rimonabant [Ligand Id: 743] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL111 (Acomplia, Rimonabant, SR-14171, SR-141716, SR-141716A, SR141716)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Mouse [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
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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]-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]-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]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 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 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 Bioorg. Med. Chem. Lett. (2010) 20: 2770-2775 [PMID:20363132]
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 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-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-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 HEK293 cells B 7.92 pKi 12 nM Ki J. Med. Chem. (2008) 51: 5075-5084 [PMID:18680276]
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 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-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 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 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 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 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 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]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 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 [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 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 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 B 7.87 pIC50 13.5 nM IC50 J. Med. Chem. (2015) 58: 5751-5769 [PMID:26151231]
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 B 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 B 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 B 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 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 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 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