Target Validation Information
Target ID T23355
Target Name mRNA of integrin beta 3
Target Type
Discontinued
Drug Potency against Target CYCLORGDFV Drug Info IC50 = 9600 nM [530622]
C(RGDfF) Drug Info IC50 = 10.31 nM [528059]
Cyclo-[-Arg-Gly-Asp-Amp25-] Drug Info IC50 = 550 nM [529343]
ST-1646 Drug Info IC50 = 5.64 nM [529343]
C[RGDf-(S,R)-alpha-Dfm-F] Drug Info IC50 = 331.8 nM [528059]
DMP-757 Drug Info IC50 = 20 nM
SKF-107260 Drug Info Ki = 4.5 nM
SKF-106760 Drug Info Ki = 175 nM [526821]
C(-GRGDfL-) Drug Info IC50 = 195 nM [529125]
C[-Arg-Gly-Asp-Acpca19-] Drug Info IC50 = 132.9 nM [527884]
XEMILOFIBAN Drug Info IC50 = 2 nM [525656]
3-(3-(carbamoyl)benzamido)propanoic acid Drug Info IC50 = 9 nM [528383]
3-(3-(benzamido)-5-nitrobenzamido)propanoic acid Drug Info IC50 = 32 nM [528383]
L-709780 Drug Info IC50 = 25 nM
SB-208651 Drug Info Ki = 1.6 nM [525429]
SC-54701A Drug Info IC50 = 35 nM [534458]
ELAROFIBAN Drug Info IC50 = 0.15 nM [527223]
SC-47643 Drug Info IC50 = 2400 nM [533764]
SB-207043 Drug Info Ki = 110 nM
L-734217 Drug Info IC50 = 32 nM [525867]
N-(3,5-dichlorophenyl)imidodicarbonimidic diamide Drug Info IC50 = 33.5 nM [530779]
L-703014 Drug Info IC50 = 94 nM [525874]
Ro-43-8857 Drug Info IC50 = 70 nM [525874]
LOTRAFIBAN Drug Info IC50 = 28 nM [525874]
Gantofiban Drug Info IC50 = 8 nM [525874]
ZD-2486 Drug Info IC50 = 50 nM [525874]
Ro-43-5054 Drug Info IC50 = 30 nM [525874]
L-756568 Drug Info IC50 = 13 nM [525874]
DMP-728 Drug Info IC50 = 46 nM [525874]
LAMIFIBAN Drug Info IC50 = 30 nM [525874]
L-734115 Drug Info IC50 = 9 nM [525874]
ROXIFIBAN Drug Info IC50 = 60 nM [525874]
C[RGD-(S)-alpha-TfmfV] Drug Info IC50 = 237.1 nM [528059]
L-767679 Drug Info IC50 = 12 nM [525874]
L-746233 Drug Info IC50 = 15 nM [525874]
L-739758 Drug Info IC50 = 8 nM [525874]
FK-633 Drug Info IC50 = 103 nM [525874]
MK-852 Drug Info IC50 = 26 nM [525874]
SIBRAFIBAN Drug Info IC50 = 38 nM [525874]
ORBOFIBAN Drug Info IC50 = 80 nM [525874]
Cypate-[(RGD)2-NH2]2 Drug Info IC50 = 104 nM [528111]
Cypate-[(RGD)3-NH2]2 Drug Info IC50 = 132 nM [528111]
C[RGDf-(S)-N-Me-alpha-TfmF] Drug Info IC50 = 18.8 nM [528059]
C[RGDf-(S)-alpha-TfmV] Drug Info IC50 = 36.3 nM [528059]
C(RGDfMeF) Drug Info IC50 = 19.75 nM [528059]
C[-Arg-Gly-Asp-Acpca21-] Drug Info IC50 = 44.7 nM [527884]
C-[-Arg-Gly-Asp-Acpca32-] Drug Info IC50 = 1.5 nM [527884]
RGDechi Drug Info IC50 = 880 nM [528215]
C[-Arg-Gly-Asp-Acpca35-] Drug Info IC50 = 7.2 nM [527884]
C[-Arg-Gly-Asp-Acpca36-] Drug Info IC50 = 5.6 nM [527884]
C[-Arg-Gly-Asp-Acpca34-] Drug Info IC50 = 35.6 nM [527884]
C[RGDf-(R)-alpha-TfmF] Drug Info IC50 = 7237.9 nM [528059]
Cyclo-[-Arg-Gly-Asp-Amp22-] Drug Info IC50 = 600 nM [529343]
3-(3-(carbamoyl)benzamido)-3-phenylpropanoic acid Drug Info IC50 = 1 nM [528383]
AcDRGDS Drug Info IC50 = 20 nM [528659]
Gly-Arg-Gly-Asp-Ser Drug Info IC50 = 120 nM [530479]
C(RGDfV) Drug Info IC50 = 600 nM [528438]
Ac-Asp-Arg-Leu-Asp-Ser-OH Drug Info IC50 = 25 nM [529045]
ISONIPECOTAMIDE Drug Info IC50 = 1810 nM [527223]
SB-223245 Drug Info Ki = 2 nM [534805]
E[c(RGDyK)]2 Drug Info IC50 = 2.9 nM [527440]
L-750034 Drug Info IC50 = 16 nM [526893]
Gly-Arg-Gly-Asp-Ser-Pro-Lys Drug Info IC50 = 1700 nM [525558]
Cyclo[RGDfK(cypate)] Drug Info IC50 = 63.9 nM [528111]
Cypate-[(RGD)3-NH2]1 Drug Info IC50 = 481 nM [528111]
Cypate-[(RGD)2-NH2]1 Drug Info IC50 = 730 nM [528111]
Cyclo(RGDfV) (control) Drug Info IC50 = 28.7 nM [528111]
Cypate-[(RGD)4-NH2]1 Drug Info IC50 = 25.9 nM [528111]
C[RGDf-(S)-alpha-TfmF] Drug Info IC50 = 35.5 nM [528059]
C[RGDf-(R)-alpha-TfmV] Drug Info IC50 = 285.3 nM [528059]
Cypate-[(RGD)4-NH2]2 Drug Info IC50 = 79.6 nM [528111]
C-[-Arg-Gly-Asp-Acpca33-] Drug Info IC50 = 9.93 nM [527884]
C[-Arg-Gly-Asp-Acpca22-] Drug Info IC50 = 51.4 nM [527884]
C[-Arg-Gly-Asp-Acpca20-] Drug Info IC50 = 712.7 nM [527884]
C-[-Arg-Gly-Asp-Acpca30-] Drug Info IC50 = 7.7 nM [527884]
C-[-Arg-Gly-Asp-Acpca31-] Drug Info IC50 = 4.6 nM [527884]
