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

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ChEMBL ligand: CHEMBL2163568 (GR-79236)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor in Rat [GtoPdb: 18] [UniProtKB: P25099]
1 CHEMBL2163568_lig_chart_1 Adenosine A1 receptor HumanRat
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
2 CHEMBL2163568_lig_chart_2 Adenosine A2a receptor Human
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • This target only has 1 pki data point
3 CHEMBL2163568_lig_chart_3 Adenosine A2b receptor Human
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • This target only has 1 pki data point
4 CHEMBL2163568_lig_chart_4 Adenosine A3 receptor Human
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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 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 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 in Rat [GtoPdb: 18] [UniProtKB: P25099]
GtoPdb - - 8.51 pKi 3.1 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
A2A receptor/Adenosine A2a receptor 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 A2b receptor 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 A3 receptor 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 27:

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]