Target Validation Information
TTD ID T23355
Target Name ITGB3 messenger RNA (ITGB3 mRNA)
Type of Target
Discontinued
Drug Potency against Target Drug Info IC50 = 600 nM [16]
3-(3-(benzamido)-5-nitrobenzamido)propanoic acid Drug Info IC50 = 32 nM [15]
3-(3-(carbamoyl)benzamido)-3-phenylpropanoic acid Drug Info IC50 = 1 nM [15]
3-(3-(carbamoyl)benzamido)propanoic acid Drug Info IC50 = 9 nM [15]
Ac-Asp-Arg-Leu-Asp-Ser-OH Drug Info IC50 = 25 nM [18]
AcDRGDS Drug Info IC50 = 20 nM [17]
C(-GRGDfL-) Drug Info IC50 = 195 nM [19]
C(Arg-Gly-Asp-D-Phe-Val) Drug Info IC50 = 680 nM [14]
C(RGDfF) Drug Info IC50 = 10.31 nM [12]
C(RGDfMeF) Drug Info IC50 = 19.75 nM [12]
C-[-Arg-Gly-Asp-Acpca30-] Drug Info IC50 = 7.7 nM [11]
C-[-Arg-Gly-Asp-Acpca31-] Drug Info IC50 = 4.6 nM [11]
C-[-Arg-Gly-Asp-Acpca32-] Drug Info IC50 = 1.5 nM [11]
C-[-Arg-Gly-Asp-Acpca33-] Drug Info IC50 = 9.93 nM [11]
Cyclo(RGDfV) (control) Drug Info IC50 = 28.7 nM [13]
Cyclo-[-Arg-Gly-Asp-Amp22-] Drug Info IC50 = 600 nM [20]
Cyclo-[-Arg-Gly-Asp-Amp24-] Drug Info IC50 = 178 nM [20]
Cyclo-[-Arg-Gly-Asp-Amp25-] Drug Info IC50 = 550 nM [20]
CYCLORGDFV Drug Info IC50 = 9600 nM [22]
Cyclo[RGDfK(cypate)] Drug Info IC50 = 63.9 nM [13]
Cypate-[(RGD)2-NH2]1 Drug Info IC50 = 730 nM [13]
Cypate-[(RGD)2-NH2]2 Drug Info IC50 = 104 nM [13]
Cypate-[(RGD)3-NH2]1 Drug Info IC50 = 481 nM [13]
Cypate-[(RGD)3-NH2]2 Drug Info IC50 = 132 nM [13]
Cypate-[(RGD)4-NH2]1 Drug Info IC50 = 25.9 nM [13]
Cypate-[(RGD)4-NH2]2 Drug Info IC50 = 79.6 nM [13]
C[-Arg-Gly-Asp-Acpca19-] Drug Info IC50 = 132.9 nM [11]
C[-Arg-Gly-Asp-Acpca20-] Drug Info IC50 = 712.7 nM [11]
C[-Arg-Gly-Asp-Acpca21-] Drug Info IC50 = 44.7 nM [11]
C[-Arg-Gly-Asp-Acpca22-] Drug Info IC50 = 51.4 nM [11]
C[-Arg-Gly-Asp-Acpca34-] Drug Info IC50 = 35.6 nM [11]
C[-Arg-Gly-Asp-Acpca35-] Drug Info IC50 = 7.2 nM [11]
C[-Arg-Gly-Asp-Acpca36-] Drug Info IC50 = 5.6 nM [11]
C[RGD-(R)-alpha-TfmfV] Drug Info IC50 = 1017.8 nM [12]
C[RGD-(S)-alpha-TfmfV] Drug Info IC50 = 237.1 nM [12]
C[RGDf-(R)-alpha-TfmF] Drug Info IC50 = 7237.9 nM [12]
C[RGDf-(R)-alpha-TfmV] Drug Info IC50 = 285.3 nM [12]
C[RGDf-(R)-N-Me-alpha-TfmF] Drug Info IC50 = 704.4 nM [12]
C[RGDf-(S)-alpha-TfmF] Drug Info IC50 = 35.5 nM [12]
C[RGDf-(S)-alpha-TfmV] Drug Info IC50 = 36.3 nM [12]
C[RGDf-(S)-N-Me-alpha-TfmF] Drug Info IC50 = 18.8 nM [12]
C[RGDf-(S,R)-alpha-Dfm-F] Drug Info IC50 = 331.8 nM [12]
DMP-728 Drug Info IC50 = 46 nM [5]
DMP-757 Drug Info IC50 = 20 nM
DMP-802 Drug Info IC50 = 29 nM [5]
ELAROFIBAN Drug Info IC50 = 0.15 nM [8]
E[c(RGDyK)]2 Drug Info IC50 = 2.9 nM [10]
E[c(RGDyK)]2-PTX conjugate Drug Info IC50 = 134 nM [10]
FK-633 Drug Info IC50 = 103 nM [5]
Gantofiban Drug Info IC50 = 8 nM [5]
Gly-Arg-Gly-Asp-Ser Drug Info IC50 = 120 nM [21]
Gly-Arg-Gly-Asp-Ser-Pro-Lys Drug Info IC50 = 1700 nM [2]
ISONIPECOTAMIDE Drug Info IC50 = 1810 nM [8]
L-703014 Drug Info IC50 = 94 nM [5]
L-709780 Drug Info IC50 = 25 nM
L-734115 Drug Info IC50 = 9 nM [5]
L-734217 Drug Info IC50 = 32 nM [4]
L-739758 Drug Info IC50 = 8 nM [5]
L-746233 Drug Info IC50 = 15 nM [5]
L-750034 Drug Info IC50 = 16 nM [7]
L-756568 Drug Info IC50 = 13 nM [5]
L-767679 Drug Info IC50 = 12 nM [5]
LAMIFIBAN Drug Info IC50 = 30 nM [5]
LOTRAFIBAN Drug Info IC50 = 28 nM [5]
MK-852 Drug Info IC50 = 26 nM [5]
N-(3,5-dichlorophenyl)imidodicarbonimidic diamide Drug Info IC50 = 33.5 nM [23]
