Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T14558 | Target Info | |||
| Target Name | Tryptase alpha/beta-1 (Tryptase) | ||||
| Synonyms |
Tryptase-1; Tryptase alpha-1; Tryptase I; TPSB1; TPS2; TPS1
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| Target Type | Successful Target | ||||
| Gene Name | TPSAB1 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 3 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(3,3-Diphenylpropyl)-4-[methyl(4-amidinobenzoyl)aminomethyl]piperidine-1-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL308376; BDBM50103791
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| Activity |
Ki = 50000 nM
|
[1] | |||
| Compound Name |
N-Benzyl-N-methyl-N'-(4-guanidinobenzyl)piperazine-1,4-dicarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL305643; BDBM50103798; Piperazine-1,4-dicarboxylic acid benzyl-methyl-amide 4-guanidino-benzylamide
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| Activity |
Ki = 80000 nM
|
[1] | |||
| Compound Name |
1beta,5beta-Bis[4-(benzylcarbamoyl)piperazinocarbonyloxy]cyclooctane
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL43463; BDBM50093140
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| Activity |
Ki = 101000 nM
|
[2] | |||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(R)-2-Acetylamino-3-(4-aminomethyl-phenyl)-propionic acid methyl ester
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL176984; BDBM50112066
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| Activity |
Ki = 213000 nM
|
[3] | |||
| Compound Name |
N-(4-Guanidinobenzyl)-N'-ethylpiperazine-1,4-dicarboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL77104; BDBM50103795; Piperazine-1,4-dicarboxylic acid ethylamide 4-guanidino-benzylamide
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| Activity |
Ki = 370000 nM
|
[1] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors. Bioorg Med Chem Lett. 2001 Sep 3;11(17):2325-30. | ||||
| REF 2 | Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors. Bioorg Med Chem Lett. 2000 Oct 16;10(20):2357-60. | ||||
| REF 3 | Bivalent inhibition of beta-tryptase: distance scan of neighboring subunits by dibasic inhibitors. Bioorg Med Chem Lett. 2002 Mar 25;12(6):985-8. | ||||
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