MRS928 [Ligand Id: 402] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL75772 (3,5,7-Trimethoxyflavone)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
  • 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]
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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 Binding affinity at Adenosine A1 receptor in rat brain membranes by [3H]PIA displacement. B 6.29 pKi 509 nM Ki J. Med. Chem. (1996) 39: 2293-2301 [PMID:8691424]
ChEMBL Displacement of specific [3H]PIA binding from adenosine A1 receptor in rat brain membranes. B 6.29 pKi 509 nM Ki J. Med. Chem. (1996) 39: 781-788 [PMID:8576921]
GtoPdb - - 6.3 pKi - - - J. Med. Chem. (1996) 39: 2293-301 [PMID:8691424]
A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 5.2 pKi - - - J. Med. Chem. (1996) 39: 2293-301 [PMID:8691424]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Affinity at Adenosine A2A receptor in rat striatal membranes by [3H]- CGS 21680 displacement. B 5.19 pKi 6450 nM Ki J. Med. Chem. (1996) 39: 781-788 [PMID:8576921]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 5.9 pKi - - - J. Med. Chem. (1996) 39: 2293-301 [PMID:8691424]
ChEMBL Binding affinity against human adenosine A3 receptor in HEK293 cells using [125I]AB-MECA 21680 radioligand. B 5.92 pKi 1210 nM Ki J. Med. Chem. (1996) 39: 2293-2301 [PMID:8691424]
ChEMBL Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells B 5.92 pKi 1210 nM Ki J. Med. Chem. (1996) 39: 781-788 [PMID:8576921]

ChEMBL data shown on this page come from version 26:

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]