Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T97589 | Target Info | |||
| Target Name | Apoptosis signal-regulating kinase 1 (MAP3K5) | ||||
| Synonyms |
Mitogen-activated protein kinase kinase kinase 5; MEKK5; MEKK 5; MEK kinase 5; MAPKKK5; MAPK/ERK kinase kinase 5; ASK1; ASK-1
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| Target Type | Clinical trial Target | ||||
| Gene Name | MAP3K5 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 6 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4279758
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Investigative | Compound Info | ||
| Synonyms |
9-hydroxy-3'-N-acetylholyrine A; BDBM50465329
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| Activity |
IC50 ~ 50000 nM
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[1] | |||
| Compound Name |
Chembl4280872
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Investigative | Compound Info | ||
| Synonyms |
Streptocarbazole E; BDBM50465335
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| Activity |
IC50 ~ 50000 nM
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[1] | |||
| Compound Name |
Chembl4284275
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Investigative | Compound Info | ||
| Synonyms |
3-hydroxy-7-methoxy-K252c; BDBM50465336
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
(4E)-1-(4,6-Dimethyl-1,3-benzothiazol-2-yl)-4-[furan-2-yl(hydroxy)methylidene]-5-phenylpyrrolidine-2,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3402484; BDBM50069542; STL151061; AKOS002178226; AKOS005750937; AKOS016058476; MCULE-1370895680; ST50066811
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| Activity |
IC50 = 63000 nM
|
[2] | |||
| Compound Name |
3-((1-Methyl-1H-indol-3-yl)methylene)indolin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL471375; SCHEMBL5469785; ZINC7340; SCHEMBL14448833; BDBM50243715; STL518629; AKOS032438625; CCG-280084; (Z)-3-((1-methyl-1H-indol-3-yl)methylene)indolin-2-one; (3Z)-3-[(1-methyl-1H-indol-3-yl)methylidene]-1,3-dihydro-2H-indol-2-one
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| Activity |
IC50 = 82700 nM
|
[3] | |||
| Compound Name |
N-(1-Ethylimidazol-4-yl)-1,3-thiazole-4-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4062930; BDBM50237292
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| Activity |
IC50 = 100000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(1-Ethylimidazol-4-yl)furan-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4082079; BDBM50237291
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| Activity |
IC50 = 500000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61. J Nat Prod. 2018 Apr 27;81(4):949-956. | ||||
| REF 2 | Identification of apoptosis signal-regulating kinase 1 (ASK1) inhibitors among the derivatives of benzothiazol-2-yl-3-hydroxy-5-phenyl-1,5-dihydro-pyrrol-2-one. Bioorg Med Chem. 2015 May 15;23(10):2489-97. | ||||
| REF 3 | Development of a novel fluorescent probe for fluorescence correlation spectroscopic detection of kinase inhibitors. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3752-5. | ||||
| REF 4 | Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1709-1713. | ||||
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