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 recombinant human CB2R expressed in CHOK1 cells assessed as increase in NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent based cAMP Hunter assay F 5.5 pEC50 3150 nM EC50 J Med Chem (2020) 63: 7369-7391 [PMID:32515588]
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 F 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 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]