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ADAM17 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
(2R)-N-Hydroxy-2-[(4-methoxyphenyl)sulfonyl-(pyridin-3-ylmethyl)amino]-3-methylbutanamide;hydrochlorideIC50750.0 [1]
[(R)-3-(Hydroxycarbamoyl)-3-[4-(2-butynyloxy)phenylsulfonylamino]propyl]carbamic acid benzyl esterIC50260.0 [1]
(2R)-2-[(4-But-2-ynoxyphenyl)sulfonylamino]-4-(1,3-dioxoisoindol-2-yl)-N-hydroxybutanamideIC50280.0 [1]
Benzyl N-[(4R)-4-[[4-[(3,5-dibromophenyl)methoxy]phenyl]sulfonylamino]-5-(hydroxyamino)-5-oxopentyl]carbamateIC50349.0 [1]
MarimastatIC503.8 [1], 4100.0 [2], 7000.0 [3], 10000.0 [4]
MarimastatKi0.4 [1], 6.3 [2]
ApratastatIC5020.0 [1]
2-[[4-[(3,5-Dibromophenyl)methoxy]phenyl]sulfonylamino]-N-hydroxyacetamideIC5010000.0 [1]
Benzyl N-[(3R)-3-[[4-[(3,5-dibromophenyl)methoxy]phenyl]sulfonylamino]-4-(hydroxyamino)-4-oxobutyl]carbamateIC502096.0 [1]
(2R)-5-(Carbamoylamino)-2-[[4-[(3,5-dibromophenyl)methoxy]phenyl]sulfonylamino]-N-hydroxypentanamideIC5058.0 [1]
4-[(4-But-2-ynoxyphenyl)sulfonylmethyl]-N-hydroxy-1-propan-2-ylsulfonylpiperidine-4-carboxamideIC501.5 [1]
4-[4-(4-Chloro-phenoxy)-benzenesulfonylmethyl]-tetrahydro-pyran-4-carboxylic acid hydroxyamideIC5014.0 [1], 176.0 [2], 440.0 [3]
CID 6914621IC500.35 [1], 0.56 [2], 1.0 [3]
CID 6914621Ki0.06 [1]
(3S)-4-{[4-(But-2-ynyloxy)phenyl]sulfonyl}-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamideIC508.0 [1], 8.4 [2], 300.0 [3]
N-(3-Methoxybenzyl)-4-Oxo-3,4-Dihydroquinazoline-2-CarboxamideIC5010000.0 [1]
(2R,3R,4R,5S)-N,3,4,5-Tetrahydroxy-1-(4-phenoxyphenyl)sulfonylpiperidine-2-carboxamideIC50350.0 [1]
(2R,3R,4R,5S)-N,3,4,5-Tetrahydroxy-1-(4-phenoxyphenyl)sulfonylpiperidine-2-carboxamideKi2.3 [1]
(7S,8R,11S)-11-Benzoyl-8-[3-(3,5-dibromophenyl)propyl]-N-hydroxy-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7-carboxamideIC5079.43 [1], 87.0 [2], 5000.0 [3], 5011.87 [4]
(7S,8R,11S)-11-Benzoyl-8-[3-(3,5-dimethoxyphenyl)propyl]-N-hydroxy-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7-carboxamideIC5039.81 [1], 43.0 [2], 2900.0 [3], 3162.28 [4]
(7S,8R,11S)-7-N-Hydroxy-11-N-methyl-8-[3-(3-methyl-5-propan-2-ylphenyl)propyl]-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamideIC5012.0 [1], 12.59 [2], 199.53 [3], 220.0 [4]
(3S)-N-Hydroxy-2,2-dimethyl-4-[4-(3,4,5-trimethoxyphenoxy)phenyl]sulfonylthiomorpholine-3-carboxamideIC501.5 [1], 1.58 [2], 501.19 [3], 550.0 [4]
(7S,8R,11S)-8-[3-(2,5-Dimethoxyphenyl)propyl]-7-N-hydroxy-11-N-methyl-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamideIC506.31 [1], 6.8 [2], 3981.07 [3], 4100.0 [4]
(7S,8R,11S)-8-[3-(4-Ethoxyphenyl)propyl]-7-N-hydroxy-11-N-methyl-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamideIC502.51 [1], 2.7 [2], 398.11 [3], 400.0 [4]
(7S,8R,11S)-8-[3-(4-Chlorophenyl)propyl]-7-N-hydroxy-11-N-methyl-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamideIC503.16 [1], 3.4 [2], 398.11 [3], 440.0 [4]
