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]
ChEMBL Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane assessed as inhibition constant incubated for 30 mins by competitive binding assay B 8.46 pKi 3.49 nM Ki J Med Chem (2023) 66: 890-912 [PMID:36517209]
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 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]