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 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]
