Target Validation Information
TTD ID	T03661
Target Name	Adenosine deaminase (ADA)
Type of Target	Successful
Drug Potency against Target	Dipyridamole	Drug Info	IC50 = 64 nM	[3]
	Pentostatin	Drug Info	Ki = 0.2 nM	[2]
	3-(6-Amino-purin-9-yl)-4-butoxy-butan-2-ol	Drug Info	Ki = 123.4 nM	[1]
	3-(6-Amino-purin-9-yl)-4-p-tolyl-butan-2-ol	Drug Info	Ki = 302 nM	[1]
	3-(6-Amino-purin-9-yl)-4-phenethyloxy-butan-2-ol	Drug Info	Ki = 93.1 nM	[1]
	3-(6-Amino-purin-9-yl)-5-m-tolyl-pentan-2-ol	Drug Info	Ki = 1.02 nM	[1]
	3-(6-Amino-purin-9-yl)-6-o-tolyl-hexan-2-ol	Drug Info	Ki = 0.51 nM	[1]
	3-(6-Amino-purin-9-yl)-6-phenyl-hexan-2-ol	Drug Info	Ki = 0.89 nM	[1]
	3-(6-Amino-purin-9-yl)-7-phenyl-heptan-2-ol	Drug Info	Ki = 0.76 nM	[1]
	3-(6-Amino-purin-9-yl)-8-phenyl-octan-2-ol	Drug Info	Ki = 0.95 nM	[1]
	3-(6-Amino-purin-9-yl)-non-5-en-2-ol	Drug Info	Ki = 3.74 nM	[1]
	3-(6-Amino-purin-9-yl)-non-5-yn-2-ol	Drug Info	Ki = 188 nM	[1]
Action against Disease Model	Cladribine	Drug Info	IC50 on h uMan promyelocytic leukemia cell line HL60: 8.7nM	[4]
References
REF 1	Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R... J Med Chem. 2000 Nov 30;43(24):4694-700.
REF 2	Recent progress in the development of adenosine receptor ligands as antiinflammatory drugs. Curr Top Med Chem. 2006;6(13):1375-99.
REF 3	Adenosine 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.
REF 4	Lack 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.

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