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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] |
CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] | ||||||||
ChEMBL | Displacement of [3H]CP55490 from CB1 receptor in mouse brain plasma membrane by radioligand displacement analysis | B | 8.09 | pKi | 8.1 | nM | Ki | J Med Chem (2023) 66: 11985-12004 [PMID:37611316] |
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 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]