Target Validation Information
Target ID T03661
Target Name Adenosine deaminase
Target Type
Successful
Drug Potency against Target Pentostatin Drug Info Ki = 0.2 nM [552627]
3-(6-Amino-purin-9-yl)-4-p-tolyl-butan-2-ol Drug Info Ki = 302 nM [525926]
3-(6-Amino-purin-9-yl)-4-phenethyloxy-butan-2-ol Drug Info Ki = 93.1 nM [525926]
3-(6-Amino-purin-9-yl)-6-o-tolyl-hexan-2-ol Drug Info Ki = 0.51 nM [525926]
3-(6-Amino-purin-9-yl)-non-5-yn-2-ol Drug Info Ki = 188 nM [525926]
3-(6-Amino-purin-9-yl)-8-phenyl-octan-2-ol Drug Info Ki = 0.95 nM [525926]
3-(6-Amino-purin-9-yl)-6-phenyl-hexan-2-ol Drug Info Ki = 0.89 nM [525926]
3-(6-Amino-purin-9-yl)-7-phenyl-heptan-2-ol Drug Info Ki = 0.76 nM [525926]
3-(6-Amino-purin-9-yl)-non-5-en-2-ol Drug Info Ki = 3.74 nM [525926]
3-(6-Amino-purin-9-yl)-4-butoxy-butan-2-ol Drug Info Ki = 123.4 nM [525926]
3-(6-Amino-purin-9-yl)-5-m-tolyl-pentan-2-ol Drug Info Ki = 1.02 nM [525926]
Dipyridamole Drug Info IC50 = 64 nM [553230]
Action against Disease Model Cladribine IC50 on h uMan promyelocytic leukemia cell line HL60: 8.7nM [553286] Drug Info
References
Ref 552627Recent progress in the development of adenosine receptor ligands as antiinflammatory drugs. Curr Top Med Chem. 2006;6(13):1375-99.
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 525926J Med Chem. 2000 Nov 30;43(24):4694-700.Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Ref 553286Lack of cross-resistance with gemcitabine and cytarabine in cladribine-resistant HL60 cells with elevated 5'-nucleotidase activity. Exp Hematol. 1998 Dec;26(13):1223-8.
Ref 553230Adenosine release and uptake in cerebellar granule neurons both occur via an equilibrative nucleoside carrier that is modulated by G proteins. J Neurochem. 1996 Jul;67(1):81-8.

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