adenosine [Ligand Id: 2844] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL477 (SR-96225, Adenoscan, NSC-7652, Adenosine, Adenocard, Adenocor)
  • 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]
  • Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • A2B receptor in Rat [GtoPdb: 20] [UniProtKB: P29276]
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  • 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]
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  • Adenosine kinase in Toxoplasma gondii [ChEMBL: CHEMBL2982] [UniProtKB: Q9TVW2]
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  • Glyceraldehyde-3-phosphate dehydrogenase liver in Human [ChEMBL: CHEMBL2284] [UniProtKB: P04406]
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  • DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3]
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  • inosine monophosphate dehydrogenase 1/Inosine-5'-monophosphate dehydrogenase 1 in Human [ChEMBL: CHEMBL1822] [GtoPdb: 2624] [UniProtKB: P20839]
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  • inosine monophosphate dehydrogenase 2/Inosine-5'-monophosphate dehydrogenase 2 in Human [ChEMBL: CHEMBL2002] [GtoPdb: 2625] [UniProtKB: P12268]
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  • mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318]
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  • TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
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  • phosphatidylinositol 4-kinase type 2 alpha in Human [GtoPdb: 2498] [UniProtKB: Q9BTU6]
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  • phosphatidylinositol 4-kinase type 2 beta in Human [GtoPdb: 2499] [UniProtKB: Q8TCG2]
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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]
GtoPdb - - 7 pKi ~100 nM Ki Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
ChEMBL Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis B 8.63 pIC50 2.34 nM IC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at human Adenosine A1 receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphai1 after 16 hrs by beta galactosidase reporter gene assay B 5.6 pEC50 2511.89 nM EC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at human A1AR assessed as induction of Ca2+ ion mobilization by orthogonal functional assay F 5.85 pEC50 1410 nM EC50 J. Med. Chem. (2012) 55: 6467-6477 [PMID:22738238]
ChEMBL Agonist activity at human adenosine A1 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine B 6.51 pEC50 310 nM EC50 J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Agonist activity at human adenosine A1 receptor expressed in CHO cells F 6.51 pEC50 310 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1933-1936 [PMID:21388809]
ChEMBL Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as increase of intracellular calcium level F 6.51 pEC50 310 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 4140-4146 [PMID:20541935]
ChEMBL Agonist activity at human recombinant adenosine A1 receptor by cAMP assay B 6.51 pEC50 310 nM EC50 J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of isoproterenol-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay F 7.41 pEC50 39 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 Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. B 4.54 pKi 29000 nM Ki J. Med. Chem. (1995) 38: 1174-1188 [PMID:7707320]
GtoPdb - - 7.14 pKi 73 nM Ki Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
ChEMBL Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. B 7.89 pKi 12.8 nM Ki J. Med. Chem. (1989) 32: 1667-1673 [PMID:2754691]
ChEMBL Affinity for Adenosine A1 receptor determined by [3H]N6-cyclohexyladenosine binding to rat brain membranes B 7.89 pKi 12.8 nM Ki Bioorg. Med. Chem. Lett. (1991) 1: 481-486
ChEMBL Displacement of [3H]R-PIA from rat brain membrane Adenosine A1 receptor B 8 pKi 10 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Evaluated for the binding affinity towards the Adenosine A1 receptor in corpora striata of rats using [3H]CHA as radioligand. B 8 pKi 10 nM Ki J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor B 8.29 pKi 5.1 nM Ki J. Med. Chem. (1990) 33: 3127-3130 [PMID:2258897]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Effective concentration required for prolongation of the stimulus-QRS interval by 50% of the maximum response at the A1 adenosine receptor in langendorff guinea pig heart preparation F 5.47 pEC50 3388.44 nM EC50 J. Med. Chem. (1991) 34: 1340-1344 [PMID:2016708]
ChEMBL Prolongation of the stimulus-QRS interval by 50% of the maximum response at the adenosine A1 receptor in langendorff guinea pig heart preparation F 5.47 pEC50 3388.44 nM EC50 J. Med. Chem. (1991) 34: 1334-1339 [PMID:2016707]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 6.51 pKi 310 nM Ki Annu. Rev. Pharmacol. Toxicol. (2005) 45: 385-412 [PMID:15822182];
Pharmacol. Toxicol. (1995) 76: 93-101 [PMID:7746802];
Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
ChEMBL Binding affinity to A2A adenosine receptor B 7.7 pKi 20 nM Ki J. Med. Chem. (2012) 55: 538-552 [PMID:22104008]
ChEMBL Effective concentration required for cyclic AMP dependent inhibition of blood platelet aggregation for A2 receptor stimulation B 4.4 pEC50 40000 nM EC50 J. Med. Chem. (1993) 36: 4113-4120 [PMID:8258836]
ChEMBL Agonist activity at human Adenosine A2A receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay B 5.24 pEC50 5754.4 nM EC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine B 6.14 pEC50 730 nM EC50 J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium level F 6.15 pEC50 700 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 4140-4146 [PMID:20541935]
ChEMBL Agonist activity at human adenosine A2A receptor expressed in CHO cells F 6.15 pEC50 700 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1933-1936 [PMID:21388809]
