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

Structure
Compound Name
Standard Type
Standard Values (in nM)
TirofibanIC5010.0 [1]
Arg-gly-asp-serIC5022700.0 [1]
3-[2-(4-Carbamimidoylbenzoyl)imino-3,4-dimethyl-1,3-thiazol-5-yl]propanoic acidIC5016.8 [1], 20.8 [2], 35.5 [3], 36.6 [4], 100000.0 [5]
3-[2-(4-Carbamimidoylbenzoyl)imino-3,4-dimethyl-1,3-thiazol-5-yl]propanoic acidKi0.05 [1]
Arginyl-glycyl-aspartic acidIC5010000.0 [1]
OrbofibanIC50130.0 [1]
3-[[2-[3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]propanoic acid;2,2,2-trifluoroacetic acidIC5060.0 [1]
2-[2-[2-(4-Carbamimidoylphenyl)-1-oxo-2,8-diazaspiro[4.5]decan-8-yl]-2-oxoethoxy]acetic acidIC50273.0 [1]
5-[2-(4-Carbamimidoylphenyl)-1-oxo-2,8-diazaspiro[4.5]decan-8-yl]-5-oxopentanoic acidIC50168.0 [1]
SibrafibanIC5051.0 [1]
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 acidIC5090.0 [1]
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 acidKi2.0 [1], 2.8 [2], 4.0 [3], 4.5 [4]
Acetyl-arginyl-glycyl-aspartyl-serinamideIC5067200.0 [1], 91300.0 [2]
Acetyl-arginyl-glycyl-aspartyl-serinamideKi4200.0 [1], 37010.0 [2], 62000.0 [3]
2-[(4R,7S,13S,16R)-16-Acetamido-4-carbamoyl-13-[3-(diaminomethylideneamino)propyl]-14-methyl-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadec-7-yl]acetic acidIC502.8 [1], 90.0 [2], 230.0 [3], 360.0 [4], 480.0 [5]
2-[(4R,7S,13S,16R)-16-Acetamido-4-carbamoyl-13-[3-(diaminomethylideneamino)propyl]-14-methyl-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadec-7-yl]acetic acidKi175.0 [1]
CilengitideIC50590.0 [1], 1000.0 [2], 4208.0 [3], 206000.0 [4], 244000.0 [5]
Arginyl-glycyl-aspartyl-phenylalanineIC5031.0 [1], 9000.0 [2], 40000.0 [3], 43000.0 [4], 725000.0 [5]
(2S)-2-(Butoxycarbonylamino)-3-[[2-[(5R)-3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]propanoic acidIC500.25 [1], 21.0 [2], 50.0 [3], 60.0 [4], 66.0 [5]
2-[(2S)-7-[1H-Benzimidazol-2-ylmethyl(methyl)carbamoyl]-4-methyl-3-oxo-2,5-dihydro-1H-1,4-benzodiazepin-2-yl]acetic acidKi30000.0 [1]
3-[[2-[3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]propanoic acidIC501.1 [1], 140.0 [2], 240.0 [3], 560.0 [4]
3-[[3-Oxo-2-(2-piperidin-4-ylethyl)-1H-isoindole-5-carbonyl]amino]propanoic acidIC5025.0 [1], 27.0 [2], 25000.0 [3]
KlervalIC5028.0 [1], 97.0 [2], 2350000.0 [3], 2400000.0 [4]
1-Oxo-6-[(4-amidinobenzoyl)amino]-3,4-dihydroisoquinoline-2(1H)-acetic acidIC503.0 [1], 76.0 [2], 90.0 [3]
(3S)-4-[[(1R)-1-Carboxy-3-cyclohexylpropyl]amino]-3-[[2-[ethyl(4-piperidin-4-ylbutanoyl)amino]acetyl]amino]-4-oxobutanoic acidIC5011.0 [1], 31.0 [2], 1930000.0 [3], 2400000.0 [4], 2500000.0 [5]
3-[[2-(4-Carbamimidoylphenyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carbonyl]amino]propanoic acidIC503.9 [1], 53.0 [2], 110.0 [3], 120.0 [4], 365.0 [5]
(3S)-4-[[(1S)-1-Carboxy-2-cyclohexylethyl]amino]-3-[[2-[ethyl(4-piperidin-4-ylbutanoyl)amino]acetyl]amino]-4-oxobutanoic acidIC5017.0 [1], 26.0 [2], 1012000.0 [3], 1650000.0 [4], 1750000.0 [5]
3-[6-[(4-Carbamimidoylphenyl)methoxy]-1-oxo-3,4-dihydroisoquinolin-2-yl]-6-ethoxyhexanoic acidIC5061.0 [1], 73.0 [2], 100.0 [3], 470.0 [4]
