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Integrin alpha-V/beta-3 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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▼
CilengitideIC500.54 [1]
CilengitideKi1.0 [1]
Cyclo(Arg-Gly-Asp-D-Phe-Val)IC5010.8 [1]
2-[(2S)-7-[1H-Benzimidazol-2-ylmethyl(methyl)carbamoyl]-4-methyl-3-oxo-2,5-dihydro-1H-1,4-benzodiazepin-2-yl]acetic acidIC50145.0 [1]
2-[(2S)-7-[1H-Benzimidazol-2-ylmethyl(methyl)carbamoyl]-4-methyl-3-oxo-2,5-dihydro-1H-1,4-benzodiazepin-2-yl]acetic acidKi2.0 [1]
2-[(9S)-14-[3-(Pyridin-2-ylamino)propoxy]-9-tricyclo[9.4.0.03,8]pentadeca-1(11),3,5,7,12,14-hexaenyl]acetic acidIC504.0 [1], 60.0 [2]
2-[(9S)-14-[3-(Pyridin-2-ylamino)propoxy]-9-tricyclo[9.4.0.03,8]pentadeca-1(11),3,5,7,12,14-hexaenyl]acetic acidKi4.0 [1]
TirofibanIC501000.0 [1], 62000.0 [2], 100000.0 [3], 260000.0 [4]
2-[(4S)-8-[2-[6-(Methylamino)pyridin-2-yl]ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-2-benzazepin-4-yl]acetic acidIC500.15 [1], 3.0 [2]
2-[(4S)-8-[2-[6-(Methylamino)pyridin-2-yl]ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-2-benzazepin-4-yl]acetic acidKi1.2 [1]
2-Benzenesulfonylamino-3-[4-(2-piperidin-4-yl-ethoxy)-benzoylamino]-propionic acidIC501000.0 [1]
(3S)-3-[[2-[(3S)-2-Oxo-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]acetyl]amino]-3-pyridin-3-ylpropanoic acidIC500.35 [1], 0.4 [2]
2-[(2S)-7-(1H-Benzimidazol-2-ylmethylcarbamoyl)-4-methyl-3-oxo-2,5-dihydro-1H-1,4-benzodiazepin-2-yl]acetic acidIC501650.0 [1]
2-[(2S)-7-(1H-Benzimidazol-2-ylmethylcarbamoyl)-4-methyl-3-oxo-2,5-dihydro-1H-1,4-benzodiazepin-2-yl]acetic acidKi15.0 [1]
3-Phenyl-4-[4-[3-(2-pyridinylamino)propoxy]phenyl]butanoic acidIC508.0 [1], 29.0 [2], 500.0 [3]
3-Phenyl-4-[4-[3-(2-pyridinylamino)propoxy]phenyl]butanoic acidKi32.0 [1]
Arginyl-glycyl-aspartic acidIC5010000.0 [1], 12000.0 [2]
MK-0429IC500.08 [1], 0.3 [2]
(S)-3-Quinolin-3-yl-3-(5-5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl-pentanoylamino)-propionic acidIC501.07 [1], 1.6 [2]
(3S)-3-(2,3-Dihydro-1-benzofuran-6-yl)-3-[5-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)pentanoylamino]propanoic acidIC503.0 [1], 3.03 [2]
3-[[2-[4-(5,6,7,8-Tetrahydro-1,8-naphthyridin-2-yl)butanoylamino]acetyl]amino]propanoic acidIC5048.0 [1], 111.0 [2]
(3S)-3-(3-Fluorophenyl)-3-[5-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)pentanoylamino]propanoic acidIC5022.7 [1], 22.8 [2], 23.0 [3]
(3S)-3-Pyridin-3-yl-3-[[2-[4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)butanoylamino]acetyl]amino]propanoic acidIC501.3 [1], 8.8 [2]
3-[[5-[(2-Pyridyl)amino]pentanoylamino]acetylamino]-3-(4-biphenylyl)propionic acidIC500.45 [1], 9500.0 [2]
