PSB603 [Ligand Id: 3284] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL483688
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • A2B receptor/Adenosine A2b receptor in Mouse [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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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 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
GtoPdb - - 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]CCPA from rat brain cortex adenosine A1 receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
GtoPdb - - 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]MSX-2 from rat brain striatum adenosine A2A receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment B 9.19 pKd 0.65 nM Kd J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
GtoPdb - - 9.39 pKd 0.4 nM Kd J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment B 9.39 pKd 0.4 nM Kd J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells B 9.26 pKi 0.55 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
GtoPdb - - 9.26 pKi 0.55 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method F 7.74 pIC50 18.3 nM IC50 J Med Chem (2018) 61: 4301-4316 [PMID:29681156]
ChEMBL Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2 F 8.95 pIC50 1.13 nM IC50 J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method B 9.13 pIC50 0.74 nM IC50 J Med Chem (2018) 61: 4301-4316 [PMID:29681156]
ChEMBL Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method B 9.27 pIC50 0.53 nM IC50 J Med Chem (2018) 61: 4301-4316 [PMID:29681156]
A2B receptor/Adenosine A2b receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614]
GtoPdb - - 9.45 pKd 0.35 nM Kd J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells B 9.45 pKd 0.35 nM Kd J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]PSB-11 from recombinant human adenosine A3 receptor expressed in CHO cell membranes after 180 mins by liquid scintillation counting method B 5 pKi >10000 nM Ki J Med Chem (2018) 61: 4301-4316 [PMID:29681156]

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]