Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T94033 | Target Info | |||
| Target Name | Coagulation factor IIa (F2) | ||||
| Synonyms |
Prothrombin; Coagulation factor II
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| Target Type | Successful Target | ||||
| Gene Name | F2 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Coagulation factor Xa (F10) | Successful Target | ||||
| UniProt ID | FA10_HUMAN | |||||
| Gene Name | F10 | |||||
| Synonyms |
Fxa; Factor Xa; F10; Activated coagulation factor X
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| Representative Drug(s) | LB-30870 | Drug Info | Ki = 22.5 nM | Click to Show More | [1] | |
| 2 | Dabigatran | Drug Info | Ki ~ 1000 nM | [4] | ||
| Co-Target Name | Rho-associated protein kinase 1 (ROCK1) | Successful Target | ||||
| UniProt ID | ROCK1_HUMAN | |||||
| Gene Name | ROCK1 | |||||
| Synonyms |
Rok; Rho-associated, coiled-coil containing protein kinase 1; Rho-associated kinase 1; Rho kinase; ROCK1; ROCK; P160ROCK; P160(rock); P160 ROCK-1; Let-502 kinase
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| Representative Drug(s) | Ximelegatran | Drug Info | Ki = 25.12 nM | [2] | ||
| Co-Target Name | Tissue-type plasminogen activator (PLAT) | Successful Target | ||||
| UniProt ID | TPA_HUMAN | |||||
| Gene Name | PLAT | |||||
| Synonyms |
TPA; T-plasminogen activator; T-PA; Reteplase; Alteplase
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| Representative Drug(s) | LB-30870 | Drug Info | Ki = 433 nM | Click to Show More | [1] | |
| 2 | MELAGATRAN | Drug Info | Ki = 900 nM | [3] | ||
| Co-Target Name | Plasminogen (PLG) | Successful Target | ||||
| UniProt ID | PLMN_HUMAN | |||||
| Gene Name | PLG | |||||
| Synonyms |
Plasmin
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| Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 700 nM | [3] | ||
| Co-Target Name | Rho-associated protein kinase 2 (ROCK2) | Successful Target | ||||
| UniProt ID | ROCK2_HUMAN | |||||
| Gene Name | ROCK2 | |||||
| Synonyms |
p164 ROCK-2; Rho-associated, coiled-coil-containing protein kinase II; Rho-associated, coiled-coil-containing protein kinase 2; Rho kinase 2; ROCK-II; KIAA0619
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| Representative Drug(s) | Ximelegatran | Drug Info | IC50 = 54 nM | [5] | ||
| Co-Target Name | Serine protease hepsin (HPN) | Patented-recorded Target | ||||
| UniProt ID | HEPS_HUMAN | |||||
| Gene Name | HPN | |||||
| Synonyms |
Transmembrane protease, serine 1; HPN; HEPSIN
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| Representative Drug(s) | Dabigatran | Drug Info | Ki = 835 nM | [6] | ||
| Co-Target Name | Protein kinase N2 (PKN2) | Literature-reported Target | ||||
| UniProt ID | PKN2_HUMAN | |||||
| Gene Name | PKN2 | |||||
| Synonyms |
Serine/threonine-protein kinase N2; Protein-kinase C-related kinase 2; Protein kinase C-like 2; PRKCL2; PRK2; PKN gamma
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| Representative Drug(s) | Ximelegatran | Drug Info | IC50 = 600 nM | [7] | ||
| Co-Target Name | Trypsin (TRY) | Co-Target | ||||
| UniProt ID | TRY1_HUMAN; TRY2_HUMAN; TRY3_HUMAN | |||||
| Gene Name | PRSS1; PRSS2; PRSS3 | |||||
| Representative Drug(s) | LB-30870 | Drug Info | Ki = 0.3 nM | Click to Show More | [1] | |
| 2 | MELAGATRAN | Drug Info | Ki = 4.3 nM | [8] | ||
| 3 | Dabigatran | Drug Info | Ki = 50 nM | [9] | ||
| 4 | RWJ-671818 | Drug Info | Ki = 128 nM | [10] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide. J Med Chem. 2003 Aug 14;46(17):3612-22. | ||||
| REF 2 | Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors. Bioorg Med Chem Lett. 2011 Jan 1;21(1):97-101. | ||||
| REF 3 | Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding. J Med Chem. 2020 Feb 27;63(4):1445-1472. | ||||
| REF 4 | 5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor. J Med Chem. 2013 Dec 12;56(23):9441-56. | ||||
| REF 5 | 3-[2-(Aminomethyl)-5-[(pyridin-4-yl)carbamoyl]phenyl] benzoates as soft ROCK inhibitors. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6442-6. | ||||
| REF 6 | Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets. Bioorg Med Chem. 2015 May 15;23(10):2328-43. | ||||
| REF 7 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. | ||||
| REF 8 | Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4779-84. | ||||
| REF 9 | Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs. J Med Chem. 2018 May 10;61(9):3799-3822. | ||||
| REF 10 | Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RW... J Med Chem. 2010 Feb 25;53(4):1843-56. | ||||
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