apadenoson [Ligand Id: 3290] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1950649 (BMS-068645, Apadenoson, Stedivaze)
  • 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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  • 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]
GtoPdb - - 7.11 pKi 77 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Binding affinity to human recombinant adenosine A1 receptor B 7.11 pKi 77 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]
GtoPdb - - 9.3 pKi 0.5 nM Ki Am. J. Physiol. Heart Circ. Physiol. (2001) 281: H67-74 [PMID:11406470]
ChEMBL Binding affinity to A2A adenosine receptor B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2012) 55: 538-552 [PMID:22104008]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor B 9.3 pKi 0.5 nM Ki ACS Med. Chem. Lett. (2011) 2: 890-895 [PMID:24900277]
ChEMBL Binding affinity to human recombinant adenosine receptor A2a B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Binding affinity to human adenosine A2A receptor B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 3253-3267 [PMID:25780876]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity to human recombinant adenosine A3 receptor B 7.35 pKi 45 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb - - 7.35 pKi 45 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]