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ChEMBL ligand: CHEMBL2105747 (A-2A (3), A2A (3), A2A-(3), RO-4494351, RO4494351, RO-4494351-000, RO-4494351000, RO4494351-000, RO-4494351-002, RO4494351-002, SYN-115, SYN115, Tozadenant) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Displacement of [3H]-DPCPX from recombinant human A1 receptor expressed in CHO-K1 cells incubated for 70 mins by liquid scintillation counting method | B | 5.47 | pKi | 3380 | nM | Ki | Eur J Med Chem (2021) 214: 113214-113214 [PMID:33548636] |
ChEMBL | Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes incubated for 90 mins by radioligand competition assay | B | 5.65 | pKi | 2240 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
ChEMBL | Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in HEK293 cell membranes measured after 90 mins | B | 5.77 | pKi | 1700 | nM | Ki | J Med Chem (2017) 60: 681-694 [PMID:28055204] |
ChEMBL | Inhibition of human recombinant adenosine A1 receptor | B | 5.87 | pKi | 1350 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Inhibition of human adenosine A1 receptor | B | 5.87 | pKi | 1350 | nM | Ki | J Med Chem (2020) 63: 12196-12212 [PMID:32667814] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membranes measured after 90 mins | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2017) 60: 681-694 [PMID:28055204] |
ChEMBL | Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assay | B | 8.08 | pKi | 8.3 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
GtoPdb | - | - | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2014) 57: 3623-50 [PMID:24164628] |
ChEMBL | Inhibition of human recombinant adenosine receptor A2a | F | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Antagonist activity at human adenosine 2A receptor (409 to 412 residues) expressed in CHO cells using Ysi-poly-1-lysine as substrate incubated for 1 hr in presence of 3H-SCH-58261 by scintillation counting method | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2020) 63: 12196-12212 [PMID:32667814] |
ChEMBL | Displacement of [3H]-ZM241385 from recombinant human A2A receptor expressed in CHO-K1 cells incubated for 70 mins by liquid scintillation counting method | B | 8.41 | pKi | 3.9 | nM | Ki | Eur J Med Chem (2021) 214: 113214-113214 [PMID:33548636] |
ChEMBL | Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins | F | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2017) 60: 681-694 [PMID:28055204] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Displacement of [3H]-ZM241385 from A2A receptor in rat brain corpora striata incubated for 70 mins by liquid scintillation counting method | B | 7.73 | pKi | 18.7 | nM | Ki | Eur J Med Chem (2021) 214: 113214-113214 [PMID:33548636] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins | B | 5.3 | pKi | 5000 | nM | Ki | J Med Chem (2017) 60: 681-694 [PMID:28055204] |
ChEMBL | Inhibition of human recombinant adenosine receptor A2b | B | 6.15 | pKi | 700 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Inhibition of human adenosine 2B receptor | B | 6.15 | pKi | 700 | nM | Ki | J Med Chem (2020) 63: 12196-12212 [PMID:32667814] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Displacement of [3H]-HEMADO from human adenosine A3 receptor expressed in HEK293 cell membranes measured after 90 mins | B | 5.3 | pKi | 5000 | nM | Ki | J Med Chem (2017) 60: 681-694 [PMID:28055204] |
ChEMBL | Inhibition of human recombinant adenosine A3 receptor | B | 5.8 | pKi | 1570 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
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]