(7S,8R,11S)-7-N-Hydroxy-11-N-methyl-9-oxo-8-[3-(3,4,5-trimethoxyphenyl)propyl]-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamideIC507.6 [1], 7.94 [2], 125.89 [3], 140.0 [4]
(7S,8R,11S)-8-[3-(3,4-Dimethoxyphenyl)propyl]-7-N-hydroxy-11-N-methyl-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamideIC505.01 [1], 5.2 [2], 180.0 [3], 199.53 [4]
(7S,8R,11S)-8-[3-[3,5-Bis(trifluoromethyl)phenyl]propyl]-7-N-hydroxy-11-N-methyl-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamideIC5031.62 [1], 33.0 [2], 300.0 [3], 316.23 [4]
(7S,8R,11S)-11-Benzoyl-N-hydroxy-9-oxo-8-[3-(3,4,5-trimethoxyphenyl)propyl]-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7-carboxamideIC5050.12 [1], 55.0 [2], 3162.28 [3], 3500.0 [4]
(7S,8R,11S)-7-N-Hydroxy-11-N-methyl-8-(3-naphthalen-1-ylpropyl)-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamideIC506.0 [1], 6.31 [2], 398.11 [3], 440.0 [4]
(2S,3R)-N-[(2S)-3,3-Dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N'-hydroxy-3-(hydroxymethyl)-2-(4-methoxyphenyl)butanediamideIC5048.0 [1], 56.0 [2]
(2S,3R)-N-[(2S)-3,3-Dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N'-hydroxy-3-(hydroxymethyl)-2-(4-methoxyphenyl)butanediamideKi0.6 [1]
(7S,8R,11S)-11-Benzoyl-N-hydroxy-8-[3-(4-methylphenyl)propyl]-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7-carboxamideIC5096.0 [1], 100.0 [2], 5000.0 [3], 5011.87 [4]
(7S,8R,11S)-11-Benzoyl-N-hydroxy-8-[3-[3-methoxy-5-(2-methoxyethoxy)phenyl]propyl]-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7-carboxamideIC5074.0 [1], 79.43 [2], 15000.0 [3], 15848.93 [4]
(3S)-N-Hydroxy-2,2-dimethyl-4-(4-pyridin-3-yloxyphenyl)sulfonylthiomorpholine-3-carboxamideIC507.9 [1], 7.94 [2], 7943.28 [3], 8600.0 [4]
2-Methyl-3-[4-(3,4,5-trimethoxyphenoxy)phenylsulfonyl]propanehydroximic acidIC506.31 [1], 6.5 [2], 39810.72 [3], 41000.0 [4]
PrinomastatIC505.5 [1], 22.0 [2], 16600.0 [3]
N^2^-[(2R)-2-{(1S)-1-[Formyl(hydroxy)amino]ethyl}-5-phenylpentanoyl]-N,3-dimethyl-L-valinamideIC50860.0 [1], 10000.0 [2]
(R)-N1-((S)-3,3-Dimethyl-1-(methylamino)-1-oxobutan-2-yl)-N4-hydroxy-2-isobutylsuccinamideIC5020.0 [1], 50000.0 [2]
(R)-N1-((S)-3,3-Dimethyl-1-(methylamino)-1-oxobutan-2-yl)-N4-hydroxy-2-isobutylsuccinamideKi87.0 [1]
CipemastatIC50230.3 [1], 10000.0 [2]
CipemastatKi230.0 [1]
(2R,3R)-1-[4-[(2-Chloro-4-fluorophenyl)methoxy]phenyl]sulfonyl-N,3-dihydroxy-3-methylpiperidine-2-carboxamideIC501.6 [1], 7.0 [2], 10000.0 [3]
(1R,2S)-2-N-Hydroxy-1-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]methyl]cyclopropane-1,2-dicarboxamideKi3.0 [1]
(2R,3R,4R,5R)-1-(4-But-2-ynoxyphenyl)sulfonyl-N,3,4,5-tetrahydroxypiperidine-2-carboxamideIC5028.0 [1]
(2R,3R,4R,5R)-1-(4-But-2-ynoxyphenyl)sulfonyl-N,3,4,5-tetrahydroxypiperidine-2-carboxamideKi0.53 [1]
2-Benzyl-N-hydroxy-3-(6-methyl-2-oxo-2H-chromen-3-yl)-propionamideIC500.5 [1], 5.0 [2], 520.0 [3]
Tert-butyl 4-[(4-but-2-ynoxyphenyl)sulfonylmethyl]-4-(hydroxycarbamoyl)piperidine-1-carboxylateIC502.0 [1], 14000.0 [2]
(5S)-5-Furo[3,2-b]pyridin-2-yl-5-[(5-methoxy-3-oxo-1H-isoindol-2-yl)methyl]imidazolidine-2,4-dioneIC50287.0 [1]
