AM-630 [Ligand Id: 750] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL181633 (AM-630)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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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 Binding affinity to cannabinoid CB1 receptor B 5.29 pKi 5152 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of [3H]CP 55940 from human CB1 receptor in cell free system B 5.29 pKi 5152 nM Ki Eur. J. Med. Chem. (2011) 46: 547-555 [PMID:21183257]
ChEMBL Inverse agonist activity at human CB1 receptor F 5.29 pKi 5152 nM Ki Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Displacement of [3H]-CP-55940 from human CB1 expressed in CHO cells after 90 mins by TopCount scintillation counting method B 6 pKi >1000 nM Ki Eur J Med Chem (2018) 146: 68-78 [PMID:29360044]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells B 6.08 pKi 840 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6505-6510 [PMID:17942307]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]-CP-55940 from human CB2 expressed in CHO cells after 90 mins by TopCount scintillation counting method B 7.04 pKi 91 nM Ki Eur J Med Chem (2018) 146: 68-78 [PMID:29360044]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells B 7.44 pKi 36 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6505-6510 [PMID:17942307]
GtoPdb - - 7.5 pKi 31.6 nM Ki Br J Pharmacol (1999) 126: 665-672 [PMID:10188977]
ChEMBL Displacement of [3H]CP 55940 from human CB2 receptor in cell free system B 7.51 pKi 31.2 nM Ki Eur. J. Med. Chem. (2011) 46: 547-555 [PMID:21183257]
ChEMBL Inverse agonist activity at CB2 receptor (unknown origin) B 7.51 pKi 31.2 nM Ki Eur J Med Chem (2016) 124: 17-35 [PMID:27560280]
ChEMBL Inverse agonist activity at human CB2 receptor F 7.51 pKi 31.2 nM Ki Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Binding affinity for human cannabinoid receptor 2 was determined by using [3H]CP-55940 as radioligand B 7.51 pKi 31.2 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 783-786 [PMID:15664857]
ChEMBL Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes measured after 90 mins B 7.51 pKi 31.2 nM Ki Eur J Med Chem (2019) 161: 239-251 [PMID:30359820]
ChEMBL Binding affinity to cannabinoid CB2 receptor B 7.51 pKi 31.2 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Antagonist activity at cannabinoid CB2 receptor F 5.14 pIC50 7200 nM IC50 J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Inverse agonist activity at human CB2 receptor expressed in Sf9 cells coexpressing Galpha i2 assessed as Galpha GTPase activity using [gamma-33P]GTP by scintillation counting in presence of CP55940 B 6.22 pEC50 602.56 nM EC50 Bioorg. Med. Chem. (2014) 22: 3938-3946 [PMID:24984935]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay F 6.78 pEC50 167 nM EC50 Eur J Med Chem (2018) 154: 155-171 [PMID:29793210]
ChEMBL Agonist activity at human CB2 receptor expressed CHO cells by [35S]GTPgamma binding assay F 7.12 pEC50 76.6 nM EC50 J. Med. Chem. (2009) 52: 433-444 [PMID:19115816]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Inverse agonist activity at mouse CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 5 mins by fluorescence assay B 7.6 pEC50 25 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
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 8.05 pEC50 9 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]