PSB36 [Ligand Id: 3285] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1316674
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor in Rat [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor in Rat [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275]
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  • A3 receptor in Human [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor in Rat [GtoPdb: 21] [UniProtKB: P28647]
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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]
ChEMBL The A1-StaR receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. B 9.19 pKd 0.64 nM Kd K4DD drug target binding kinetics data
A1 receptor in Rat [GtoPdb: 18] [UniProtKB: P25099]
GtoPdb - - 9.9 pKi 0.12 nM Ki J. Pharmacol. Exp. Ther. (2004) 308: 358-66 [PMID:14563788]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction. B 8.61 pKd 2.45 nM Kd K4DD drug target binding kinetics data
GtoPdb - - 6.01 pKi 980 nM Ki ChemMedChem (2006) 1: 891-902 [PMID:16902942]
A2A receptor in Rat [GtoPdb: 19] [UniProtKB: P30543]
GtoPdb - - 6.26 pKi 552 nM Ki ChemMedChem (2006) 1: 891-902 [PMID:16902942]
A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 6.73 pKi 187 nM Ki Bioorg. Med. Chem. (2006) 14: 3654-61 [PMID:16458010]
A3 receptor in Human [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 5.64 pKi 2300 nM Ki ChemMedChem (2006) 1: 891-902 [PMID:16902942]
A3 receptor in Rat [GtoPdb: 21] [UniProtKB: P28647]
GtoPdb - - 5.19 pKi 6500 nM Ki ChemMedChem (2006) 1: 891-902 [PMID:16902942]

ChEMBL data shown on this page come from version 27:

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]