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]
ChEMBL Antagonist activity at adenosine A2A receptor (unknown origin) F 9.26 pKi 0.55 nM Ki Eur J Med Chem (2022) 227: 113907-113907 [PMID:34695776]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]