[3H]PSB603 [Ligand Id: 5728] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
1 CHEMBL483688_lig_chart_1 Adenosine A1 receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • 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]
2 CHEMBL483688_lig_chart_2 Adenosine A2a receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • 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]
  • This target only has 1 pki data point
3 CHEMBL483688_lig_chart_3 Adenosine A2b receptor HumanMouse
There should be some charts here, you may need to enable JavaScript!
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
4 CHEMBL483688_lig_chart_4 Adenosine A3 receptor Human
There should be some charts here, you may need to enable JavaScript!
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 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]
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]
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]
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]
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]
GtoPdb - - 9.4 pKd - - - 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]
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]
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]
GtoPdb - - 9.5 pKd - - - 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]
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]