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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]