Target Validation Information
TTD ID T67103
Target Name Integrin alpha-V (ITGAV)
Type of Target
Clinical trial
Drug Potency against Target Drug Info IC50 = 600 nM [9]
Ac-Asp-Arg-Leu-Asp-Ser-OH Drug Info IC50 = 25 nM [13]
AcDRGDS Drug Info IC50 = 20 nM [12]
C(-GRGDfL-) Drug Info IC50 = 100 nM [14]
C(Arg-Gly-Asp-D-Phe-Val) Drug Info IC50 = 680 nM [8]
C(RGDfF) Drug Info IC50 = 15.65 nM [6]
C(RGDfMeF) Drug Info IC50 = 19.81 nM [6]
C-[-Arg-Gly-Asp-Acpca30-] Drug Info IC50 = 6.56 nM [5]
C-[-Arg-Gly-Asp-Acpca31-] Drug Info IC50 = 3.43 nM [5]
C-[-Arg-Gly-Asp-Acpca32-] Drug Info IC50 = 0.59 nM [5]
C-[-Arg-Gly-Asp-Acpca33-] Drug Info IC50 = 26 nM [5]
Cyclo(RGDfV) (control) Drug Info IC50 = 28.7 nM [7]
Cyclo-[-Arg-Gly-Asp-Amp21-] Drug Info IC50 = 390 nM [15]
Cyclo-[-Arg-Gly-Asp-Amp22-] Drug Info IC50 = 600 nM [15]
CYCLORGDFV Drug Info IC50 = 9600 nM [18]
Cyclo[RGDfK(cypate)] Drug Info IC50 = 63.9 nM [7]
Cypate-[(RGD)2-NH2]1 Drug Info IC50 = 730 nM [7]
Cypate-[(RGD)2-NH2]2 Drug Info IC50 = 104 nM [7]
Cypate-[(RGD)3-NH2]1 Drug Info IC50 = 481 nM [7]
Cypate-[(RGD)3-NH2]2 Drug Info IC50 = 132 nM [7]
Cypate-[(RGD)4-NH2]1 Drug Info IC50 = 25.9 nM [7]
Cypate-[(RGD)4-NH2]2 Drug Info IC50 = 79.6 nM [7]
C[-Arg-Gly-Asp-Acpca19-] Drug Info IC50 = 411.5 nM [5]
C[-Arg-Gly-Asp-Acpca20-] Drug Info IC50 = 1300 nM [5]
C[-Arg-Gly-Asp-Acpca21-] Drug Info IC50 = 125.4 nM [5]
C[-Arg-Gly-Asp-Acpca22-] Drug Info IC50 = 165.5 nM [5]
C[-Arg-Gly-Asp-Acpca34-] Drug Info IC50 = 29.6 nM [5]
C[-Arg-Gly-Asp-Acpca35-] Drug Info IC50 = 13.1 nM [5]
C[-Arg-Gly-Asp-Acpca36-] Drug Info IC50 = 4.56 nM [5]
C[RGD-(R)-alpha-TfmfV] Drug Info IC50 = 72.7 nM [6]
C[RGD-(S)-alpha-TfmfV] Drug Info IC50 = 10.03 nM [6]
C[RGDf-(3R)-Carboxymorpholine] Drug Info IC50 = 21 nM [16]
C[RGDf-(3S)-Carboxymorpholine] Drug Info IC50 = 157 nM [16]
C[RGDf-(R)-alpha-TfmF] Drug Info IC50 = 93.5 nM [6]
C[RGDf-(R)-alpha-TfmV] Drug Info IC50 = 42.8 nM [6]
C[RGDf-(R)-N-Me-alpha-TfmF] Drug Info IC50 = 93.9 nM [6]
C[RGDf-(S)-alpha-TfmF] Drug Info IC50 = 35.5 nM [6]
C[RGDf-(S)-alpha-TfmV] Drug Info IC50 = 3.4 nM [6]
C[RGDf-(S)-N-Me-alpha-TfmF] Drug Info IC50 = 7.7 nM [6]
C[RGDf-(S,R)-alpha-Dfm-F] Drug Info IC50 = 5.5 nM [6]
E[c(RGDyK)]2 Drug Info IC50 = 2.9 nM [4]
E[c(RGDyK)]2-PTX conjugate Drug Info IC50 = 134 nM [4]
G(D-Pen)-G-H-R-G-D-L-R-C-A Drug Info IC50 = 5270 nM [20]
Gly-Arg-Gly-Asp-Ser Drug Info IC50 = 750 nM [17]
Gly-Arg-Gly-Asp-Ser-Pro-Lys Drug Info IC50 = 210 nM [1]
ISONIPECOTAMIDE Drug Info IC50 = 45.7 nM [2]
N-(3,5-dichlorophenyl)imidodicarbonimidic diamide Drug Info IC50 = 33.5 nM [19]
NAVPNLRGDLQVLAQKVART Drug Info IC50 = 1540 nM [11]
RGDechi Drug Info IC50 = 880 nM [8]
SB-223245 Drug Info Ki = 2 nM [21]
SB-265123 Drug Info IC50 = 2.9 nM [3]
ST-1646 Drug Info IC50 = 0.9 nM [15]
TR-14035 Drug Info IC50 = 414 nM [10]
References
REF 1 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 2 Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.
REF 3 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 4 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 5 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 6 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 7 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 8 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 9 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 10 2,6-Quinolinyl derivatives as potent VLA-4 antagonists. Bioorg Med Chem Lett. 2007 Jan 1;17(1):142-6.
REF 11 Structure-function analysis of Arg-Gly-Asp helix motifs in alpha v beta 6 integrin ligands. J Biol Chem. 2007 Mar 30;282(13):9657-65.
REF 12 Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2329-33.
REF 13 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 14 Multiple N-methylation by a designed approach enhances receptor selectivity. J Med Chem. 2007 Nov 29;50(24):5878-81.
REF 15 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 16 Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity. Bioorg Med Chem. 2009 Feb 15;17(4):1542-9.
REF 17 alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers. J Med Chem. 2009 Nov 26;52(22):7029-43.
REF 18 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 19 Emerging targets in osteoporosis disease modification. J Med Chem. 2010 Jun 10;53(11):4332-53.
REF 20 Design and synthesis of novel cyclic RGD-containing peptides as highly potent and selective integrin alpha IIb beta 3 antagonists. J Med Chem. 1994 Jan 7;37(1):1-8.
REF 21 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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