Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T39195 | Target Info | |||
| Target Name | Kallikrein-14 (KLK14) | ||||
| Synonyms |
hK14; Kallikrein-like protein 6; KLKL6; KLK-L6
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| Target Type | Patented-recorded Target | ||||
| Gene Name | KLK14 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 10 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(2R)-2-[[(2R)-2-[[2-[[2-[[2-[[(2S)-2-[[(1R,7S,10S,13S,16S,22S,25S,28S,40R,43S,46S,49S,52S,58S,61S)-40-Acetamido-43,52-bis(2-amino-2-oxoethyl)-13-(carboxymethyl)-46-[(1R)-1-hydroxyethyl]-10,49,61-tris(1H-indol-3-ylmethyl)-16-methyl-25-(2-methylpropyl)-2,8,11,14,17,23,26,41,44,47,50,53,59,62-tetradecaoxo-30,38,65-trithia-3,9,12,15,18,24,27,42,45,48,51,54,60,63-tetradecazahexacyclo[32.29.3.132,36.03,7.018,22.054,58]heptahexaconta-32,34,36(67)-triene-28-carbonyl]amino]propanoyl]-methylamino]acetyl]-methylamino]acetyl]-methylamino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4059991; BDBM50256261
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| 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
|
[1] | |||
| 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 = 87000 nM
|
[2] | |||
| Compound Name |
4-[4-(4-Hydroxy-phenyl)-phthalazin-1-ylamino]-N-methyl-benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1462676; Cambridge id 7235017; MLS001212820; HMS2833P12; BDBM50444600; STK081312; AKOS000664808; ZINC100627035; MCULE-9143457757; SMR000523125; 4-{[4-(4-hydroxyphenyl)phthalazin-1-yl]amino}-N-methylbenzamide
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| Activity |
IC50 = 96000 nM
|
[2] | |||
| 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 = 99000 nM
|
[2] | |||
| 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 = 101000 nM
|
[2] | |||
| 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 = 106000 nM
|
[2] | |||
| 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 = 108000 nM
|
[2] | |||
| 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 = 112000 nM
|
[2] | |||
| 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 = 122000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor 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 | 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. | ||||
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