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/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
Created with Highcharts 10.3.3ValuesChart context menuAdenosine A1 receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
Created with Highcharts 10.3.3ValuesChart context menuAdenosine A2a receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
Created with Highcharts 10.3.3ValuesChart context menuAdenosine A2b receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
Created with Highcharts 10.3.3ValuesChart context menuAdenosine A3 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
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 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 A1 receptor 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 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 35:

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]