AG-26 [Ligand Id: 6268] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1289260 (AG-26) |
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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 | Allosteric antagonist activity against human CB1 receptor expressed in HEK293 cells membrane measured after 60 mins by [35S]GTPgammaS binding assay | F | 5.25 | pIC50 | 5623.41 | nM | IC50 | J Med Chem (2022) 65: 257-270 [PMID:34929081] |
| ChEMBL | Antagonist activity at N-terminal tagged human CB1 receptor transfected with HEK293 cells assessed as forskolin-stimulated cAMP level in presence of CP55940 by BRET assay | F | 5.38 | pIC50 | 4168.69 | nM | IC50 | J Med Chem (2022) 65: 257-270 [PMID:34929081] |
| ChEMBL | Allosteric antagonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization incubated for 15 mins FLIPR assay | F | 6.67 | pIC50 | 213.8 | nM | IC50 | J Med Chem (2022) 65: 257-270 [PMID:34929081] |
| CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] | ||||||||
| ChEMBL | Allosteric antagonist activity against mouse CB1 receptor expressed in HEK293 cells membrane measured after 60 mins by [35S]GTPgammaS binding assay | F | 5.43 | pIC50 | 3715.35 | nM | IC50 | J Med Chem (2022) 65: 257-270 [PMID:34929081] |
| FPR2/ALX/Lipoxin A4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090] | ||||||||
| ChEMBL | Agonist activity at human FPR2 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method | B | 6 | pEC50 | 990 | nM | EC50 | J Med Chem (2020) 63: 9003-9019 [PMID:32407089] |
| GtoPdb | - | - | 6.3 | pEC50 | - | - | - | Mol Pharmacol (2010) 77: 159-70 [PMID:19903830] |
| ChEMBL | Agonist activity against human FPR2 expressed in human HL60 cells by Fluo-4AM dye based intracellular Ca2+ mobilization assay | F | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem (2015) 23: 4072-4081 [PMID:25882522] |
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]