(2S)-2-(Benzenesulfonamido)-3-[[4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]benzoyl]amino]propanoic acidIC500.07 [1], 0.3 [2]
(2S)-2-(Benzenesulfonamido)-3-[[3-methoxy-4-[4-(1,4,5,6-tetrahydropyrimidin-2-ylamino)piperidin-1-yl]benzoyl]amino]propanoic acidIC500.19 [1], 110.0 [2]
3-{4-[2-(6-Amino-pyridin-2-yl)-ethyl]-benzoylamino}-2-(4-iodo-benzenesulfonylamino)-propionic acidIC500.08 [1], 0.1 [2]
(3S)-3-(1,3-Benzodioxol-5-yl)-4-[3-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]-1,2,4-oxadiazol-5-yl]butanoic acidIC500.4 [1], 0.65 [2]
4-[2-[5-[(4-Methyl-2-pyridyl)amino]pentanoyl]hydrazinocarbonyl]-3-(3,5-dichlorophenyl)butyric acidIC506.0 [1], 20000.0 [2]
4-[2-[5-[(4-Methyl-2-pyridyl)amino]pentanoyl]hydrazinocarbonyl]-3-(4-biphenylyl)butyric acidIC503.0 [1], 4.0 [2], 970.0 [3]
3-{4-[2-(6-Amino-pyridin-2-yl)-ethyl]-benzoylamino}-2-benzenesulfonylamino-propionic acidIC500.08 [1], 0.4 [2], 0.44 [3]
3-[[4-[(2-Pyridyl)amino]butyrylamino]acetylamino]-3-(3-nitrophenyl)propionic acidIC5013.0 [1], 6900.0 [2]
3-((5-(2-Chloro-4,5-dimethoxybenzylidene)-3-methyl-4-oxothiazolidin-2-ylidene)amino)benzoic acidIC500.03 [1], 30.0 [2]
3-[2-(5-Guanidinopentanoyl)hydrazinocarbonylamino]-3-phenylpropionic acidIC5040.0 [1], 50000.0 [2]
2-[(1S,4S,10S,13S)-10-[3-(Diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-14-propanoyl-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acidIC500.03 [1], 5.6 [2], 251.0 [3]
2-[(1S,4S,10S,13S)-14-Benzoyl-10-[3-(diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acidIC500.16 [1], 5.15 [2], 600.0 [3]
2-[(1R,4S,10S,13S)-14-Benzoyl-10-[3-(diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acidIC500.91 [1], 174.0 [2], 327.0 [3]
2-[(1R,4S,10S,13S)-10-[3-(Diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acidIC505.12 [1], 7.01 [2], 550.0 [3]
2-[(1S,4S,10S,13S)-10-[3-(Diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acidIC500.47 [1], 4.4 [2], 23.7 [3]
2-[(1S,4S,10S,13S)-10-[3-(Diaminomethylideneamino)propyl]-14-heptyl-3,6,9,12-tetraoxo-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acidIC500.08 [1], 2.84 [2], 178.0 [3]
2-[(1R,4S,10S,13R)-10-[3-(Diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acidIC500.18 [1], 75.14 [2], 1350.0 [3]
(2S)-2-[[4-[4-[[(19S)-19-Ethyl-19-hydroxy-10-[(E)-(2-methylpropan-2-yl)oxyiminomethyl]-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl]oxycarbonyl]piperazine-1-carbonyl]phenyl]methoxycarbonylamino]-5-oxo-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acidIC504.83 [1], 130.0 [2], 670.0 [3]
