PSB1115 [Ligand Id: 3286] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8565 (PSB-1115)
  • 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 Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
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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. (2002) 45: 1500-10 [PMID:11906291]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells B 5 pKi >10000 nM Ki J. Med. Chem. (2006) 49: 4384-4391 [PMID:16821798]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity at Adenosine A1 receptor in rat brain cortical membrane using [3H]N6-R-phenylisopropyladenosine (R-PIA) as radioligand B 5.66 pKi 2200 nM Ki J. Med. Chem. (1993) 36: 3341-3349 [PMID:8230124]
ChEMBL Displacement of [3H]R-PIA from adenosine A1 receptor in rat brain cortical membranes B 5.66 pKi 2200 nM Ki J. Med. Chem. (2006) 49: 4384-4391 [PMID:16821798]
GtoPdb - - 5.66 pKi 2200 nM Ki J. Med. Chem. (1993) 36: 3341-9 [PMID:8230124]
ChEMBL Displacement of [3H]-CCPA from adenosine A1 receptor of rat brain cortical membrane preparations B 5.91 pKi 1238 nM Ki J. Med. Chem. (2004) 47: 1031-1043 [PMID:14761205]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement of [3H]R-PIA from adenosine A2A receptor in rat brain striatal membranes B 4.62 pKi 24000 nM Ki J. Med. Chem. (2006) 49: 4384-4391 [PMID:16821798]
GtoPdb - - 4.62 pKi 24000 nM Ki J. Med. Chem. (1993) 36: 3341-9 [PMID:8230124]
ChEMBL Displacement of [3H]MSX-2 from adenosine A2A receptor of rat brain striatal membranes B 4.93 pKi 11800 nM Ki J. Med. Chem. (2004) 47: 1031-1043 [PMID:14761205]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 7.27 pKi 53.4 nM Ki J. Med. Chem. (2002) 45: 1500-10 [PMID:11906291]
ChEMBL Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in CHO cells B 7.27 pKi 53.4 nM Ki J. Med. Chem. (2006) 49: 4384-4391 [PMID:16821798]
ChEMBL Displacement of [3H]ZM241385 from human recombinant Adenosine A2B receptor B 7.27 pKi 53.4 nM Ki J. Med. Chem. (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL Displacement of [3H]ZM241385 from human recombinant adenosine A2B receptor B 7.27 pKi 53.4 nM Ki J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
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. (2002) 45: 1500-10 [PMID:11906291]
ChEMBL Displacement of [3H]PSB11 from human recombinant adenosine A3 receptor expressed in CHO cells B 5 pKi >10000 nM Ki J. Med. Chem. (2006) 49: 4384-4391 [PMID:16821798]

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]