MRS1706 [Ligand Id: 3287] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL17002
  • 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]
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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 recombinant human adenosine A1 receptor expressed in HEK293 cells in presence of [125I]IABA radioligand. F 6.8 pKi 157 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Antagonist activity against human adenosine A1 receptor F 6.8 pKi 157 nM Ki Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Antagonist activity against adenosine A1 receptor in rat brain membrane in presence of [3H]R-PIA radioligand. F 7.42 pKi 37.6 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand. F 6.95 pKi 112 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Antagonist activity against human adenosine A2A receptor F 6.95 pKi 112 nM Ki Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand. F 6.26 pKi 548 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX F 8.86 pKi 1.39 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Antagonist activity against human adenosine A2B receptor F 8.86 pKi 1.39 nM Ki Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Antagonist activity against human adenosine A3 receptor expressed in HEK cells in presence of [125]IAB-MECA or [125I]IABA radioligand. F 6.64 pKi 230 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Antagonist activity against human adenosine A3 receptor F 6.64 pKi 230 nM Ki Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438]

ChEMBL data shown on this page come from version 28:

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]