[3H]OSIP339391 [Ligand Id: 454] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL485862 (OSIP-339391)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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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]
ChEMBL Antagonist activity against human adenosine A1 receptor F 6.35 pKi 450 nM Ki Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL Binding affinity to human adenosine A1 receptor B 7.43 pKi 37 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Binding affinity to human adenosine A1 receptor B 7.43 pKi 37 nM Ki J. Med. Chem. (2012) 55: 797-811 [PMID:22148859]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding affinity to human adenosine A2A receptor B 6.48 pKi 328 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Antagonist activity against human adenosine A2A receptor F 6.48 pKi 328 nM Ki Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL Binding affinity to human adenosine A2A receptor B 6.48 pKi 328 nM Ki J. Med. Chem. (2012) 55: 797-811 [PMID:22148859]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 9.8 pKd - - - Biochem Pharmacol (2004) 68: 305-12 [PMID:15194002]
ChEMBL Antagonist activity against human adenosine A2B receptor F 9.3 pKi 0.5 nM Ki Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes B 9.3 pKi 0.5 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Antagonist activity at human A2B receptor B 9.3 pKi 0.5 nM Ki J Med Chem (2021) 64: 458-480 [PMID:33372800]
ChEMBL Binding affinity to human adenosine A2B receptor B 9.39 pKi 0.41 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Binding affinity to human adenosine A2B receptor B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2012) 55: 797-811 [PMID:22148859]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity to human adenosine A3 receptor B 6.35 pKi 450 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Antagonist activity against human adenosine A3 receptor F 6.35 pKi 450 nM Ki Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL Binding affinity to human adenosine A3 receptor B 6.35 pKi 450 nM Ki J. Med. Chem. (2012) 55: 797-811 [PMID:22148859]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]