(2S)-2-[[4-[4-[[(19S)-8-[(Dimethylamino)methyl]-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl]oxycarbonyl]piperazine-1-carbonyl]phenyl]methoxycarbonylamino]-5-oxo-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acidIC504.97 [1], 540.0 [2], 1000.0 [3]
(2S)-2-[[4-[4-[[(19S)-19-Ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2(11),3,5,7,9,15(20)-heptaen-7-yl]oxycarbonyl]piperazine-1-carbonyl]phenyl]methoxycarbonylamino]-5-oxo-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acidIC502.28 [1], 350.0 [2], 730.0 [3]
4-[[(1S)-1-Carboxy-4-oxo-4-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]butyl]carbamoyloxymethyl]benzoic acidIC500.08 [1], 6.3 [2], 17.0 [3]
(1S,5S,11S,19R)-5,16-Diamino-3,6,9,18-tetraoxo-2,7,10,15,17,20-hexazabicyclo[17.2.1]docos-15-ene-11-carboxylic acidIC501.1 [1], 530.0 [2], 840.0 [3]
(2S)-2-[[4-[4-[[(19S)-10,19-Diethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl]oxycarbonyl]piperazine-1-carbonyl]phenyl]methoxycarbonylamino]-5-oxo-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acidIC501.3 [1], 37.0 [2], 89.0 [3]
Glycyl-arginyl-glycyl-aspartyl-seryl-prolyl-lysineIC50210.0 [1]
Arginyl-glycyl-aspartyl-tryptophanIC5014000.0 [1], 34000.0 [2]
2-[(12S,18S)-18-[3-(Diaminomethylideneamino)propyl]-19-methyl-11,14,17,20-tetraoxo-2,3-dithia-10,13,16,19-tetrazatricyclo[19.4.0.04,9]pentacosa-1(25),4,6,8,21,23-hexaen-12-yl]acetic acidKi3.5 [1]
Arg-Gly-Asp-Arg-Gly-AspIC5070.0 [1], 619000.0 [2]
3-(3,5-Dichlorophenyl)-3-[[2-[(3-guanidinobenzoyl)amino]acetyl]amino]propanoic acidIC501.1 [1], 25.12 [2]
3-(3-Pyridyl)-3-[4-[2-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-yl)ethyl]indol-1-yl]propionic acidIC500.5 [1]
(2S)-3-[[(5S,8S)-8-[(1H-Imidazol-2-ylamino)methyl]-7-(pyridin-3-ylmethoxycarbonyl)-1-oxa-2,7-diazaspiro[4.4]non-2-ene-3-carbonyl]amino]-2-[(2,4,6-trimethylphenyl)sulfonylamino]propanoic acidIC5032.0 [1]
2-[(1S,3R,9S,11R,14S)-9-[3-(Diaminomethylideneamino)propyl]-4,7,10,18-tetraoxo-2,5,8,19-tetrazatricyclo[9.6.2.014,19]nonadecan-3-yl]acetic acidIC501.4 [1], 5.64 [2]
N-(3,5-Dichlorophenyl)imidodicarbonimidic diamideIC5033.5 [1], 33500.0 [2]
3-(1,3-Benzodioxol-5-yl)-3-[5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]indol-1-yl]propanoic acidIC500.38 [1]
3-[5-[2-(5,6,7,8-Tetrahydro[1,8]naphthyridin-2-yl)ethoxy]indol-1-yl]-3-(3-pyridyl)propionic acidIC500.25 [1]
7-[[4-(2-Pyridylamino)butyrylamino]methyl]-6,9-dihydro-5H-benzocycloheptene-5-acetic acidIC501.9 [1], 2.0 [2]
3-[4-(6-Amino-hexyloxy)-phenyl]-2-(butane-1-sulfonylamino)-propionic acidIC50150000.0 [1], 330000.0 [2]
(2-{4-[2-(5,6,7,8-Tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acidIC503.0 [1], 5.0 [2]
3-Phenyl-3-{5-[2-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-ethoxy]-indol-1-yl}-propionic acidIC501.0 [1]
