Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T09909 | ||||
Target Name | Type-2 angiotensin II receptor | ||||
Target Type | Successful |
||||
Drug Potency against Target | SC-55634 | Drug Info | IC50 = 4.9 nM | ||
SC-51895 | Drug Info | IC50 = 12 nM | |||
Sar-Arg-Val-Tyr-Ile-His-Pro-Ile | Drug Info | IC50 = 0.1 nM | [530232] | ||
PD-123319 | Drug Info | IC50 = 210 nM | [530232] | ||
Macrocyclic Quinazolinone analogue | Drug Info | IC50 = 20 nM | |||
L-158809 | Drug Info | IC50 = 37 nM | |||
L-158282 | Drug Info | IC50 = 3 nM | |||
L-162313 | Drug Info | IC50 = 2 nM | [530937] | ||
Sar-Arg-Val-Tyr-Ile-His-Pro-Ala | Drug Info | IC50 = 5.1 nM | [530232] | ||
SC-50560 | Drug Info | IC50 = 5.6 nM | |||
L-162234 | Drug Info | IC50 = 0.45 nM | [525772] | ||
L-159689 | Drug Info | IC50 = 0.7 nM | |||
L-159093 | Drug Info | IC50 = 4500 nM | [533939] | ||
Sar-Arg-Val-Tyr-Ile-His-Pro-Phe-OH | Drug Info | IC50 = 1.3 nM | [530734] | ||
ANGIOTENSIN II | Drug Info | IC50 = 2 nM | |||
Forasartan | Drug Info | IC50 = 6.9 nM | |||
SARALASIN | Drug Info | Ki = 0.15 nM | [529789] | ||
SC-52892 | Drug Info | IC50 = 6.5 nM | |||
References | |||||
Ref 530232 | J Med Chem. 1991 Nov;34(11):3248-60.Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. | ||||
Ref 530232 | J Med Chem. 1991 Nov;34(11):3248-60.Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. | ||||
Ref 530937 | Bioorg Med Chem. 2010 Jun 15;18(12):4570-90. Epub 2010 Apr 9.Selective angiotensin II AT(2) receptor agonists with reduced CYP 450 inhibition. | ||||
Ref 530232 | J Med Chem. 1991 Nov;34(11):3248-60.Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. | ||||
Ref 525772 | J Med Chem. 2000 May 18;43(10):1993-2006.Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity. | ||||
Ref 533939 | J Med Chem. 1993 Oct 15;36(21):3207-10.A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor. | ||||
Ref 530734 | J Med Chem. 1991 Apr;34(4):1514-7.1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists. | ||||
Ref 529789 | J Med Chem. 2008 Nov 27;51(22):7094-8.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 responses against carrageenan-induced hyperalgesia. |
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