Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T31543 | Target Info | |||
| Target Name | Suppressor of tumorigenicity 14 protein (ST14) | ||||
| Synonyms |
Tumor-associated differentially-expressed gene 15 protein; Tumor associated differentially-expressed gene-15 protein; TADG15; Serine protease TADG-15; Serine protease 14; SNC19; Prostamin; PRSS14; Membrane-type serine protease 1; Membrane type serine protease 1; Matriptase; MT-SP1
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| Target Type | Patented-recorded Target | ||||
| Gene Name | ST14 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 12 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(7R,10S,13S,21S,24S,27S,30S,33S,36S,39S,42S,45R)-7-Acetamido-36-(3-amino-3-oxopropyl)-13-benzyl-24-(4-carbamimidamidobutyl)-39-(carboxymethyl)-10-(hydroxymethyl)-21-[(4-hydroxyphenyl)methyl]-33-(1H-imidazol-5-ylmethyl)-30-methyl-42-(2-methylpropyl)-8,11,14,19,22,25,28,34,37,40,43-undecaoxo-5,47,52-trithia-9,12,15,20,23,26,29,32,35,38,41,44-dodecazatetracyclo[25.23.3.13,49.015,18]tetrapentaconta-1,3(54),49-triene-45-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4094403; BDBM50256260
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| Activity |
Ki = 50000 nM
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[1] | |||
| Compound Name |
Chembl4162159
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Investigative | Compound Info | ||
| Synonyms |
BDBM50449676
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| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
2-(2-Hydroxyphenyl)-1H-indole-5-carboximidamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL284805; SCHEMBL4995709; BDBM14327; CTK0A6699; DTXSID10274311; CRA-8328; ZINC3591066; BDBM50102768; 2-(2-Hydroxyphenyl)-1H-indole-5-carboxamidine; 1H-Indole-5-carboximidamide, 2-(2-hydroxyphenyl)-; 2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}benzen-1-olate
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| Activity |
Ki = 60000 nM
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[3] | |||
| Compound Name |
2-(4-{(1Z)-2-Cyano-2-[N-(3-ethoxyphenyl)carbamoyl]vinyl}-2-methoxyphenoxy)acet ic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3099875; ZINC5059113; BDBM50444599; AKOS024279048; ST025143; SR-01000222996; SR-01000222996-1
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| Activity |
IC50 = 75000 nM
|
[4] | |||
| Compound Name |
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43R,49S)-25-(4-Aminobutyl)-49-benzyl-4,19-bis[(2S)-butan-2-yl]-34-[[4-(diaminomethylideneamino)phenyl]methyl]-28-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL412487
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| Activity |
Ki = 90000 nM
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[5] | |||
| Compound Name |
(Z)-2-Cyano-3-(3-ethoxy-4-hydroxyphenyl)-N-(4-hydroxyphenyl)prop-2-enamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3099871; BDBM50444603; ZINC15219993; SR-01000218135; SR-01000218135-1
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| Activity |
IC50 = 98000 nM
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[4] | |||
| Compound Name |
(5E)-5-(3,4-Dimethoxybenzylidene)-3-{[(5-fluoro-2-methylphenyl)amino]methyl}-1,3-thiazolidine-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3099882; HMS591L04; BDBM50444597; ZINC16677485; BIM-0030827.P001; AB00095447-01
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| Activity |
IC50 = 103000 nM
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[4] | |||
| Compound Name |
2-[(1S,7S,10S,13S,16S,22R,25S,31S,34S,37S,40S,43S,46S)-40-(4-Aminobutyl)-16-benzyl-10,46-bis[(2S)-butan-2-yl]-31-[3-(diaminomethylideneamino)propyl]-37-[(1R)-1-hydroxyethyl]-13,34,43-tris(hydroxymethyl)-2,8,11,14,17,23,26,29,32,35,38,41,44,47-tetradecaoxo-3,9,12,15,18,24,27,30,33,36,39,42,45,48-tetradecazatetracyclo[46.3.0.03,7.018,22]henpentacontan-25-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL397831
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| Activity |
Ki = 107000 nM
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[5] | |||
| Compound Name |
(2Z)-2-Cyano-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenyl)prop-2-enamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3099870; BDBM50444604; ZINC12418985; AKOS024279418; ST026815; SR-01000218255; SR-01000218255-1
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| Activity |
IC50 = 111000 nM
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[4] | |||
| Compound Name |
(Z)-2-Cyano-3-(4-hydroxy-3-methoxyphenyl)-N-(4-methoxyphenyl)prop-2-enamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3099874; ZINC5023753; BDBM50444602; SR-01000218328; SR-01000218328-1
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| Activity |
IC50 = 120000 nM
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[4] | |||