3-[6-[(4-Carbamimidoylphenyl)methoxy]-1-oxo-3,4-dihydroisoquinolin-2-yl]octanoic acidIC5024.0 [1], 40.0 [2], 100.0 [3], 570.0 [4]
3-[6-[(4-Carbamimidoylphenyl)methoxy]-1-oxo-3,4-dihydroisoquinolin-2-yl]nonanoic acidIC5041.0 [1], 80.0 [2], 310.0 [3], 3000.0 [4]
((4-(4-Amidinophenoxy)butanoyl)aspartyl)valineIC5088.0 [1], 100.0 [2], 103.0 [3], 109.65 [4]
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 acidIC501200.0 [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 acidKi9000.0 [1]
4-(4-Amidinobenzoylglycyl)-3-methoxycarbonyl-2-oxopiperazine-1-acetic acidIC500.49 [1], 30.0 [2], 38.0 [3], 53.0 [4]
2-Benzenesulfonylamino-3-[4-(2-piperidin-4-yl-ethoxy)-benzoylamino]-propionic acidIC500.81 [1], 10.0 [2], 13.0 [3]
2-[8-[(4-Carbamimidoylphenyl)-methylcarbamoyl]-3-oxo-4-(2-phenylethyl)-2,5-dihydro-1H-1,4-benzodiazepin-2-yl]acetic acidIC5065.0 [1]
2-[8-[(4-Carbamimidoylphenyl)-methylcarbamoyl]-3-oxo-4-(2-phenylethyl)-2,5-dihydro-1H-1,4-benzodiazepin-2-yl]acetic acidKi1.6 [1]
2-[8-[(4-Carbamimidoylphenyl)carbamoyl]-3-oxo-4-(2-phenylethyl)-2,5-dihydro-1H-1,4-benzodiazepin-2-yl]acetic acidKi2.3 [1], 2.8 [2]
2-[(5S,11S,14S)-11-[3-(Diaminomethylideneamino)propyl]-14-ethyl-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-1(21),17,19-trien-5-yl]acetic acidIC502.3 [1], 20.0 [2], 46.0 [3]
2-[(5S,11S,14S)-11-[3-(Diaminomethylideneamino)propyl]-14-ethyl-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-1(21),17,19-trien-5-yl]acetic acidKi0.1 [1]
(3S)-3-[[2-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-4-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acidIC5027000.0 [1], 32000.0 [2], 55500.0 [3]
(3S)-3-[[2-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-4-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acidKi10000.0 [1]
1-Oxo-6-[(4-amidinobenzyl)oxy]-3,4-dihydroisoquinoline-2(1H)-acetic acidIC50600.0 [1], 30000.0 [2]
3-[7-[2-(4-Carbamimidoylphenyl)ethynyl]-1-methyl-2,5-dioxo-3H-1,4-benzodiazepin-4-yl]propanoic acidIC5011.0 [1], 120.0 [2], 213.0 [3]
3-[3-(2,3-Dihydro-1H-isoindol-5-ylcarbamoyl)-propionylamino]-3-phenyl-propionic acid; hydrochlorideIC508.3 [1], 270.0 [2], 860.0 [3]
3-[3-(2,3-Dihydro-1H-isoindol-5-ylcarbamoyl)-propionylamino]-3-phenyl-propionic acid; hydrochlorideKi4.2 [1]
3-[3-(2,3-Dihydro-1H-isoindol-5-ylcarbamoyl)-propionylamino]-propionic acid; hydrochlorideIC5010.0 [1], 2090.0 [2], 2750.0 [3]
3-[3-(2,3-Dihydro-1H-isoindol-5-ylcarbamoyl)-propionylamino]-propionic acid; hydrochlorideKi7.1 [1]
2-[1-[2-[3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]piperidin-2-yl]acetic acid;2,2,2-trifluoroacetic acidIC50280.0 [1], 100000.0 [2], 5800000.0 [3], 9800000.0 [4]
3-[[2-[3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]-2-(dibutoxyphosphorylamino)propanoic acidIC501.2 [1], 55.0 [2], 114.0 [3], 221.0 [4]
2-[Bis(prop-2-enoxy)phosphorylamino]-3-[[2-[3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]propanoic acidIC501.5 [1], 46.0 [2], 122.0 [3], 224.0 [4]
