Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T79570 | Target Info | |||
| Target Name | Aggrecanase-1 (ADAMTS4) | ||||
| Synonyms |
Aggrecanase 1; ADMP-1; ADAMTS4; ADAM-TS4; ADAM-TS 4; A disintegrin and metalloproteinase with thrombospondin motifs 4
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| Target Type | Patented-recorded Target | ||||
| Gene Name | ADAMTS4 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 9 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Biphenylsulfonamide carboxylate, 5
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL373058; BDBM24028; (2R)-3-methyl-2-{[4-(2-nitrophenyl)benzene]sulfonamido}butanoic acid
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
(2R)-3-Methyl-2-[[4-[4-(methylcarbamoyloxy)phenyl]phenyl]sulfonylamino]butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910447; SCHEMBL1655878; BDBM50356233
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| Activity |
IC50 = 50000 nM
|
[2] | |||
| Compound Name |
2-(4-Methoxyphenoxy)-N-((5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL472144; BDBM50256313; N-[(5-chloro-8-hydroxyquinolin-7-yl)-(4-methoxyphenyl)methyl]-2-(4-methoxyphenoxy)acetamide
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
(2R)-2-[[4-[4-(Cyclohexylmethoxy)phenyl]phenyl]sulfonylamino]-3-methylbutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910457; BDBM50356241
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| Activity |
IC50 ~ 75000 nM
|
[2] | |||
| Compound Name |
(2R)-2-[[4-(4-Acetamidophenyl)phenyl]sulfonylamino]-3-methylbutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910446; BDBM50356232
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| Activity |
IC50 = 100000 nM
|
[2] | |||
| Compound Name |
Biphenylsulfonamide carboxylate, 9
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL43147; BDBM24032; N-(biphenyl-4-ylsulfonyl)-l-valine; ZINC13803822; N-(1,1'-Biphenyl-4-ylsulfonyl)valine; (2S)-3-methyl-2-[(4-phenylbenzene)sulfonamido]butanoic acid
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Biphenylsulfonamide carboxylate, 3
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL199943; BDBM24026; N-(biphenyl-3-ylsulfonyl)-d-valine; (2R)-3-methyl-2-[(3-phenylbenzene)sulfonamido]butanoic acid
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Biphenylsulfonamide carboxylate, 10
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL199631; BDBM24033; 3-[(biphenyl-4-ylsulfonyl)amino]-4-methylpentanoic acid; 4-methyl-3-[(4-phenylbenzene)sulfonamido]pentanoic acid
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
(2R)-2-[[4-[4-(Benzamidomethyl)phenyl]phenyl]sulfonylamino]-3-methylbutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910451; BDBM50356236
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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, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(2R)-2-[[4-[3-(Acetamidomethyl)phenyl]phenyl]sulfonylamino]-3-methylbutanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910443; BDBM50356229
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| Activity |
IC50 > 200000 nM
|
[2] | |||
| Compound Name |
(2R)-2-[[4-[4-[[Acetyl(methyl)amino]methyl]phenyl]phenyl]sulfonylamino]-3-methylbutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910450; BDBM50356235
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| Activity |
IC50 > 200000 nM
|
[2] | |||
| Compound Name |
N-[(2s,4s)-1-({4-[2-(3,5-Dimethyl-1,2-Oxazol-4-Yl)ethyl]piperidin-1-Yl}sulfonyl)-4-(5-Fluoropyrimidin-2-Yl)-2-Methylpentan-2-Yl]-N-Hydroxyformamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1615187; 3q2h; BDBM50337735; Q27464726; QHF
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| Activity |
IC50 = 25118864.32 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors. Bioorg Med Chem Lett. 2006 Jan 15;16(2):311-6. | ||||
| REF 2 | Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6800-3. | ||||
| REF 3 | N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2). Bioorg Med Chem Lett. 2008 Dec 15;18(24):6454-7. | ||||
| REF 4 | Orally active achiral N-hydroxyformamide inhibitors of ADAM-TS4 (aggrecanase-1) and ADAM-TS5 (aggrecanase-2) for the treatment of osteoarthritis. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3301-6. | ||||
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