(2S)-2-(Benzenesulfonamido)-3-[[4-[4-(1,4,5,6-tetrahydropyrimidin-2-ylamino)piperidin-1-yl]benzoyl]amino]propanoic acidIC501.3 [1], 190.0 [2]
2-Benzyloxycarbonylamino-3-[4-(4-piperidin-4-yl-butoxy)-phenyl]-propionic acidIC5056000.0 [1], 158000.0 [2]
(2S)-3-[[5-[4-(1H-Imidazol-2-ylamino)-4-oxobutyl]-4,5-dihydro-1,2-oxazole-3-carbonyl]amino]-2-[(2,4,6-trimethylphenyl)sulfonylamino]propanoic acidIC5031.0 [1]
(2S)-3-[[5-[4-(Diaminomethylideneamino)butyl]-4,5-dihydro-1,2-oxazole-3-carbonyl]amino]-2-[(2,4,6-trimethylphenyl)sulfonylamino]propanoic acidIC500.7 [1], 169.0 [2]
3-[[4-[(4-Methyl-2-pyridyl)amino]butyrylamino]acetylamino]-3-[4-(1-naphthyl)phenyl]propionic acidIC508.0 [1], 3000.0 [2]
(3S)-3-[[2-[2-Oxo-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]piperidin-1-yl]acetyl]amino]-3-pyridin-3-ylpropanoic acidIC501.2 [1]
3-[4-(7-Amino-heptyloxy)-phenyl]-2-benzyloxycarbonylamino-propionic acidIC50147000.0 [1], 315000.0 [2]
2-[(2S,5R,8S,11S,14S)-5-Benzyl-11-[3-(diaminomethylideneamino)propyl]-14-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acidIC50100000.0 [1]
CID 11452690IC500.24 [1]
(3S)-3-(6-Methoxypyridin-3-yl)-9-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)nonanoic acidIC500.65 [1]
Ac-Asp-Arg-Leu-Asp-Ser-OHIC5025.0 [1]
(2S)-5-Oxo-2-(phenylmethoxycarbonylamino)-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acidIC500.06 [1], 3.26 [2]
2-Benzyloxycarbonylamino-3-[4-(3-tert-butylamino-2-hydroxy-propoxy)-phenyl]-propionic acidIC50300000.0 [1]
3-[4-[4-[[(4-Methylpyridin-2-yl)amino]methyl]piperidin-1-yl]phenyl]-2-[(2,4,6-trimethylbenzoyl)amino]propanoic acidIC5084.0 [1]
(2S)-3-[[2-[(3R,5S)-1-Phenylmethoxycarbonyl-5-[(pyridin-2-ylamino)methyl]pyrrolidin-3-yl]oxyacetyl]amino]-2-[(2,4,6-trimethylbenzoyl)amino]propanoic acidIC501200.0 [1], 30000.0 [2]
(2S)-2-[(2,6-Dichlorobenzoyl)amino]-3-[4-[3-(pyridin-2-ylamino)propoxy]phenyl]propanoic acidIC5084.0 [1], 2600.0 [2]
(2S)-2-[(2,6-Dichlorobenzoyl)amino]-3-[4-[2-[6-(methylamino)pyridin-2-yl]ethoxy]phenyl]propanoic acidIC507.0 [1], 230.0 [2]
3-[[1-(4-Aminobutyl)-4-methyl-6-oxo-2-phenyl-2,3-dihydropyridin-5-yl]-propylamino]-3-oxopropanoic acidIC5038.0 [1]
(2S)-3-[4-[3-(Diaminomethylideneamino)phenyl]phenyl]-2-[(2,4,6-trimethylphenyl)sulfonylamino]propanoic acidKi11.0 [1]
3-Pyrimidin-5-yl-3-[5-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)pentanoylamino]propanoic acidIC503.3 [1]
3-(1,3-Benzodioxol-5-yl)-3-[[1-[3-[[N'-(pyridin-4-ylmethyl)carbamimidoyl]amino]benzoyl]piperidine-4-carbonyl]amino]propanoic acidIC5025.3 [1]
3-[[1-[(4-Aminophenyl)methyl]-4-methyl-6-oxo-2-phenyl-2,3-dihydropyridin-5-yl]-propylamino]-3-oxopropanoic acidIC50600.0 [1]