ORBOFIBAN Drug Info IC50 = 80 nM [5]
RGDechi Drug Info IC50 = 880 nM [14]
Ro-43-5054 Drug Info IC50 = 30 nM [5]
Ro-43-8857 Drug Info IC50 = 70 nM [5]
ROXIFIBAN Drug Info IC50 = 60 nM [5]
SB-207043 Drug Info Ki = 110 nM
SB-208651 Drug Info Ki = 1.6 nM [1]
SB-223245 Drug Info Ki = 2 nM [26]
SB-265123 Drug Info IC50 = 1200 nM [9]
SC-47643 Drug Info IC50 = 2400 nM [24]
SC-54701A Drug Info IC50 = 35 nM [25]
SIBRAFIBAN Drug Info IC50 = 38 nM [5]
SKF-106760 Drug Info Ki = 175 nM [6]
SKF-107260 Drug Info Ki = 4.5 nM
ST-1646 Drug Info IC50 = 5.64 nM [20]
XEMILOFIBAN Drug Info IC50 = 2 nM [3]
ZD-2486 Drug Info IC50 = 50 nM [5]
References
REF 1 Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists. J Med Chem. 1999 Feb 25;42(4):545-59.
REF 2 N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists. J Med Chem. 1999 Aug 12;42(16):3033-40.
REF 3 Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308. J Med Chem. 1999 Dec 16;42(25):5254-65.
REF 4 Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity o... Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8.
REF 5 Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. J Med Chem. 2000 Sep 21;43(19):3453-73.
REF 6 Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists. J Med Chem. 1992 Oct 16;35(21):3970-2.
REF 7 Molecular model of the alpha(IIb)beta(3) integrin. J Med Chem. 2003 Dec 4;46(25):5316-25.
REF 8 Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.
REF 9 1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5937-41.
REF 10 Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery. J Med Chem. 2005 Feb 24;48(4):1098-106.
REF 11 Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders. J Med Chem. 2005 Dec 1;48(24):7675-87.
REF 12 Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study ... J Med Chem. 2006 Mar 9;49(5):1808-17.
REF 13 Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors. J Med Chem. 2006 Apr 6;49(7):2268-75.
REF 14 Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior. J Med Chem. 2006 Jun 1;49(11):3416-20.
REF 15 Derivatives of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids as novel fibrinogen receptor antagonists. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5294-7.
REF 16 Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5878-82.
REF 17 Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2329-33.
REF 18 Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one sc... Bioorg Med Chem. 2007 Dec 1;15(23):7380-90.
REF 19 Multiple N-methylation by a designed approach enhances receptor selectivity. J Med Chem. 2007 Nov 29;50(24):5878-81.
REF 20 Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues. J Med Chem. 2008 Mar 27;51(6):1771-82.
REF 21 alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers. J Med Chem. 2009 Nov 26;52(22):7029-43.
REF 22 Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetr... J Med Chem. 2010 Jan 14;53(1):106-18.
REF 23 Emerging targets in osteoporosis disease modification. J Med Chem. 2010 Jun 10;53(11):4332-53.
REF 24 Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation. J Med Chem. 1995 Jan 6;38(1):34-41.
REF 25 Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists. J Med Chem. 1997 Aug 29;40(18):2843-57.
REF 26 Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a resten... Bioorg Med Chem Lett. 1998 Nov 17;8(22):3171-6.

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