (2012) 55: 7967-7977 [PMID:22916707] |
| ChEMBL | Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 6.05 | pKi | 900 | nM | Ki | ACS Med Chem Lett (2013) 4: 41-45 [PMID:24900561] |
| ChEMBL | Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in Sf9 cells | B | 6.07 | pKi | 851.14 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 2034-2039 [PMID:21334892] |
| ChEMBL | Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding | F | 6.09 | pKi | 815 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3376-3381 [PMID:18448340] |
| ChEMBL | Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells | B | 6.1 | pKi | 790 | nM | Ki | Eur J Med Chem (2010) 45: 5878-5886 [PMID:20943290] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 6.1 | pKi | 790 | nM | Ki | J Med Chem (2008) 51: 1560-1576 [PMID:18293908] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells | B | 6.1 | pKi | 790 | nM | Ki | J Med Chem (2008) 51: 5075-5084 [PMID:18680276] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 6.1 | pKi | 790 | nM | Ki | Bioorg Med Chem (2008) 16: 7510-7515 [PMID:18579386] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 6.1 | pKi | 790 | nM | Ki | Bioorg Med Chem (2009) 17: 5549-5564 [PMID:19595596] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells | B | 6.1 | pKi | 790 | nM | Ki | J Med Chem (2010) 53: 5915-5928 [PMID:20718492] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 6.1 | pKi | 790 | nM | Ki | J Med Chem (2011) 54: 5444-5453 [PMID:21702498] |
| ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB2 receptor transfected in HEK cells | B | 6.1 | pKi | 790 | nM | Ki | J Med Chem (2012) 55: 5391-5402 [PMID:22548457] |
| ChEMBL | Displacement of [3H]CP55940 from human recombinant CB2 receptor transfected in HEK cell membranes | B | 6.1 | pKi | 790 | nM | Ki | Eur J Med Chem (2012) 58: 30-43 [PMID:23085772] |
| ChEMBL | Binding affinity to human CB2 receptor by [35S]GTPgammaS binding assay | F | 6.16 | pKi | 697 | nM | Ki | J Med Chem (2008) 51: 5608-5616 [PMID:18754613] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells | B | 6.25 | pKi | 560 | nM | Ki | J Med Chem (2008) 51: 2439-2446 [PMID:18363352] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 6.25 | pKi | 560 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1278-1283 [PMID:20018510] |
| ChEMBL | Displacement of radioligand from human CB2 receptor expressed in HEK293 cells | B | 6.26 | pKi | 554 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1199-1206 [PMID:18083560] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting | B | 6.28 | pKi | 522 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
| ChEMBL | Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells | B | 6.4 | pKi | 398.11 | nM | Ki | J Med Chem (2009) 52: 1975-1982 [PMID:19338356] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | B | 6.4 | pKi | 398.11 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells | B | 6.5 | pKi | 313 | nM | Ki | J Med Chem (2008) 51: 3526-3539 [PMID:18512901] |
| ChEMBL | Displacement of [3H]CP55940 from human CB2 receptor expressed in CHOK1 cells | B | 6.5 | pKi | 313 | nM | Ki | J Med Chem (2010) 53: 7048-7060 [PMID:20845959] |
| ChEMBL | Binding affinity at cannabinoid receptor 2 in a competition assay with [3H]CP-55940 as radioligand | B | 6.5 | pKi | 313 | nM | Ki | J Med Chem (2002) 45: 2708-2719 [PMID:12061874] |
| ChEMBL | Displacement of [3H]CP55940 from CB2 receptor expressed in CHO-K1 cells | B | 6.5 | pKi | 313 | nM | Ki | J Med Chem (2012) 55: 2820-2834 [PMID:22372835] |
| ChEMBL | Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO cell membranes | B | 6.5 | pKi | 313 | nM | Ki | Bioorg Med Chem (2016) 24: 1063-1070 [PMID:26827137] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting | B | 6.9 | pKi | 126 | nM | Ki | Eur J Med Chem (2010) 45: 1133-1139 [PMID:20047779] |
| ChEMBL | Displacement of [3H]-CP-55940 from human CB2 receptor expressed in HEK293T cell membranes by scintillation counting | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem (2014) 22: 3245-3251 [PMID:24856183] |
| ChEMBL | Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay | F | 5.01 | pIC50 | 9800 | nM | IC50 | Eur J Med Chem (2014) 74: 73-84 [PMID:24445310] |
| ChEMBL | Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay | F | 5.04 | pIC50 | 9100 | nM | IC50 | J Med Chem (2015) 58: 5751-5769 [PMID:26151231] |
| ChEMBL | Binding affinity to human CB2 receptor by [35S]GTPgammaS binding assay | F | 5.34 | pIC50 | 4570 | nM | IC50 | J Med Chem (2008) 51: 5608-5616 [PMID:18754613] |
| ChEMBL | Inverse agonist activity at human CB2 receptor expressed in CHO-K1 cell membrane in presence of CP55940 by GTP-gamma-S assay | F | 5.59 | pIC50 | 2600 | nM | IC50 | Bioorg Med Chem Lett (2024) 98: 129572-129572 [PMID:38043690] |
