MSA-2 [Ligand Id: 13531] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4434776 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| stimulator of interferon response cGAMP interactor 1/Stimulator of interferon genes protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523377] [GtoPdb: 2902] [UniProtKB: Q86WV6] | ||||||||
| ChEMBL | Agonist activity at wild type human STING expressed in baculovirus infected Sf21 insect cells | B | 4.62 | pEC50 | 24000 | nM | EC50 | J Med Chem (2021) 64: 1649-1669 [PMID:33470814] |
| ChEMBL | Agonist activity at human STING HAQ mutant | B | 5.08 | pEC50 | 8300 | nM | EC50 | Eur J Med Chem (2022) 238: 114482-114482 [PMID:35671593] |
| ChEMBL | Agonist activity at STING in human THP1-Dual cells assessed as ISG pathway activation incubated for 24 hrs by Quanti-Luc or Quanti-blue reagent based luminescence assay | B | 5.09 | pEC50 | 8140 | nM | EC50 | Eur J Med Chem (2022) 241: 114627-114627 [PMID:35963129] |
| GtoPdb | Determined in a filtration binding assay measuring displacement of [3H]-cGAMP from full length wild type STING. | - | 5.61 | pEC50 | 2480 | nM | EC50 | WO2018067423A1. BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS (2018) |
| GtoPdb | Determined in a filtration binding assay measuring displacement of [3H]-cGAMP from full length STING (with HAQ modification) in human THP1 cells. | - | 5.76 | pEC50 | 1720 | nM | EC50 |
J Med Chem (2020) 63: 3785-3816 [PMID:31820978]; WO2018067423A1. BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS (2018) |
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]
