Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T98022 | Target Info | |||
| Target Name | Carboxypeptidase B2 (CPB2) | ||||
| Synonyms |
Thrombin-activable fibrinolysis inhibitor; TAFI; Plasma carboxypeptidase B; Carboxypeptidase U; CPU; CPB2
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| Target Type | Clinical trial Target | ||||
| Gene Name | CPB2 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 9 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
6-Dimethylamino-2-(1H-imidazol-4-yl)-hexanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL432907; SCHEMBL7256094; BDBM50144338; 6-(dimethylamino)-2-(1H-imidazol-5-yl)hexanoic acid
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
(2R)-2-[[(1S)-2-(6-Aminopyridin-3-yl)-1-cyanoethyl]carbamoylamino]-3-cyclohexyl-N-(4,7,7-trimethyl-2-bicyclo[2.2.1]heptanyl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3577446; BDBM50089782
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| Activity |
IC50 = 54000 nM
|
[2] | |||
| Compound Name |
(2S)-6-Amino-2-[[(2R)-3-cyclohexyl-1-oxo-1-pyrrolidin-1-ylpropan-2-yl]carbamoylamino]hexanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3577331; SCHEMBL3203822; BDBM50089693
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| Activity |
IC50 = 59000 nM
|
[2] | |||
| Compound Name |
Ethyl 7-amino-2-(sulfanylmethyl)heptanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164455; BDBM50395739
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| Activity |
IC50 = 62000 nM
|
[3] | |||
| Compound Name |
3-(2-Amino-pyrimidin-5-yl)-2-(1H-imidazol-4-yl)-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL66976; BDBM50144326
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| Activity |
IC50 = 67000 nM
|
[1] | |||
| Compound Name |
(2S)-6-Amino-2-[[(2R)-1-(2-bicyclo[2.2.1]heptanylamino)-3-cyclohexyl-1-oxopropan-2-yl]sulfamoylamino]hexanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3890531; BDBM50197571
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| Activity |
IC50 = 75000 nM
|
[4] | |||
| Compound Name |
alpha-Benzyl-1H-imidazole-4-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL33352; BDBM50100009; 2-(1H-Imidazol-4-yl)-3-phenyl-propionic acid; 2-(3H-Imidazol-4-yl)-3-phenyl-propionic acid
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
7-(3-Aminopropyl)-3-ethyl-6,8-dihydro-5H-imidazo[1,2-a]pyridine-7-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3235138; BDBM50008277
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
Ethyl 2-[(6-aminopyridin-3-yl)methyl]-3-propanoylselanylpropanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164452; BDBM50395731
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| Activity |
IC50 = 180000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Ethyl 2-(acetylsulfanylmethyl)-7-aminoheptanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164454; BDBM50395740
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| Activity |
IC50 = 310000 nM
|
[3] | |||
| Compound Name |
Chembl4127473
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Investigative | Compound Info | ||
| Synonyms |
BDBM50275212
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| Activity |
IC50 = 370000 nM
|
[7] | |||
| Compound Name |
Ethyl 2-[(6-amino-5-chloropyridin-3-yl)methyl]-3-propanoylselanylpropanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164451; BDBM50395729
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| Activity |
IC50 > 3800000 nM
|
[3] | |||
| Compound Name |
7-Amino-2-[[(7-amino-2-carboxyheptyl)diselanyl]methyl]heptanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164457; BDBM50395737
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| Activity |
IC50 > 3800000 nM
|
[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group. Bioorg Med Chem Lett. 2004 May 3;14(9):2141-5. | ||||
| REF 2 | Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin. J Med Chem. 2015 Jun 11;58(11):4839-44. | ||||
| REF 3 | Design and characterization of a selenium-containing inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa), a zinc-containing metalloprotease. J Med Chem. 2012 Sep 13;55(17):7696-705. | ||||
| REF 4 | Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa). J Med Chem. 2016 Oct 27;59(20):9567-9573. | ||||
| REF 5 | Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics. J Med Chem. 2003 Dec 4;46(25):5294-7. | ||||
| REF 6 | Design and synthesis of conformationally restricted inhibitors of active thrombin activatable fibrinolysis inhibitor (TAFIa). Bioorg Med Chem. 2014 Apr 1;22(7):2261-8. | ||||
| REF 7 | Structural basis for the selective inhibition of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) by a selenium-containing inhibitor with chloro-aminopyridine as a basic group. Bioorg Med Chem Lett. 2018 Jul 15;28(13):2256-2260. | ||||
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