Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T73471 | Target Info | |||
| Target Name | Serine protease hepsin (HPN) | ||||
| Synonyms |
Transmembrane protease, serine 1; HPN; HEPSIN
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| Target Type | Patented-recorded Target | ||||
| Gene Name | HPN | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 5 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-[3-(1-Benzyl-piperidin-4-yl)-ureido]-benzamidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL327254; BDBM50071945
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| Activity |
Ki = 53100 nM
|
[1] | |||
| Compound Name |
Chembl4126725
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Investigative | Compound Info | ||
| Synonyms |
BDBM50272236
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| Activity |
IC50 = 58000 nM
|
[2] | |||
| Compound Name |
4-[3-(1-Benzylpiperidin-4-yl)-5-methyl-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780437; BDBM50158162
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| Activity |
Ki = 61200 nM
|
[1] | |||
| Compound Name |
2-(2-Hydroxy-5-thiophen-2-ylphenyl)-1H-indole-5-carboximidamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3828185; SCHEMBL18817912; BDBM50187712
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| Activity |
IC50 = 70000 nM
|
[3] | |||
| Compound Name |
Chembl4126876
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Investigative | Compound Info | ||
| Synonyms |
BDBM50272281
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| Activity |
IC50 = 73000 nM
|
[2] | |||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1H-Indole-5-carboximidamide
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Investigative | Compound Info | ||
| Synonyms |
1H-Indole-5-carboxamidine; 5-Amidinoindole; CHEMBL26490; SCHEMBL563181; CTK2I0095; ZINC1439372; 4714AH; BDBM50027306; AKOS006352033; AB18264; SC-58549; DB-074491; FT-0756503
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| Activity |
Ki = 500000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation. ACS Med Chem Lett. 2015 Dec 22;7(2):177-81. | ||||
| REF 2 | Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform. J Med Chem. 2018 May 24;61(10):4335-4347. | ||||
| REF 3 | Design, synthesis and biological evaluation of PSMA/hepsin-targeted heterobivalent ligands. Eur J Med Chem. 2016 Aug 8;118:208-218. | ||||
| REF 4 | Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5309-14. | ||||
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