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ChEMBL ligand: CHEMBL412262 (BMS-646256, Ibipinabant, Slv319, SLV-319) |
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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 | Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells | F | 9.9 | pKd | 0.13 | nM | Kd | J Med Chem (2004) 47: 627-643 [PMID:14736243] |
ChEMBL | Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells | F | 9.9 | pKd | 0.13 | nM | Kd | Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010] |
ChEMBL | Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release | F | 9.9 | pKd | 0.13 | nM | Kd | Bioorg Med Chem Lett (2010) 20: 1752-1757 [PMID:20137935] |
ChEMBL | Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (2008) 51: 2115-2127 [PMID:18335976] |
ChEMBL | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1 | B | 8.11 | pKi | 7.8 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010] |
ChEMBL | Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (2004) 47: 627-643 [PMID:14736243] |
ChEMBL | Binding affinity to CB1 receptor | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (2008) 51: 2439-2446 [PMID:18363352] |
ChEMBL | Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting | B | 8.11 | pKi | 7.8 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572] |
ChEMBL | Displacement of [3H]CP-55940 from human cannabinoid CB1 receptor expressed in CHO cells | B | 8.11 | pKi | 7.8 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1752-1757 [PMID:20137935] |
GtoPdb | Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells | - | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (2004) 47: 627-43 [PMID:14736243] |
ChEMBL | Displacement of radioligand from human CB1 receptor expressed in HEK293 cells | B | 8.39 | pKi | 4.1 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1199-1206 [PMID:18083560] |
ChEMBL | Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (2009) 52: 1975-1982 [PMID:19338356] |
ChEMBL | Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting | B | 9.38 | pKi | 0.42 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6856-6860 [PMID:21962575] |
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 | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (2009) 52: 1975-1982 [PMID:19338356] |
ChEMBL | Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2006) 49: 7584-7587 [PMID:17181138] |
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
GtoPdb | Displacement of specific CP-55,940 binding in CHO cells stably transfected with human CB2 receptor | - | 5.1 | pKi | 7943 | nM | Ki | J Med Chem (2004) 47: 627-43 [PMID:14736243] |
ChEMBL | Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells | B | 5.1 | pKi | 7943 | nM | Ki | J Med Chem (2004) 47: 627-643 [PMID:14736243] |
ChEMBL | Binding affinity to CB2 receptor | B | 5.1 | pKi | 7943 | nM | Ki | J Med Chem (2008) 51: 2439-2446 [PMID:18363352] |
ChEMBL | Displacement of [3H]rimonabant from human CB2 receptor expressed in HEK293 cells by liquid scintillation counting | B | 5.1 | pKi | 7943 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572] |
ChEMBL | Displacement of [3H]CP-55940 from human cannabinoid CB2 receptor expressed in CHO cells | B | 5.1 | pKi | 7943 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1752-1757 [PMID:20137935] |
ChEMBL | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2 | B | 5.13 | pKi | 7493 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010] |
ChEMBL | Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells | B | 5.7 | pKi | 1995.26 | nM | Ki | J Med Chem (2009) 52: 1975-1982 [PMID:19338356] |
ChEMBL | Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2006) 49: 7584-7587 [PMID:17181138] |
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]