Target Validation Information
Target ID T80782
Target Name mRNA of VEGFR1
Target Type
Clinical Trial
Drug Potency against Target CB-676475 Drug Info IC50 = 14100 nM [530858]
Phenyl-(5-phenyl-oxazol-2-yl)-amine Drug Info IC50 = 3000 nM [527458]
[3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol Drug Info IC50 = 1650 nM [527458]
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info IC50 = 14400 nM [527458]
4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 6300 nM [527245]
N3-GHQMFYYPra-NH2 Drug Info IC50 = 19400 nM [529026]
4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 14000 nM [527245]
(2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info IC50 = 3260 nM [527458]
3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info IC50 = 7600 nM [527458]
N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide Drug Info IC50 = 15000 nM [527245]
N-(2,4-Dichloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 530 nM [527245]
4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide Drug Info IC50 = 15000 nM [527245]
(5-Phenyl-oxazol-2-yl)-m-tolyl-amine Drug Info IC50 = 1700 nM [527458]
4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide Drug Info IC50 = 11000 nM [527245]
3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine Drug Info IC50 = 622 nM [526421]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info IC50 = 720 nM [528122]
SEMAXINIB Drug Info IC50 = 8 nM [525812]
C[homoPhe-Hca-Glu-Gly-Leu-Glu-Glu]-NH2 Drug Info IC50 = 19300 nM [529068]
VATALANIB Drug Info IC50 = 140 nM [528016]
Brivanib Drug Info Ki = 60 nM [528103]
4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide Drug Info IC50 = 4660 nM [527458]
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide Drug Info IC50 = 14000 nM [527245]
AAL-993 Drug Info IC50 = 170 nM [528016]
References
Ref 530858Bioorg Med Chem. 2010 May 15;18(10):3575-87. Epub 2010 Mar 27.Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.
Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 529026Bioorg Med Chem Lett. 2007 Oct 15;17(20):5590-4. Epub 2007 Aug 22.On-resin cyclization of peptide ligands of the Vascular Endothelial Growth Factor Receptor 1 by copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 526421Bioorg Med Chem Lett. 2002 Oct 7;12(19):2767-70.Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.
Ref 528122Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases.
Ref 525812J Med Chem. 2000 Jun 15;43(12):2310-23.New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.
Ref 529068J Med Chem. 2007 Oct 18;50(21):5135-46. Epub 2007 Sep 27.Rational design, structure, and biological evaluation of cyclic peptides mimicking the vascular endothelial growth factor.
Ref 528016Bioorg Med Chem Lett. 2006 Apr 1;16(7):1913-9. Epub 2006 Feb 3.Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.
Ref 528103J Med Chem. 2006 Apr 6;49(7):2143-6.Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 528016Bioorg Med Chem Lett. 2006 Apr 1;16(7):1913-9. Epub 2006 Feb 3.Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.

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