MRS5698 [Ligand Id: 8421] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2064657 (MRS-5698) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | Displacement of [3H]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting | B | 8.46 | pKi | 3.49 | nM | Ki | J Med Chem (2012) 55: 4847-4860 [PMID:22559880] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human recombinant A3 adenosine receptor expressed in CHO cells after 60 mins by liquid scintillation counting | B | 8.46 | pKi | 3.49 | nM | Ki | J Med Chem (2014) 57: 9901-9914 [PMID:25422861] |
| ChEMBL | Binding affinity to human A3AR assessed as inhibitor constant | B | 8.46 | pKi | 3.49 | nM | Ki | ACS Med Chem Lett (2020) 11: 1935-1941 [PMID:33062176] |
| GtoPdb | - | - | 8.5 | pKi | - | - | - | J Med Chem (2012) 55: 4847-60 [PMID:22559880] |
| ChEMBL | Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay | B | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay | F | 8.3 | pEC50 | 5.01 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay | F | 8.92 | pEC50 | 1.2 | nM | EC50 | J Med Chem (2012) 55: 4847-4860 [PMID:22559880] |
| ChEMBL | Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay | B | 9.5 | pEC50 | 0.32 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| A3 receptor/Adenosine A3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618] | ||||||||
| ChEMBL | Displacement of [3H]CGS21680 from mouse adenosine A3 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting | B | 8.51 | pKi | 3.08 | nM | Ki | J Med Chem (2012) 55: 4847-4860 [PMID:22559880] |
| ChEMBL | Displacement of [125I]I-AB-MECA from mouse A3 adenosine receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting | B | 8.51 | pKi | 3.08 | nM | Ki | J Med Chem (2014) 57: 9901-9914 [PMID:25422861] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by PDSP screening | B | 4.91 | pIC50 | 12200 | nM | IC50 | J Med Chem (2014) 57: 9901-9914 [PMID:25422861] |
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]
