binodenoson [Ligand Id: 5595] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1950554 (Binodenoson, Corvue, MRE0470, MRE-0470, Wrc0470)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
  • Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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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]CCPA from human recombinant adenosine A1 receptor B 4.32 pKi 48000 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Binding affinity to human recombinant adenosine A1 receptor B 4.32 pKi 48000 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb - - 4.32 pKi 48000 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells 90 mins by liquid scintillation counting analysis B 6.77 pKi 169 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by liquid scintillation counting analysis B 7.15 pKi 70.8 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL In vitro prolonging of the stimulus-QRS interval in guinea pig heart. B 5.45 pEC50 3548.13 nM EC50 J. Med. Chem. (1992) 35: 4557-4561 [PMID:1469687]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding affinity to A2A adenosine receptor B 6.57 pKi 270 nM Ki J. Med. Chem. (2012) 55: 538-552 [PMID:22104008]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells B 6.57 pKi 270 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Binding affinity to human recombinant adenosine receptor A2a B 6.57 pKi 270 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Binding affinity to human adenosine A2A receptor B 6.57 pKi 270 nM Ki J. Med. Chem. (2015) 58: 3253-3267 [PMID:25780876]
GtoPdb - - 6.57 pKi 270 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells after 60 mins by liquid scintillation counting B 7.09 pKi 81 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis B 7.59 pKi 25.5 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 3.37 pKi 430000 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis B 5 pKi >10000 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Agonist activity at human recombinant adenosine receptor A2b by cAMP assay F 4 pEC50 >100000 nM EC50 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]
GtoPdb - - 6.04 pKi 903 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A3 receptor B 6.04 pKi 903 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Binding affinity to human recombinant adenosine A3 receptor B 6.04 pKi 903 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells after 180 mins by liquid scintillation counting analysis B 7.28 pKi 52.6 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]

ChEMBL data shown on this page come from version 31:

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]