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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]