| ChEMBL | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting | B | 5.7 | pIC50 | 1980 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4913-4918 [PMID:21741835] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells | B | 5.71 | pIC50 | 1939.8 | nM | IC50 | J Med Chem (2008) 51: 5397-5412 [PMID:18712856] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells | B | 5.75 | pIC50 | 1760 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 142-145 [PMID:19022666] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry | B | 5.75 | pIC50 | 1760 | nM | IC50 | J Med Chem (2008) 51: 7216-7233 [PMID:18954042] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry | B | 5.75 | pIC50 | 1760 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1899-1902 [PMID:19269817] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells | B | 5.75 | pIC50 | 1760 | nM | IC50 | Bioorg Med Chem (2008) 16: 4035-4051 [PMID:18243711] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human recombinant CB2 receptor expressed in CHO-K1 cell membrane | B | 5.75 | pIC50 | 1760 | nM | IC50 | Bioorg Med Chem (2010) 18: 1149-1162 [PMID:20045337] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting | B | 5.75 | pIC50 | 1760 | nM | IC50 | Bioorg Med Chem (2010) 18: 6377-6388 [PMID:20673729] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells | B | 5.75 | pIC50 | 1760 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2385-2389 [PMID:18337096] |
| ChEMBL | Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells | B | 5.75 | pIC50 | 1760 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6632-6636 [PMID:19850473] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells | B | 5.79 | pIC50 | 1631.1 | nM | IC50 | J Med Chem (2009) 52: 4496-4510 [PMID:19530697] |
| ChEMBL | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 639-643 [PMID:19128970] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells | B | 6.22 | pIC50 | 603.3 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2184-2187 [PMID:17293109] |
| ChEMBL | Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2006) 49: 7584-7587 [PMID:17181138] |
| ChEMBL | Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay | B | 7.03 | pIC50 | 92.5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6632-6636 [PMID:19850473] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1022-1025 [PMID:19095444] |
| ChEMBL | Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity | F | 4.51 | pEC50 | 31210 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2546-2550 [PMID:19328683] |
| ChEMBL | Inverse agonist activity at human CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2018) 61: 10276-10298 [PMID:30339387] |
| CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] | ||||||||
| ChEMBL | Binding affinity against Cannabinoid receptor 2 in mouse spleen | B | 5.79 | pKi | 1640 | nM | Ki | J Med Chem (1999) 42: 769-776 [PMID:10052983] |
| ChEMBL | Antagonist activity at mouse spleen CB2R assessed as inhibition constant | B | 5.79 | pKi | 1640 | nM | Ki | RSC Med Chem (2022) 13: 497-510 [PMID:35694688] |
| ChEMBL | Displacement of [3H]CP-55940 from CB2 receptor in CD1 mouse spleen | B | 6.29 | pKi | 514 | nM | Ki | J Med Chem (2005) 48: 7351-7362 [PMID:16279795] |
| ChEMBL | Displacement of [3H]-CP55,940 from CB2 receptor in CD1 mouse spleen homogenates after 60 mins by liquid scintillation counting method | B | 6.29 | pKi | 514 | nM | Ki | Eur J Med Chem (2016) 121: 194-208 [PMID:27240274] |
| ChEMBL | Displacement of [3H]CP55940 from CB2 receptor in CD1 mouse spleen membrane by liquid scintillation counting analysis | B | 6.43 | pKi | 375 | nM | Ki | Eur J Med Chem (2013) 62: 256-269 [PMID:23357307] |
| ChEMBL | Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay | B | 7.82 | pEC50 | 15 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6] | ||||||||
| ChEMBL | Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay | B | 5.7 | pEC50 | 2010 | nM | EC50 | ACS Med Chem Lett (2013) 4: 41-45 [PMID:24900561] |
| 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 | 5.7 | pEC50 | 2010 | nM | EC50 | Medchemcomm (2014) 5: 632-649 |
| GtoPdb | - | - | 6.55 | pEC50 | 280 | nM | EC50 |
Br J Pharmacol (2010) 160: 604-14 [PMID:20136841]; J Pharmacol Exp Ther (2011) 337: 236-46 [PMID:21233197] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG at holding potential of -80 mV to +40 mV | B | 5.32 | pIC50 | 4800 | nM | IC50 | Bioorg Med Chem (2010) 18: 6377-6388 [PMID:20673729] |
| ChEMBL | Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay | B | 5.55 | pIC50 | 2790 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4913-4918 [PMID:21741835] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: CHRM2 | F | 5.21 | pIC50 | 6215.16 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 | pIC50 | 10100 | 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 | pEC50 | 10100 | nM | EC50 | Medchemcomm (2014) 5: 632-649 |
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]