(2S)-2-(Benzenesulfonamido)-3-[[4-[(3S)-3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)piperidin-1-yl]benzoyl]amino]propanoic acidIC500.48 [1], 31.0 [2]
3-({[2-(3-{[(E)-Amino(imino)methyl]amino}benzoyl)hydrazino]carbonyl}amino)-3-phenylpropanoic acidIC500.8 [1], 2.6 [2]
(3S)-3-(3-Bromo-5-chloro-2-hydroxyphenyl)-3-[[2-[[5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]pyridine-3-carbonyl]amino]acetyl]amino]propanoic acidIC500.4 [1]
3-(2-Methylpyrimidin-5-yl)-4-[1-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propanoyl]piperidin-4-yl]butanoic acidIC500.7 [1]
(3S)-3-(3-Bromo-5-chloro-2-hydroxyphenyl)-3-[[2-[[3-hydroxy-5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]benzoyl]amino]acetyl]amino]propanoic acidIC501.6 [1], 2.6 [2]
(2S)-2-(Benzenesulfonamido)-3-[[3-fluoro-4-[4-(1,4,5,6-tetrahydropyrimidin-2-ylamino)piperidin-1-yl]benzoyl]amino]propanoic acidIC500.36 [1], 48.0 [2]
3-{5-[3-(Pyridin-2-ylamino)-propoxy]-indol-1-yl}-propionic acidIC50470.0 [1]
3-{5-[2-(6-Methylamino-pyridin-2-yl)-ethoxy]-indol-1-yl}-propionic acidIC5036.0 [1], 49.0 [2]
2-[(4S)-3-Oxo-8-[3-(pyridin-2-ylamino)propoxy]-2-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-2-benzazepin-4-yl]acetic acidIC5012.0 [1]
2-[(4S)-3-Oxo-8-[3-(pyridin-2-ylamino)propoxy]-2-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-2-benzazepin-4-yl]acetic acidKi0.9 [1]
(2S)-3-[4-[3-(Cyclopropylcarbamoylamino)phenyl]phenyl]-2-[(2,4,6-trimethylphenyl)sulfonylamino]propanoic acidKi2.5 [1]
3-(1,3-Benzodioxol-5-yl)-4-[3-[2-(1-methyl-3,4-dihydro-2H-pyrido[2,3-b]pyrazin-6-yl)ethoxy]-1,2-oxazol-5-yl]butanoic acidIC500.69 [1], 1.2 [2]
3-(1,3-Benzodioxol-5-yl)-4-[3-[3-[6-(methylamino)pyridin-2-yl]propyl]-1,2,4-oxadiazol-5-yl]butanoic acidIC502.1 [1], 3.2 [2]
3-(1,3-Benzoxazol-6-yl)-4-[3-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]-1,2,4-oxadiazol-5-yl]butanoic acidIC500.32 [1], 0.5 [2]
3-[2-(4-Chlorophenyl)-1,3-thiazol-5-yl]-4-[1-methyl-5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]pyrazol-3-yl]butanoic acidIC500.9 [1], 1.4 [2]
3-(1,3-Benzodioxol-5-yl)-4-[1-phenyl-5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]pyrazol-3-yl]butanoic acidIC501.18 [1], 1.4 [2]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Integrin alpha-V/beta-3 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 9 May. 2024, https://www.aatbio.com/data-sets/integrin-alpha-v-beta-3-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 9). Quest Database™ Integrin alpha-V/beta-3 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/integrin-alpha-v-beta-3-inhibitors-ic50-ki.
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