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 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]