ChEMBL Agonist activity at human recombinant adenosine receptor A2a by cAMP assay B 6.15 pEC50 700 nM EC50 J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
GtoPdb - - 6.82 pKi 150 nM Ki Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
ChEMBL Displacement of specific [3H]-CGS- 21680 binding to adenosine A2A receptor in rat striatal membranes B 7.52 pKi 30 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 4.82 pKi 15000 nM Ki Annu. Rev. Pharmacol. Toxicol. (2005) 45: 385-412 [PMID:15822182];
Pharmacol. Toxicol. (1995) 76: 93-101 [PMID:7746802];
Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
ChEMBL Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay B 4.29 pEC50 51286.14 nM EC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level F 4.62 pEC50 24000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 4140-4146 [PMID:20541935]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells F 4.62 pEC50 24000 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1933-1936 [PMID:21388809]
ChEMBL Agonist activity at human recombinant adenosine receptor A2b by cAMP assay B 4.62 pEC50 24000 nM EC50 J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine B 4.63 pEC50 23500 nM EC50 J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
A2B receptor in Rat [GtoPdb: 20] [UniProtKB: P29276]
GtoPdb - - 5.29 pKi 5100 nM Ki Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 6.54 pKi 290 nM Ki Annu. Rev. Pharmacol. Toxicol. (2005) 45: 385-412 [PMID:15822182];
Pharmacol. Toxicol. (1995) 76: 93-101 [PMID:7746802];
Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
ChEMBL Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis B 8.94 pIC50 1.15 nM IC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
ChEMBL Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay F 5.98 pEC50 1040 nM EC50 J. Med. Chem. (2006) 49: 2689-2702 [PMID:16640329]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level F 6.54 pEC50 290 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 4140-4146 [PMID:20541935]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in CHO cells F 6.54 pEC50 290 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1933-1936 [PMID:21388809]
ChEMBL Agonist activity at human recombinant adenosine A3 receptor by cAMP assay B 6.54 pEC50 290 nM EC50 J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine B 6.54 pEC50 290 nM EC50 J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
GtoPdb - - 5.19 pKi 6500 nM Ki Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
ChEMBL Displacement of [125I]- AB-MECA from rat adenosine A3 receptor expressed in CHO cells B 7 pKi 100 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
Adenosine kinase in Toxoplasma gondii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2982] [UniProtKB: Q9TVW2]
ChEMBL Binding affinity to purified Toxoplasma gondii adenosine kinase B 5.05 pKi 8900 nM Ki J. Med. Chem. (2008) 51: 3934-3945 [PMID:18563892]
cAMP-dependent protein kinase A in Bovine (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2111446] [UniProtKB: P00515P00517P05131P31322]
ChEMBL Inhibitory constant for Protein Kinase A B 4.82 pKi 15000 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 899-902
Glyceraldehyde-3-phosphate dehydrogenase liver in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2284] [UniProtKB: P04406]
ChEMBL Tested for the inhibitory activity against Glycosomal glyceraldehyde 3-phosphate dehydrogenase (gGAPDH) of Trypanosoma brucei B 4 pIC50 100000 nM IC50 J. Med. Chem. (1994) 37: 3605-3613 [PMID:7932587]
ChEMBL Tested for the inhibitory activity against Glycosomal glyceraldehyde 3-phosphate dehydrogenase (gGAPDH) of Leishmania mexicana B 4.3 pIC50 50000 nM IC50 J. Med. Chem. (1994) 37: 3605-3613 [PMID:7932587]
ChEMBL Tested for the inhibitory activity against Glycosomal glyceraldehyde 3-phosphate dehydrogenase (gGAPDH) of human erythrocyte B 4.46 pIC50 35000 nM IC50 J. Med. Chem. (1994) 37: 3605-3613 [PMID:7932587]
DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3]
ChEMBL Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate addition in presence of [3H-Me]SAM by scintillation proximity assay B 4 pIC50 100000 nM IC50 ACS Med Chem Lett (2017) 8: 338-343 [PMID:28337327]
inosine monophosphate dehydrogenase 1/Inosine-5'-monophosphate dehydrogenase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1822] [GtoPdb: 2624] [UniProtKB: P20839]
ChEMBL Inhibition of human IMP dehydrogenase 1 B 4 pKi >100000 nM Ki Bioorg. Med. Chem. (2008) 16: 7462-7469 [PMID:18583139]
inosine monophosphate dehydrogenase 2/Inosine-5'-monophosphate dehydrogenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2002] [GtoPdb: 2625] [UniProtKB: P12268]
ChEMBL Inhibition of human IMP dehydrogenase 2 B 4 pKi >100000 nM Ki Bioorg. Med. Chem. (2008) 16: 7462-7469 [PMID:18583139]
mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318]
ChEMBL Binding affinity to recombinant human biotinylated N-terminal GST-tagged non-autophosphorylated TAK1 (1 to 303 residues) fused with TAB1 (437 to 504 residues) expressed in baculovirus infected sf9 cells by SPR assay B 4.47 pKd 34000 nM Kd Bioorg Med Chem Lett (2017) 27: 1031-1036 [PMID:28109791]
ChEMBL Binding affinity to recombinant human biotinylated N-terminal GST-tagged autophosphorylated TAK1 (1 to 303 residues) fused with TAB1 (437 to 504 residues) expressed in baculovirus infected sf9 cells by SPR assay B 5.36 pKd 4400 nM Kd Bioorg Med Chem Lett (2017) 27: 1031-1036 [PMID:28109791]
TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
GtoPdb - - 3.2 pIC50 630000 nM IC50
phosphatidylinositol 4-kinase type 2 alpha in Human [GtoPdb: 2498] [UniProtKB: Q9BTU6]
GtoPdb - - 5 pIC50 - - - Anal. Biochem. (2011) 417: 97-102 [PMID:21704602]
phosphatidylinositol 4-kinase type 2 beta in Human [GtoPdb: 2499] [UniProtKB: Q8TCG2]
GtoPdb - - 5 pIC50 - - - Anal. Biochem. (2011) 417: 97-102 [PMID:21704602]

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]