Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T53612 | Target Info | |||
| Target Name | Kallikrein-6 (KLK6) | ||||
| Synonyms |
Zyme; Serine protease 9; Serine protease 18; SP59; Protease M; PRSS9; PRSS18; Neurosin; MSP; K6
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| Target Type | Literature-reported Target | ||||
| Gene Name | KLK6 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 7 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 |
Chembl4213650
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Investigative | Compound Info | ||
| Synonyms |
BDBM50459528
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(2R)-2-[[(2R)-2-[[2-[[2-[[2-[[(2S)-2-[[(7R,10S,13S,16S,22S,25S,28S,31R,34S,37S,45S,48S,51R)-51-Acetamido-45-benzyl-10-[(2S)-butan-2-yl]-34-(4-carbamimidamidobutyl)-13-(carboxymethyl)-48-(hydroxymethyl)-22,25,37-tris[(4-hydroxyphenyl)methyl]-9,12,15,21,24,27,30,33,36,39,44,47,50-tridecaoxo-28-propan-2-yl-5,53,58-trithia-8,11,14,20,23,26,29,32,35,38,43,46,49-tridecazapentacyclo[29.25.3.13,55.016,20.040,43]hexaconta-1(56),2,55(60)-triene-7-carbonyl]amino]propanoyl]-methylamino]acetyl]-methylamino]acetyl]-methylamino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4070056; BDBM50256262
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4202434
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL20037288; BDBM50459532
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| Activity |
IC50 = 58000 nM
|
[2] | |||
| Compound Name |
Chembl4202971
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Investigative | Compound Info | ||
| Synonyms |
BDBM50459533
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| Activity |
IC50 = 110000 nM
|
[2] | |||
| Compound Name |
Chembl4211470
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Investigative | Compound Info | ||
| Synonyms |
ZINC9670559; BDBM50459513; AKOS001221230; MCULE-9165584447
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| Activity |
IC50 = 170000 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 |
Chembl4214840
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50459519
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| Activity |
IC50 > 200000 nM
|
[2] | |||
| Compound Name |
Chembl4210437
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Investigative | Compound Info | ||
| Synonyms |
BDBM50459521
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| Activity |
IC50 > 200000 nM
|
[2] | |||
| Compound Name |
Chembl4207321
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50459517; AKOS006617928
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| Activity |
IC50 > 200000 nM
|
[2] | |||
| 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 | Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity. J Med Chem. 2018 Oct 11;61(19):8859-8874. | ||||
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