GW842166 [Ligand Id: 12753] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL225411 (GW 842166, GW-842166, GW842166, Gw-842,166x, Gw842166x, GW 842166X, GW842166X) |
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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 | Agonist activity at CB1 receptor | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem (2008) 16: 1111-1124 [PMID:18006322] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor | B | 4.52 | pEC50 | >30000 | nM | EC50 | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry | F | 4.52 | pEC50 | >30000 | nM | EC50 | J Med Chem (2009) 52: 5785-5788 [PMID:19743867] |
| ChEMBL | Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells by calcium mobilization assay | F | 5 | pEC50 | >10000 | nM | EC50 | Eur J Med Chem (2015) 93: 16-32 [PMID:25644673] |
| ChEMBL | Agonist activity at CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as increase in intracellular calcium level by microplate reader based assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2015) 58: 5751-5769 [PMID:26151231] |
| ChEMBL | Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay | F | 5 | pEC50 | >10000 | nM | EC50 | Eur J Med Chem (2017) 137: 598-611 [PMID:28651225] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Displacement of [3H]Win55212 form human CB2 receptor transfected in HEK cells | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1604-1609 [PMID:19243942] |
| ChEMBL | Displacement of [3H]CP-55940 form human CB2 receptor transfected in HEK cells | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1604-1609 [PMID:19243942] |
| ChEMBL | Agonist activity at CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as increase in intracellular calcium level by microplate reader based assay | F | 6.36 | pEC50 | 437 | nM | EC50 | J Med Chem (2015) 58: 5751-5769 [PMID:26151231] |
| ChEMBL | Agonist activity at CB2 receptor (unknown origin) expressed in CHO cells by calcium mobilization assay | F | 6.37 | pEC50 | 431 | nM | EC50 | Eur J Med Chem (2015) 93: 16-32 [PMID:25644673] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release | F | 6.46 | pEC50 | 350 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1604-1609 [PMID:19243942] |
| ChEMBL | Agonist activity at CB2 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay | F | 6.46 | pEC50 | 342.8 | nM | EC50 | Eur J Med Chem (2017) 137: 598-611 [PMID:28651225] |
| ChEMBL | Agonist activity at CB2 receptor (unknown origin) expressed in CHO cells co-expressing G-alpha16 incubated for 24 hrs by fluo-4 AM dye based whole-cell calcium mobilization assay | F | 6.46 | pEC50 | 342.8 | nM | EC50 | ACS Med Chem Lett (2017) 8: 678-681 [PMID:28626532] |
| GtoPdb | - | - | 7.2 | pEC50 | 63 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 385-9 [PMID:17084082] |
| ChEMBL | Agonist activity at human recombinant cannabinoid CB2 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry | F | 7.2 | pEC50 | 63 | nM | EC50 | J Med Chem (2009) 52: 5785-5788 [PMID:19743867] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level | F | 7.2 | pEC50 | 63 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1725-1729 [PMID:18255291] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in Saccharomyces cerevisiae cells | F | 7.2 | pEC50 | 63 | nM | EC50 | J Med Chem (2007) 50: 2597-2600 [PMID:17477516] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor | B | 7.3 | pEC50 | 50 | nM | EC50 | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Agonist activity at CB2 receptor | F | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem (2008) 16: 1111-1124 [PMID:18006322] |
| CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] | ||||||||
| GtoPdb | - | - | 7.04 | pEC50 | 91 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 385-9 [PMID:17084082] |
| ChEMBL | Agonist activity at rat CB2 receptor | F | 7.04 | pEC50 | 91 | nM | EC50 | J Med Chem (2007) 50: 2597-2600 [PMID:17477516] |
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]
