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

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ChEMBL ligand: CHEMBL1950649 (Apadenoson, Bms-068645, BMS-068645, BMS068645, DWH-146E, 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]