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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL315984
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
There should be some charts here, you may need to enable JavaScript!
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]