KF26777 [Ligand Id: 5618] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2181965
  • 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 - - 5.74 pKi 1800 nM Ki Eur J Pharmacol (2002) 444: 133-41 [PMID:12063073]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter B 5.74 pKi 1800 nM Ki J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter B 6.33 pKi 470 nM Ki J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
GtoPdb - - 6.33 pKi 470 nM Ki Eur J Pharmacol (2002) 444: 133-41 [PMID:12063073]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter B 9.7 pKi 0.2 nM Ki J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
GtoPdb - - 9.7 pKi 0.2 nM Ki Eur J Pharmacol (2002) 444: 133-41 [PMID:12063073]
ChEMBL Antagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assay F 6.57 pIC50 270 nM IC50 J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 6.21 pKi 620 nM Ki Eur J Pharmacol (2002) 444: 133-41 [PMID:12063073]

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]