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

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ChEMBL ligand: CHEMBL477 (9-.beta.-d-ribofuranosyladenine, Adenocard, Adenocor, Adenoscan, Adenosine, NSC-7652, SR 96225, SR-96225)
  • 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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  • heat shock protein 90 beta family member 1/Endoplasmin in Human [ChEMBL: CHEMBL1075323] [GtoPdb: 2904] [UniProtKB: P14625]
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  • Equilibrative nucleoside transporter 1 in Human [ChEMBL: CHEMBL1997] [GtoPdb: 1117] [UniProtKB: Q99808]
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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]
ChEMBL Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay B 6.53 pKd 295.12 nM Kd J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay B 6.09 pKi 812.83 nM Ki J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
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 F 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 recombinant adenosine A1 receptor by cAMP assay F 6.51 pEC50 310 nM EC50 J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
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 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 transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine F 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-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay F 7.16 pEC50 69.18 nM EC50 J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
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 Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay B 5.71 pKd 1949.84 nM Kd J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
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]
ChEMBL Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay B 6.06 pKi 870.96 nM Ki J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
GtoPdb - - 7.14 pKi 73 nM Ki Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
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 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 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]
ChEMBL Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay B 7.76 pKd 17.3 nM Kd ACS Med Chem Lett (2022) 13: 1172-1181 [PMID:35859869]
ChEMBL Binding affinity to human recombinant adenosine receptor A2A expressed in CHO cells assessed as inhibitory constant by radioligand competition assay B 6.15 pKi 700 nM Ki Eur J Med Chem (2019) 179: 310-324 [PMID:31255928]
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 human wild type adenosine A2A receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assay B 6.82 pKi 150 nM Ki ACS Med Chem Lett (2022) 13: 1172-1181 [PMID:35859869]
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 F 6.14 pEC50 730 nM EC50 J Med Chem (2016) 59: 788-809 [PMID:26356532]
ChEMBL Agonist activity at human recombinant adenosine receptor A2a by cAMP assay F 6.15 pEC50 700 nM EC50 J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
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 adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay F 7.6 pEC50 25.12 nM EC50 J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
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 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 F 4.62 pEC50 24000 nM EC50 J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
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 A2B receptor (unknown origin) B 4.62 pEC50 24000 nM EC50 J Med Chem (2021) 64: 458-480 [PMID:33372800]
ChEMBL Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine F 4.63 pEC50 23500 nM EC50 J Med Chem (2016) 59: 788-809 [PMID:26356532]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay F 7.28 pEC50 52.48 nM EC50 J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
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]
ChEMBL Binding affinity to human wild type adenosine A3 receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay B 6.13 pKd 740 nM Kd ACS Med Chem Lett (2022) 13: 1172-1181 [PMID:35859869]
ChEMBL Binding affinity to human wild type adenosine A3 receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assay B 6.54 pKi 290 nM Ki ACS Med Chem Lett (2022) 13: 1172-1181 [PMID:35859869]
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 F 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 F 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 F 6.54 pEC50 290 nM EC50 J Med Chem (2016) 59: 788-809 [PMID:26356532]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay F 7.87 pEC50 13.49 nM EC50 J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
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: P00515, P00517, P05131, P31322]
ChEMBL Inhibitory constant for Protein Kinase A B 4.82 pKi 15000 nM Ki Bioorg Med Chem Lett (1996) 6: 899-902
heat shock protein 90 beta family member 1/Endoplasmin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075323] [GtoPdb: 2904] [UniProtKB: P14625]
ChEMBL Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay B 4.3 pKd >50000 nM Kd ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064]
ChEMBL Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay B 5 pKi >10000 nM Ki ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064]
Equilibrative nucleoside transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1997] [GtoPdb: 1117] [UniProtKB: Q99808]
ChEMBL Inhibition of the equilibrative nucleoside transporter (ENT1, SLC29A1) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay (PubChem AID: 1745861) F 4.2 pEC50 63000 nM EC50 Sci Rep (2019) 9: 13802-null [PMID:31551431]
Glyceraldehyde-3-phosphate dehydrogenase liver in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2284] [UniProtKB: P04406]
ChEMBL Inhibition of glyceraldehyde-3-phosphate dehydrogenase in Trypanosoma brucei B 1 pIC50 100000000 nM IC50 J Med Chem (1995) 38: 3838-3849 [PMID:7562915]
ChEMBL Inhibitory activity measured for Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) in Leishmania. mexicana B 1.3 pIC50 50000000 nM IC50 J Med Chem (1998) 41: 4790-4799 [PMID:9822549]
ChEMBL TInhibition of glyceraldehyde-3-phosphate dehydrogenase in Leishmania mexicana B 1.3 pIC50 50000000 nM IC50 J Med Chem (1995) 38: 3838-3849 [PMID:7562915]
ChEMBL Inhibition of Glyceraldehyde-3-phosphate dehydrogenase in human erythrocytes. B 1.46 pIC50 35000000 nM IC50 J Med Chem (1995) 38: 3838-3849 [PMID:7562915]
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 34:

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]