tozadenant [Ligand Id: 5611] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2105747 (RO-4494351, Tozadenant, RO4494351-000, A-2A (3), SYN-115, RO4494351, A2A-(3), RO-4494351-002, A2A (3), SYN115, RO4494351-002, RO-4494351000, RO-4494351-000)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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]
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]
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 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 B 9.52 pKi 0.3 nM Ki J Med Chem (2017) 60: 681-694 [PMID:28055204]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]