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 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]