(5S)-5-Furo[3,2-b]pyridin-2-yl-5-[(5-methoxy-3-oxo-1H-isoindol-2-yl)methyl]imidazolidine-2,4-dioneKi0.5 [1]
Methyl (5R)-5-[7-[(3,5-diethoxyphenyl)methoxy]-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]-6-(hydroxyamino)-6-oxohexanoateIC501100.0 [1], 24000.0 [2]
Methyl (5R)-5-[7-[(3,5-diethoxyphenyl)methoxy]-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]-6-(hydroxyamino)-6-oxohexanoateKi13.0 [1]
(2R)-N-Hydroxy-2-[7-(4-nitrophenoxy)-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]propanamideIC501200.0 [1], 15000.0 [2]
(2R)-N-Hydroxy-2-[7-(4-nitrophenoxy)-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]propanamideKi11.0 [1]
(2R)-2-[7-[(3,5-Dimethoxyphenyl)methoxy]-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]-N-hydroxypropanamideIC50770.0 [1], 28000.0 [2]
(2R)-2-[7-[(3,5-Dimethoxyphenyl)methoxy]-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]-N-hydroxypropanamideKi27.0 [1]
(4s)-3-{[4-(4-Cyano-2-Methylphenyl)piperazin-1-Yl]sulfonyl}-N-Hydroxy-1,3-Thiazolidine-4-CarboxamideIC501500.0 [1], 10000.0 [2], 12000.0 [3]
(2R)-N-Hydroxy-2-[7-(3-nitrophenoxy)-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]propanamideIC50470.0 [1], 1400.0 [2]
(2R)-N-Hydroxy-2-[7-(3-nitrophenoxy)-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]propanamideKi129.0 [1]
(5S)-4-[2-(1-Adamantyl)ethyl]-5-[(4-hydroxyphenyl)methyl]-1-[(2R)-1-[(2S)-2-[[(6R)-6-[(4-hydroxyphenyl)methyl]-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-naphthalen-2-ylpropan-2-yl]piperazine-2,3-dioneIC501900.0 [1], 4200.0 [2], 100000.0 [3]
Benzyl N-[(4R)-4-[[4-(4-cyano-2-methylphenyl)piperazin-1-yl]sulfonylamino]-5-(hydroxyamino)-5-oxopentyl]carbamateIC5090.0 [1], 1000.0 [2]
N-Hydroxy-3-[methyl-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]-1-(2-methylpropanoyl)azetidine-3-carboxamideIC503.0 [1], 4.0 [2], 9.0 [3]
N-Hydroxy-1-(3-methylbutanoyl)-3-[methyl-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]azetidine-3-carboxamideIC507.0 [1], 20.0 [2], 33.0 [3]
(2R)-2-[7-[(3,5-Dimethoxyphenyl)methoxy]-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]-N-hydroxy-6-(methanesulfonamido)hexanamideIC501900.0 [1], 38000.0 [2]
(2R)-2-[7-[(3,5-Dimethoxyphenyl)methoxy]-1,1-dioxo-4,5-dihydro-3H-1lambda6,2,5-benzothiadiazepin-2-yl]-N-hydroxy-6-(methanesulfonamido)hexanamideKi5.0 [1]
IlomastatIC507.5 [1], 13.1 [2]
BatimastatIC500.4 [1], 14.9 [2]
(2S,3R)-N-Hydroxy-N'-[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-prop-2-enylbutanediamideIC500.2 [1], 2300.0 [2]
CID 9847838IC500.2 [1], 12.0 [2]
N-Hydroxy-2-(N-isopropoxybiphenyl-4-ylsulfonamido)acetamideIC50100000.0 [1], 120000.0 [2]
Unii-Q56UE7E40YIC5014.0 [1], 1000.0 [2]
(2S,3R)-N-Hydroxy-N'-[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-(phenylsulfanylmethyl)butanediamideIC501.8 [1], 5300.0 [2]
n-Hydroxy-2-[(4-methoxy-benzenesulfonyl)-pyridin-3-ylmethyl-amino]-3-methyl-benzamideIC50231.0 [1]
cis-2-Aminocyclohexylcarbamoylphosphonic acidIC50100000.0 [1]
