PF-514273 [Ligand Id: 11693] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL484929 (PF-0514273) |
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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 CB1 receptor | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting | B | 9 | pKi | 1 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay | F | 9.09 | pKi | 0.82 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting | F | 9.09 | pKi | 0.82 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
| GtoPdb | Antagonism of CP-55940-induced GTPgamma[35S] binding at CB1 expressed in CHOK1 cells | - | 9.09 | pKi | 0.82 | nM | Ki | J Med Chem (2009) 52: 2652-5 [PMID:19351113] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Binding affinity to CB2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting | B | 5 | pKi | >10000 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
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]
