GR79236 [Ligand Id: 3288] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2163568
  • A1 receptor/Adenosine receptor A1 in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine receptor A1 in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine receptor A2a in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A2B receptor/Adenosine receptor A2b in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
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  • A3 receptor/Adenosine receptor A3 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 receptor A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Agonist activity at Homo sapiens (human) adenosine A1 receptor expressed in CHO cells B 7.8 pKi 15.85 nM Ki Med Chem Res (2004) 13: 88-98
ChEMBL Displacement of [3H]DPCPX from recombinant human A1 receptor expressed in CHO cell membranes B 8.41 pKi 3.89 nM Ki Medchemcomm (2018) 9: 1920-1932 [PMID:30568760]
ChEMBL Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay F 8.23 pEC50 5.9 nM EC50 J Med Chem (2012) 55: 6467-6477 [PMID:22738238]
A1 receptor/Adenosine receptor A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H]DPCPX from rat A1 receptor B 8.51 pKi 3.1 nM Ki Medchemcomm (2018) 9: 1920-1932 [PMID:30568760]
GtoPdb - - 8.51 pKi 3.1 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
A2A receptor/Adenosine receptor A2a in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells F 4.6 pKi 25118.86 nM Ki Med Chem Res (2004) 13: 88-98
GtoPdb - - 5.89 pKi 1300 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
A2B receptor/Adenosine receptor A2b in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells B 4.5 pKi 31622.78 nM Ki Med Chem Res (2004) 13: 88-98
A3 receptor/Adenosine receptor A3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells B 5.6 pKi 2511.89 nM Ki Med Chem Res (2004) 13: 88-98

ChEMBL data shown on this page come from version 36:

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]