3-[[2-[3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]-2-(diethoxyphosphorylamino)propanoic acidIC501.7 [1], 102.0 [2], 117.0 [3], 240.0 [4]
3-[[2-[3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]-2-[di(propan-2-yloxy)phosphorylamino]propanoic acidIC500.86 [1], 73.0 [2], 103.0 [3], 210.0 [4]
3-[[2-[3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]-2-(dimethoxyphosphorylamino)propanoic acidIC500.55 [1], 54.0 [2], 105.0 [3], 197.0 [4]
3-[[2-[3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]-2-(phosphonoamino)propanoic acidIC502.6 [1], 229.0 [2], 260.0 [3], 376.0 [4]
2-(Benzenesulfonamido)-3-[6-[(4-carbamimidoylphenyl)methoxy]naphthalen-2-yl]propanoic acidIC50840.0 [1], 22900.0 [2], 23600.0 [3], 27700.0 [4]
2-(Benzenesulfonamido)-3-[6-(3-piperazin-1-ylpropoxy)naphthalen-2-yl]propanoic acidIC50180.0 [1], 530.0 [2], 1010.0 [3], 1320.0 [4]
Gly-arg-gly-asp-serIC50120.0 [1], 133.0 [2], 160000.0 [3]
Arginyl-glycyl-aspartyl-valineIC506000.0 [1], 10000.0 [2]
Butanoic acid, 3-((2-((3R)-2-oxo-3-(2-(4-piperidinyl)ethyl)-1-piperidinyl)acetyl)amino)-, (3R)-IC505.0 [1], 23.0 [2], 32.0 [3]
2-[2-(Carboxymethoxy)-4-[2-(4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonylamino)acetyl]phenoxy]acetic acidIC505.6 [1], 28.0 [2], 100000.0 [3]
ElarofibanIC500.06 [1], 0.15 [2], 0.36 [3]
Xemilofiban acidIC5035.0 [1], 67.0 [2]
2-[4-[2-[(4-Carbamimidoylbenzoyl)-methylamino]acetyl]-2-(carboxymethoxy)phenoxy]acetic acidIC500.4 [1], 1.0 [2], 70.0 [3]
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 acidIC5010000.0 [1]
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 acidKi3800.0 [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 acidIC503000.0 [1], 10000.0 [2]
N-{3-[5-Oxo-7-(Piperazin-1-Yl)-5h-[1,3,4]thiadiazolo[3,2-A]pyrimidin-2-Yl]phenyl}glycinamideIC5095.0 [1], 96.0 [2]
2-Ethyl-7-Piperazin-1-Yl-5h-[1,3,4]thiadiazolo[3,2-A]pyrimidin-5-OneIC509600.0 [1], 9700.0 [2], 13000.0 [3]
[6-(4-Carbamimidoyl-benzoylamino)-chroman-2-yl]-acetic acidIC502.0 [1], 190.0 [2]
3-[[2-[(5R)-3-(4-Carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]propanoic acidIC5060.0 [1], 140.0 [2], 240.0 [3]
(2S)-2-(Benzenesulfonamido)-3-[(4-piperazin-1-ylbenzoyl)amino]propanoic acidIC5016.0 [1], 17.0 [2]
1-Oxo-6-[(4-amidinobenzoyl)amino]tetralin-2-acetic acidIC502.0 [1], 60.0 [2]
(3S)-3-Pyridin-3-yl-3-[[2-[4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)butanoylamino]acetyl]amino]propanoic acidIC503000.0 [1], 10000.0 [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 acidIC5061000.0 [1], 100000.0 [2]
(2S)-2-(Benzenesulfonamido)-3-[3-[(5-carbamimidoyl-1-benzofuran-2-carbonyl)amino]propanoylamino]propanoic acidIC501.8 [1], 35.0 [2]
2-[(4S,7S,13R,16S)-16-Acetamido-4-carbamoyl-13-[3-(diaminomethylideneamino)propyl]-3,3-dimethyl-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadec-7-yl]acetic acidIC50200000.0 [1]
2-[(4S,7S,13R,16S)-16-Acetamido-4-carbamoyl-13-[3-(diaminomethylideneamino)propyl]-3,3-dimethyl-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadec-7-yl]acetic acidKi720.0 [1], 1000000.0 [2]
