ISAM-140 [Ligand Id: 11223] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3787197
  • 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 Displacement of [3H]DPCPX from human recombinant A1 receptor expressed in CHOA1 cell membranes incubated for 60 mins by radioligand binding competition assay B 7.7 pKi 20 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]ZM241385 from human recombinant A2A receptor expressed in human HeLa cell membranes incubated for 30 mins by radioligand binding competition assay B 7.55 pKi 28 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins B 8.46 pKi 3.49 nM Ki J. Med. Chem. (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay B 8.46 pKi 3.49 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method B 8.46 pKi 3.49 nM Ki J Med Chem (2020) 63: 7721-7739 [PMID:32573250]
ChEMBL Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method B 8.46 pKi 3.49 nM Ki J Med Chem (2021) 64: 458-480 [PMID:33372800]
GtoPdb - - 8.46 pKi 3.49 nM Ki J Med Chem (2016) 59: 1967-83 [PMID:26824742]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [3H]NECA from human A3 receptor expressed in human HeLa cell membranes incubated for 180 mins by radioligand binding competition assay B 8.7 pKi 2 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]

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, 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]