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ChEMBL ligand: CHEMBL181633 (AM-630) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]