MRS1097 [Ligand Id: 467] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL315984
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of specific [3H](R)-PIA binding at adenosine A1 receptor from rat brain membranes. B 5.23 pKi 5930 nM Ki J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL Binding affinity against adenosine A1 receptor in rat cerebral cortex membrane by radioligand binding assay using [3H](R)-PIA. B 5.23 pKi 5930 nM Ki J Med Chem (1996) 39: 4667-4675 [PMID:8917655]
ChEMBL Displacement of [3H]-R-PIA from adenosine A1 receptor of rat brain membrane B 5.23 pKi 5930 nM Ki J Med Chem (1999) 42: 3055-3065 [PMID:10447949]
ChEMBL Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes B 5.23 pKi 5930 nM Ki J Med Chem (1996) 39: 2980-2989 [PMID:8709132]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement of specific [3H]-CGS- 21680 binding at Adenosine A2A receptor in rat striatal membranes. B 5.32 pKi 4770 nM Ki J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor of rat striatal membrane B 5.32 pKi 4770 nM Ki J Med Chem (1996) 39: 4667-4675 [PMID:8917655]
ChEMBL Displacement of [3H]CGS-21680 from Adenosine A2A receptor of rat striatal membrane at 10e-4 uM B 5.32 pKi 4770 nM Ki J Med Chem (1999) 42: 3055-3065 [PMID:10447949]
ChEMBL Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes B 5.32 pKi 4770 nM Ki J Med Chem (1996) 39: 2980-2989 [PMID:8709132]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [125 I]AB-MECA from Adenosine A3 receptor expressed in HEK cells B 6.96 pKi 110 nM Ki J Med Chem (1999) 42: 3055-3065 [PMID:10447949]
ChEMBL Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor. B 6.97 pKi 108 nM Ki J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL Inhibition of [125I]- AB-MECA binding to human Adenosine A3 receptors expressed in HEK cells B 6.97 pKi 108 nM Ki J Med Chem (1996) 39: 4667-4675 [PMID:8917655]
ChEMBL Displacement of [125]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells B 6.97 pKi 108 nM Ki J Med Chem (1996) 39: 2980-2989 [PMID:8709132]
GtoPdb - - 7 pKi - - - Neuropharmacology (1997) 36: 1157-65 [PMID:9364471];
J Med Chem (1996) 39: 2980-9 [PMID:8709132]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Binding affinity against rat Adenosine A3 receptor from CHO cells B 5.38 pKi 4160 nM Ki J Med Chem (1996) 39: 2980-2989 [PMID:8709132]

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]