| Compound Name |
(2Z)-2-Benzimidazol-2-yl-3-[3-methoxy-4-(2-morpholin-4-yl-2-oxoethoxy)phenyl]p rop-2-enenitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3099878; ZINC4453116; BDBM50444598; AKOS000605166; ST50282865
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| Activity |
IC50 = 128000 nM
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[4] | |||
| Compound Name |
(E)-3-[3-[(4-Chlorophenoxy)methyl]-4-methoxyphenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3099883; ZINC5102252; BDBM50444596
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| Activity |
IC50 = 138000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 8 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43R,49S)-25-(3-Aminopropyl)-49-benzyl-4,19-bis[(2S)-butan-2-yl]-34-[3-(diaminomethylideneamino)propyl]-28-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL412486
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| Activity |
Ki > 250000 nM
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[5] | |||
| Compound Name |
Mupain-1
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3734777; BDBM50499239
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| Activity |
Ki > 1000000 nM
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[6] | |||
| Compound Name |
(3R,8R,11S,14S,17S,20S,23S,26S,29S,32S)-3-Amino-20-[(1-carbamimidoylpiperidin-4-yl)methyl]-11-(carboxymethyl)-23-(hydroxymethyl)-17,26-bis[(4-hydroxyphenyl)methyl]-29-methyl-14-(2-methylpropyl)-2,10,13,16,19,22,25,28,31-nonaoxo-5,6-dithia-1,9,12,15,18,21,24,27,30-nonazabicyclo[30.3.0]pentatriacontane-8-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3735080; BDBM50499240
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| Activity |
Ki > 1000000 nM
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[6] | |||
| Compound Name |
3-Amino-N-(3-{(S)-1-[4-(2-amino-ethyl)-piperidine-1-carbonyl]-4-phenyl-butylsulfamoyl}-phenyl)-propionamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL518010; BDBM50254023
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| Activity |
Ki > 1000000 nM
|
[7] | |||
| Compound Name |
(3R,8R,11S,14S,17S,20S,23S,26S,29S,32S)-3-Amino-23-benzyl-20-[(1-carbamimidoylpiperidin-4-yl)methyl]-26-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-17,29-dimethyl-14-(2-methylpropyl)-2,10,13,16,19,22,25,28,31-nonaoxo-5,6-dithia-1,9,12,15,18,21,24,27,30-nonazabicyclo[30.3.0]pentatriacontane-8-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3735263; BDBM50499238
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| Activity |
Ki > 1000000 nM
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[6] | |||
| Compound Name |
(3R,8R,11S,14S,17S,20S,23S,26S,29S,32S)-3-Amino-11,23-dibenzyl-20-[(1-carbamimidoylpiperidin-4-yl)methyl]-26-[3-(diaminomethylideneamino)propyl]-17,29-dimethyl-14-(2-methylpropyl)-2,10,13,16,19,22,25,28,31-nonaoxo-5,6-dithia-1,9,12,15,18,21,24,27,30-nonazabicyclo[30.3.0]pentatriacontane-8-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3735513; BDBM50499241
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| Activity |
Ki > 1000000 nM
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[6] | |||
| Compound Name |
3-Amino-N-(3-{(S)-1-[4-(2-amino-ethyl)-piperidine-1-carbonyl]-3-phenyl-propylsulfamoyl}-phenyl)-propionamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL459507; BDBM50254022
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| Activity |
Ki > 1000000 nM
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[7] | |||
| Compound Name |
(3R,8R,11S,14S,17S,20S,23S,26S,29S,32S)-3-Amino-29-(4-aminobutyl)-11,23-dibenzyl-20-[(1-carbamimidoylpiperidin-4-yl)methyl]-26-[3-(diaminomethylideneamino)propyl]-17-methyl-14-(2-methylpropyl)-2,10,13,16,19,22,25,28,31-nonaoxo-5,6-dithia-1,9,12,15,18,21,24,27,30-nonazabicyclo[30.3.0]pentatriacontane-8-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3735217; BDBM50499237
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| Activity |
Ki > 1000000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema. J Med Chem. 2018 Apr 12;61(7):2823-2836. | ||||
| REF 2 | Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1. Eur J Med Chem. 2018 Jul 15;155:695-704. | ||||
| REF 3 | 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. | ||||
| REF 4 | Identification by in silico and in vitro screenings of small organic molecules acting as reversible inhibitors of kallikreins. Eur J Med Chem. 2013;70:661-8. | ||||
| REF 5 | Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1. J Med Chem. 2007 Nov 29;50(24):5976-83. | ||||
| REF 6 | Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor. J Med Chem. 2015 Nov 25;58(22):8868-76. | ||||
| REF 7 | Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors. Bioorg Med Chem Lett. 2009 Jan 1;19(1):67-73. | ||||
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