TCPA [Ligand Id: 5590] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2113457
  • 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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  • A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275]
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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 - - 8.55 pKi 2.8 nM Ki J Med Chem (2003) 46: 1492-503 [PMID:12672250]
ChEMBL In vitro binding affinity towards human adenosine A1 receptor by [3H]DPCPX displacement. B 8.55 pKi 2.8 nM Ki J. Med. Chem. (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL Inhibition of cAMP formation in CHO cells expressing human adenosine A1 receptor B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2003) 46: 1492-1503 [PMID:12672250]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Tested for binding affinity towards human adenosine A2A receptor using [3H]ZM-241385 as radioligand B 6.68 pKi 210 nM Ki J. Med. Chem. (2003) 46: 1492-1503 [PMID:12672250]
GtoPdb - - 6.68 pKi 210 nM Ki J Med Chem (2003) 46: 1492-503 [PMID:12672250]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 6.22 pKi 600 nM Ki J Med Chem (2003) 46: 1492-503 [PMID:12672250]
ChEMBL Inhibition of [125 I]-IABMECA binding to human adenosine A3 receptor B 6.22 pKi 600 nM Ki J. Med. Chem. (2003) 46: 1492-1503 [PMID:12672250]
A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 5 pKi >10000 nM Ki Br J Pharmacol (1997) 122: 867-74 [PMID:9384502]

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]