Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T67022
(Former ID: TTDR00960)
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| Target Name |
Caspase (CASP)
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| Gene Name |
NO-GeName
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Cardiovascular disease [ICD-11: BA00-BE2Z] | |||||
| BioChemical Class |
Peptidase
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | NCX-1000 | Drug Info | Phase 2 | Cardiovascular disease | [2] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | VX-166 | Drug Info | Preclinical | Hepatic fibrosis | [3] | |
| 2 | Z-VAD-fmk | Drug Info | Preclinical | Pulmonary fibrosis | [3] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | ALS-769 | Drug Info | Terminated | Solid tumour/cancer | [4] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | NCX-1000 | Drug Info | [1] | |||
| Inhibitor | [+] 5 Inhibitor drugs | + | ||||
| 1 | VX-166 | Drug Info | [5] | |||
| 2 | Z-VAD-fmk | Drug Info | [6] | |||
| 3 | Ac-DEVD-CHO | Drug Info | [9] | |||
| 4 | IDN-1965 | Drug Info | [10] | |||
| 5 | Isoquinoline-1,3,4(2H)-trione | Drug Info | [11] | |||
| Inducer | [+] 1 Inducer drugs | + | ||||
| 1 | ALS-769 | Drug Info | [7] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | 2-aminophenoxazine-3-one | Drug Info | [8] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Liver delivery of NO by NCX-1000 protects against acute liver failure and mitochondrial dysfunction induced by APAP in mice. Br J Pharmacol. 2004 Sep;143(1):33-42. | |||||
| REF 2 | ClinicalTrials.gov (NCT00414869) Preliminary Efficacy and Tolerability of NCX-1000 After Repeated Oral Doses in Patients With Elevated Portal Pressure. U.S. National Institutes of Health. | |||||
| REF 3 | Drugs and Targets in Fibrosis. Front Pharmacol. 2017 Nov 23;8:855. | |||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025089) | |||||
| REF 5 | VX-166: a novel potent small molecule caspase inhibitor as a potential therapy for sepsis. Crit Care. 2009;13(5):R146. | |||||
| REF 6 | Clinical pipeline report, company report or official report of InvivoGen. | |||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025089) | |||||
| REF 8 | Apoptosis as a mechanism for the treatment of adult T cell leukemia: promising drugs from benchside to bedside. Drug Discov Today. 2020 Jul;25(7):1189-1197. | |||||
| REF 9 | Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study. Eur J Med Chem. 2010 Sep;45(9):3858-63. | |||||
| REF 10 | Inhibition of cardiac myocyte apoptosis improves cardiac function and abolishes mortality in the peripartum cardiomyopathy of Galpha(q) transgenic ... Circulation. 2003 Dec 16;108(24):3036-41. | |||||
| REF 11 | Design, synthesis, and biological evaluation of isoquinoline-1,3,4-trione derivatives as potent caspase-3 inhibitors. J Med Chem. 2006 Mar 9;49(5):1613-23. | |||||
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