N-Hydroxy-2-[[4-(4-methoxyphenyl)phenyl]methyl]-1,1-dioxo-1,2-thiazolidine-3-carboxamideIC501000.0 [1]
N-Hydroxy-4-[(4-methoxyphenyl)sulfonyl-(pyridin-3-ylmethyl)amino]-8-phenylquinoline-3-carboxamideIC50120.0 [1]
5-Methyl-5-[4-(2-methyl-quinolin-4-ylmethoxy)-phenyl]-pyrimidine-2,4,6-trioneIC501.0 [1], 1030.0 [2]
(3R)-2-[Ethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamideIC50230.0 [1]
(3R)-2-[Ethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamideKi7.15 [1]
(2R,5R)-1-[4-[(2,4-Dichlorophenyl)methoxy]phenyl]sulfonyl-N,5-dihydroxy-3,3-dimethylpiperidine-2-carboxamideIC5019.0 [1], 20000.0 [2]
2-[Methyl(4-methoxyphenylsulfonyl)amino]-3-methyl-5-bromobenzohydroximic acidIC5032.0 [1]
4-[(4-But-2-ynoxyphenyl)sulfonyl-methylamino]-N-hydroxy-8-methoxyquinoline-3-carboxamideIC5017.0 [1]
2-[Methyl[4-(2-propynyloxy)phenylsulfonyl]amino]-3-methyl-5-bromobenzohydroximic acidIC5011.0 [1]
2-[Methyl[4-(2-butynyloxy)phenylsulfonyl]amino]acetohydroximic acidIC507.0 [1]
2-[Methyl[4-(2-butynyloxy)phenylsulfonyl]amino]acetohydroximic acidKi10.0 [1]
2-[4-(2-Butynyloxy)phenylsulfonylamino]acetohydroximic acidIC505.0 [1], 17.0 [2]
N-Hydroxy-4-[(4-methoxyphenyl)sulfonyl-(pyridin-3-ylmethyl)amino]-3-methyl-[1,2]oxazolo[5,4-b]pyridine-5-carboxamideIC50147.0 [1]
N-Hydroxy-2-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-1,1-dioxothiazinane-3-carboxamideIC503.7 [1]
1-Acetyl-4-(4-but-2-ynoxyphenyl)sulfonyl-N-hydroxy-8-(hydroxymethyl)-3,5-dihydro-2H-1,4-benzodiazepine-3-carboxamideIC5012.0 [1]
5-((5-Methoxy-3-oxo-1H-indazol-2(3H)-yl)methyl)-5-phenylimidazolidine-2,4-dioneKi6.0 [1]
(1S,2R)-N-Hydroxy-2-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]cyclopentane-1-carboxamideIC500.6 [1], 0.63 [2]
4-[2-[[6-Fluoro-2-[(3-methoxyphenyl)methylcarbamoyl]-4-oxo-3H-quinazolin-5-yl]oxy]ethyl]benzoic acidIC5010000.0 [1]
3-[2-[(E)-(4-Oxo-1,3-thiazolidin-2-ylidene)methyl]-4-pyridin-2-yl-1,3-thiazol-5-yl]propanoic acidIC5030000.0 [1]
(2R,4S)-N,4-Dihydroxy-1-(4-phenylmethoxyphenyl)sulfonylpiperidine-2-carboxamideIC509.0 [1]
N-Hydroxy-1-methyl-2-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylmethyl]pyrrolidine-3-carboxamideIC501.0 [1], 180.0 [2]
4-((4-(But-2-ynyloxy)phenylsulfonyl)methyl)-N-hydroxy-1-(pyridin-4-ylmethyl)piperidine-4-carboxamideIC502.1 [1]
1-Benzoyl-4-[(4-but-2-ynoxyphenyl)sulfonylmethyl]-N-hydroxypiperidine-4-carboxamideIC501.0 [1]
3-{[4-(But-2-Yn-1-Yloxy)phenyl]sulfonyl}propane-1-ThiolKi10.0 [1]
Methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1-carboxylateKi12.0 [1]
Methyl (1R,2S)-2-(hydroxycarbamoyl)-1-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]methyl]cyclopropane-1-carboxylateKi8.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ ADAM17 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/adam17-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). Quest Database™ ADAM17 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/adam17-inhibitors-ic50-ki.
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