Target Validation Information
TTD ID T09909
Target Name Angiotensin II receptor type-2 (AGTR2)
Type of Target
Successful
Drug Potency against Target Drug Info IC50 = 20 nM
ANGIOTENSIN II Drug Info IC50 = 2 nM
Forasartan Drug Info IC50 = 6.9 nM
L-158282 Drug Info IC50 = 3 nM
L-158809 Drug Info IC50 = 37 nM
L-159093 Drug Info IC50 = 4500 nM [6]
L-159689 Drug Info IC50 = 0.7 nM
L-162234 Drug Info IC50 = 0.45 nM [1]
L-162313 Drug Info IC50 = 2 nM [5]
PD-123319 Drug Info IC50 = 210 nM [3]
Sar-Arg-Val-Tyr-Ile-His-Pro-Ala Drug Info IC50 = 5.1 nM [3]
Sar-Arg-Val-Tyr-Ile-His-Pro-Ile Drug Info IC50 = 0.1 nM [3]
Sar-Arg-Val-Tyr-Ile-His-Pro-Phe-OH Drug Info IC50 = 1.3 nM [4]
SARALASIN Drug Info Ki = 0.15 nM [2]
SC-50560 Drug Info IC50 = 5.6 nM
SC-51895 Drug Info IC50 = 12 nM
SC-52892 Drug Info IC50 = 6.5 nM
SC-55634 Drug Info IC50 = 4.9 nM
References
REF 1 Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity. J Med Chem. 2000 May 18;43(10):1993-2006.
REF 2 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 3 Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 sub... J Med Chem. 1991 Nov;34(11):3248-60.
REF 4 1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists. J Med Chem. 1991 Apr;34(4):1514-7.
REF 5 Selective angiotensin II AT(2) receptor agonists with reduced CYP 450 inhibition. Bioorg Med Chem. 2010 Jun 15;18(12):4570-90.
REF 6 A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor. J Med Chem. 1993 Oct 15;36(21):3207-10.

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