Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T31902 | Target Info | |||
| Target Name | Mammalian disintegrin-metalloprotease (ADAM10) | ||||
| Synonyms |
Mammalian disintegrinmetalloprotease; MADM; Kuzbanian protein homolog; KUZ; Disintegrin and metalloproteinase domaincontaining protein 10; Disintegrin and metalloproteinase domain-containing protein 10; CDw156; CD156c; ADAM 10
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| Target Type | Clinical trial Target | ||||
| Gene Name | ADAM10 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 24 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
GRASSYSTATIN A
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Investigative | Compound Info | ||
| Synonyms |
Grassystatin A; CHEMBL567893; GTPL8674
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Grassystatin B
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL568553; BDBM50302109
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| Activity |
IC50 = 87200 nM
|
[1] | |||
| Compound Name |
(5S)-4-(1-Adamantylmethyl)-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-[(4-hydroxyphenyl)methyl]piperazine-2,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593357; BDBM50104637
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-(Cyclobutylmethyl)-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-[(4-hydroxyphenyl)methyl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593359; BDBM50104635
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5R)-4-[2-(1-Adamantyl)ethyl]-5-[(4-hydroxyphenyl)methyl]-1-[(2S)-1-(4-hydroxyphenyl)-3-[(2S)-2-[[(6R)-6-(naphthalen-2-ylmethyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl]propan-2-yl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593546; BDBM50104626
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-[2-(1-Adamantyl)ethyl]-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-(naphthalen-2-ylmethyl)piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593542; BDBM50104630
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-[2-(1-Adamantyl)ethyl]-5-butyl-1-[(2S)-1-(4-hydroxyphenyl)-3-[(2S)-2-[[(6R)-6-(naphthalen-2-ylmethyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl]propan-2-yl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593549; BDBM50104623
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
Schembl21751149
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3235912; BDBM50104619
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5R)-4-[2-(1-Adamantyl)ethyl]-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-(naphthalen-2-ylmethyl)piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593543; BDBM50104629
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-Dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-[(4-hydroxyphenyl)methyl]-4-(2-phenylbutyl)piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593360; BDBM50104634
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5R)-4-[2-(1-Adamantyl)ethyl]-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-[(4-hydroxyphenyl)methyl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593541; BDBM50104631
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(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-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593550; BDBM50104622
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-[2-(1-Adamantyl)ethyl]-5-butyl-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593544; BDBM50104628
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-5-Benzyl-1-[(2R)-1-[(2S)-2-[[(6R)-6-benzyl-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-cyclohexylpropan-2-yl]-4-(2-phenylethyl)piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593552; BDBM50104618
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5R)-4-[2-(1-Adamantyl)ethyl]-1-[(2S)-1-(4-hydroxyphenyl)-3-[(2S)-2-[[(6R)-6-(naphthalen-2-ylmethyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl]propan-2-yl]-5-(naphthalen-2-ylmethyl)piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593548; BDBM50104624
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
CID 78426619
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3235911; SCHEMBL20271444; BDBM50104621
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-5-Benzyl-1-[(2R)-1-cyclohexyl-3-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]propan-2-yl]-4-(2-phenylethyl)piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593551; BDBM50104620
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
Grassystatin C
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL569445; BDBM50302108
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(5S)-4-[2-(1-Adamantyl)ethyl]-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-[(4-hydroxyphenyl)methyl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593361; BDBM50104633
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-[2-(1-Adamantyl)ethyl]-1-[(2S)-1-(4-hydroxyphenyl)-3-[(2S)-2-[[(6R)-6-(naphthalen-2-ylmethyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl]propan-2-yl]-5-(naphthalen-2-ylmethyl)piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593547; BDBM50104625
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-[2-(1-Adamantyl)ethyl]-5-[(4-hydroxyphenyl)methyl]-1-[(2S)-1-(4-hydroxyphenyl)-3-[(2S)-2-[[(6R)-6-(naphthalen-2-ylmethyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl]propan-2-yl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593545; BDBM50104627
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-[(4-Tert-butylcyclohexyl)methyl]-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-[(4-hydroxyphenyl)methyl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593356; BDBM50104638
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-(Cyclopentylmethyl)-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-[(4-hydroxyphenyl)methyl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593362; BDBM50104632
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(5S)-4-(Cyclohexylmethyl)-1-[(2S)-1-[(2S)-2-[[(6S)-2,3-dioxo-6-propylpiperazin-1-yl]methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-[(4-hydroxyphenyl)methyl]piperazine-2,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3593358; BDBM50104636
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 7 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(1R,2S)-1-({3-Fluoro-4-[(2-phenylquinolin-4-yl)methoxy]phenyl}methyl)-2-N-hydroxycyclopropane-1,2-dicarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL461220; SCHEMBL13648029; BDBM26524; hydroxamate-cyclopropyl compound, 1
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| Activity |
Ki > 10000000 nM
|
[3] | |||
| Compound Name |
Hydroxamate deriv., 78
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Investigative | Compound Info | ||
| Synonyms |
BMCL1954 Compound 3; CHEMBL269834; SCHEMBL8357412; BDBM23487
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| Activity |
Ki > 10000000 nM
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[3] | |||
| Compound Name |
(1R,2S)-Ethyl 2-(hydroxycarbamoyl)-1-(4-((2-phenylquinolin-4-yl)methoxy)benzyl)cyclopropanecarboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL495555; SCHEMBL13648000; BDBM50292683
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| Activity |
Ki > 10000000 nM
|
[3] | |||
| Compound Name |
(1R,2S)-Ethyl 2-(hydroxycarbamoyl)-1-(4-((2-methylquinolin-4-yl)methoxy)benzyl)cyclopropanecarboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL497810; SCHEMBL13648009; BDBM50292684
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| Activity |
Ki > 10000000 nM
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[3] | |||
| Compound Name |
(1S,2R)-2-Cyano-N-hydroxy-2-(4-((2-phenylquinolin-4-yl)methoxy)benzyl)cyclopropanecarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL497769; BDBM50292680
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| Activity |
Ki > 10000000 nM
|
[3] | |||
| Compound Name |
(1R,2S)-1-(3-Fluoro-4-((2-phenylquinolin-4-yl)methoxy)benzyl)-N2-hydroxy-N1,N1-dimethylcyclopropane-1,2-dicarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL496309; SCHEMBL13648378; BDBM50292682
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| Activity |
Ki > 10000000 nM
|
[3] | |||
| Compound Name |
(1S,2R)-N-Hydroxy-2-((S)-2-(hydroxymethyl)pyrrolidine-1-carbonyl)-2-(4-((2-phenylquinolin-4-yl)methoxy)benzyl)cyclopropanecarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL506057; SCHEMBL13648344; BDBM50292681
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| Activity |
Ki > 10000000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47. | ||||
| REF 2 | SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes. J Med Chem. 2015 Aug 13;58(15):5808-24. | ||||
| REF 3 | Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5809-14. | ||||
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