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]
ChEMBL Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay B 8.86 pKi 1.39 nM Ki J Med Chem (2021) 64: 7156-7178 [PMID:34019396]
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 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]