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 [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 | 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 | 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 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 | 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 | 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 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]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]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]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 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 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 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]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 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]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 CHO cells incubated for 1 hr | B | 7.97 | pKi | 10.6 | nM | Ki | J Med Chem (2012) 55: 9973-9987 [PMID:23072339] |
| 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 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]-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]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-K1 cells | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (2012) 55: 2820-2834 [PMID:22372835] |
| 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 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 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]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 | Binding affinity to CB1 receptor | B | 8.7 | pKi | 1.98 | nM | Ki | J Med Chem (2008) 51: 2439-2446 [PMID:18363352] |
| 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 | 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 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 | 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 [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 | 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 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 | 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 | 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 HEK293 cells | B | 8.93 | pKi | 1.18 | nM | Ki | J Med Chem (2010) 53: 7048-7060 [PMID:20845959] |
| 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]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 | 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 | 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 | 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 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 | 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 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]-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 | 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 | ||||||||