PSB603 [Ligand Id: 3284] 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]
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]
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]
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]
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]
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 Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay F 8.89 pKi 1.3 nM Ki J Med Chem (2021) 64: 8161-8178 [PMID:34120444]
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 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]