2-[(4S,7R,13R,16S)-16-Acetamido-4-carbamoyl-13-[3-(diaminomethylideneamino)propyl]-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadec-7-yl]acetic acidIC5016200.0 [1]
2-[(4S,7R,13R,16S)-16-Acetamido-4-carbamoyl-13-[3-(diaminomethylideneamino)propyl]-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadec-7-yl]acetic acidKi780.0 [1]
N-[3-(Propylamino)propyl]-5-(trifluoromethyl)-1-[4-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrazole-4-carboxamideIC503500.0 [1], 4100.0 [2], 10000.0 [3]
6-[[(5-Amidino-1H-indol-2-yl)carbonyl]amino]hexanoic acidIC5030000.0 [1], 100000.0 [2]
7-[[(5-Amidino-1H-indol-2-yl)carbonyl]amino]heptanoic acidIC50680.0 [1], 700.0 [2], 2800.0 [3]
N-[3-(Diethylamino)propyl]-5-(trifluoromethyl)-1-[4-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrazole-4-carboxamideIC50400.0 [1], 2500.0 [2], 4100.0 [3]
(3S)-3-[7-[2-(4-Carbamimidoylphenyl)ethynyl]-9-chloro-1-methyl-2,5-dioxo-3H-1,4-benzodiazepin-4-yl]butanoic acidIC507.0 [1], 159.0 [2], 313.0 [3]
7-[[(6-Amidino-1H-indol-3-yl)carbonyl]amino]heptanoic acidIC50100.0 [1], 650.0 [2]
N-(3-Piperidin-1-ylpropyl)-5-(trifluoromethyl)-1-[4-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrazole-4-carboxamideIC503000.0 [1], 12000.0 [2], 30000.0 [3]
7-[[(6-Amidino-1H-indol-2-yl)carbonyl]amino]heptanoic acidIC50150.0 [1], 1300.0 [2]
(3S)-3-[1-Tert-butyl-7-[2-(4-carbamimidoylphenyl)ethynyl]-9-chloro-2,5-dioxo-3H-1,4-benzodiazepin-4-yl]butanoic acidIC5060.0 [1], 140.0 [2], 1500.0 [3]
2-Oxo-4-[[[(4-amidinophenyl)carbonyl]amino]acetyl]piperazine-1-acetic acidIC500.42 [1], 94.0 [2], 210.0 [3]
2-Oxo-4-[[[4-(2-aminoethyl)benzoyl]amino]acetyl]piperazine-1-acetic acidIC501.6 [1], 150.0 [2], 180.0 [3]
2-[(3S)-4-[2-[[4-[2-(Dimethylamino)ethyl]benzoyl]amino]acetyl]-3-(3-methoxy-3-oxopropyl)-2-oxopiperazin-1-yl]acetic acidIC5037.0 [1], 2300.0 [2], 7300.0 [3]
{(S)-4-Carboxymethyl-1-[2-(4-guanidino-benzoylamino)-acetyl]-3-oxo-piperazin-2-yl}-acetic acidIC504.8 [1], 340.0 [2], 350.0 [3]
(3S)-3-[1-Tert-butyl-7-[2-(4-carbamimidoylphenyl)ethynyl]-2,5-dioxo-3H-1,4-benzodiazepin-4-yl]butanoic acidIC503.0 [1], 12.0 [2], 92.0 [3]
3-[(2S)-4-(Carboxymethyl)-1-[2-[[4-[2-(dimethylamino)ethyl]benzoyl]amino]acetyl]-3-oxopiperazin-2-yl]propanoic acidIC5045.0 [1], 2500.0 [2], 4200.0 [3]
{(S)-4-[2-(4-Carbamimidoyl-benzoylamino)-acetyl]-3-carbamoylmethyl-2-oxo-piperazin-1-yl}-acetic acidIC500.92 [1], 110.0 [2], 740.0 [3]
{(S)-1-[2-(3-Carbamimidoyl-benzoylamino)-acetyl]-4-carboxymethyl-3-oxo-piperazin-2-yl}-acetic acidIC50130.0 [1], 13000.0 [2], 16000.0 [3]
2-[(2S)-1-[2-[[2-(4-Carbamimidoylphenyl)acetyl]amino]acetyl]-4-(carboxymethyl)-3-oxopiperazin-2-yl]acetic acidIC508.1 [1], 1200.0 [2], 1600.0 [3]
2-[(2S)-1-[2-[[4-(3-Aminopropyl)benzoyl]amino]acetyl]-4-(carboxymethyl)-3-oxopiperazin-2-yl]acetic acidIC5015.0 [1], 1030.0 [2], 1100.0 [3]
8-[[(5-Amidino-1H-indol-3-yl)carbonyl]amino]octanoic acidIC50100000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Integrin alpha-IIb/beta-3 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/integrin-alpha-iib-beta-3-inhibitors-ic50-ki.

APA

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