C[RGD-(R)-alpha-TfmfV] Drug Info IC50 = 1017.8 nM [528059]
E[c(RGDyK)]2-PTX conjugate Drug Info IC50 = 134 nM [527440]
Cyclo-[-Arg-Gly-Asp-Amp24-] Drug Info IC50 = 178 nM [529343]
C[RGDf-(R)-N-Me-alpha-TfmF] Drug Info IC50 = 704.4 nM [528059]
C(Arg-Gly-Asp-D-Phe-Val) Drug Info IC50 = 680 nM [528215]
DMP-802 Drug Info IC50 = 29 nM [525874]
SB-265123 Drug Info IC50 = 1200 nM [527268]
References
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Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 529343J Med Chem. 2008 Mar 27;51(6):1771-82. Epub 2008 Feb 28.Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
Ref 529343J Med Chem. 2008 Mar 27;51(6):1771-82. Epub 2008 Feb 28.Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 526821J Med Chem. 1992 Oct 16;35(21):3970-2.Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists.
Ref 529125J Med Chem. 2007 Nov 29;50(24):5878-81. Epub 2007 Nov 1.Multiple N-methylation by a designed approach enhances receptor selectivity.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 525656J Med Chem. 1999 Dec 16;42(25):5254-65.Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.
Ref 528383Bioorg Med Chem Lett. 2006 Oct 15;16(20):5294-7. Epub 2006 Aug 21.Derivatives of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids as novel fibrinogen receptor antagonists.
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Ref 534458J Med Chem. 1997 Aug 29;40(18):2843-57.Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists.
Ref 527223Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.
Ref 533764J Med Chem. 1995 Jan 6;38(1):34-41.Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation.
Ref 525867Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8.Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.
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Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 528215J Med Chem. 2006 Jun 1;49(11):3416-20.Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 529343J Med Chem. 2008 Mar 27;51(6):1771-82. Epub 2008 Feb 28.Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
Ref 528383Bioorg Med Chem Lett. 2006 Oct 15;16(20):5294-7. Epub 2006 Aug 21.Derivatives of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids as novel fibrinogen receptor antagonists.
Ref 528659Bioorg Med Chem Lett. 2007 Apr 15;17(8):2329-33. Epub 2007 Jan 27.Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics.
Ref 530479J Med Chem. 2009 Nov 26;52(22):7029-43.alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers.
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Ref 529045Bioorg Med Chem. 2007 Dec 1;15(23):7380-90. Epub 2007 Aug 22.Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffolds.
Ref 527223Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.
Ref 534805Bioorg Med Chem Lett. 1998 Nov 17;8(22):3171-6.Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model.
Ref 527440J Med Chem. 2005 Feb 24;48(4):1098-106.Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery.
Ref 526893J Med Chem. 2003 Dec 4;46(25):5316-25.Molecular model of the alpha(IIb)beta(3) integrin.
Ref 525558J Med Chem. 1999 Aug 12;42(16):3033-40.N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists.
Ref 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 527884J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 527440J Med Chem. 2005 Feb 24;48(4):1098-106.Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery.
Ref 529343J Med Chem. 2008 Mar 27;51(6):1771-82. Epub 2008 Feb 28.Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
Ref 528059J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Ref 528215J Med Chem. 2006 Jun 1;49(11):3416-20.Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior.
Ref 525874J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Ref 527268Bioorg Med Chem Lett. 2004 Dec 6;14(23):5937-41.1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability.

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