Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T20474
(Former ID: TTDR00142)
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| Target Name |
DNA topoisomerase (TOP)
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| Gene Name |
NO-GeName
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Lung cancer [ICD-11: 2C25] | |||||
| 2 | Ovarian cancer [ICD-11: 2C73] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | Karenitecin | Drug Info | Phase 3 | Lung cancer | [2] | |
| 2 | Icofungipen | Drug Info | Phase 2 | Fungal infection | [3] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 16 Inhibitor drugs | + | ||||
| 1 | Karenitecin | Drug Info | [1] | |||
| 2 | Icofungipen | Drug Info | [4] | |||
| 3 | 2-Amino-6-(indan-5-ylamino)-3H-pyrimidin-4-one | Drug Info | [5] | |||
| 4 | 3-(9-Acridinylamino)-5-(hydroxymethyl)aniline (AHMA) | Drug Info | [4] | |||
| 5 | 5-Bromo-6-p-tolylamino-1H-pyrimidine-2,4-dione | Drug Info | [5] | |||
| 6 | 6-(3-Bromo-phenylamino)-1H-pyrimidine-2,4-dione | Drug Info | [6] | |||
| 7 | 6-(3-Ethyl-phenylamino)-1H-pyrimidine-2,4-dione | Drug Info | [6] | |||
| 8 | 6-(3-Iodo-phenylamino)-1H-pyrimidine-2,4-dione | Drug Info | [6] | |||
| 9 | 6-(Indan-5-ylamino)-1H-pyrimidine-2,4-dione | Drug Info | [6] | |||
| 10 | 6-(Naphthalen-2-ylamino)-1H-pyrimidine-2,4-dione | Drug Info | [6] | |||
| 11 | 6-Benzylamino-1H-pyrimidine-2,4-dione | Drug Info | [5] | |||
| 12 | 6-Benzylamino-5-bromo-1H-pyrimidine-2,4-dione | Drug Info | [5] | |||
| 13 | 6-Benzylamino-5-iodo-1H-pyrimidine-2,4-dione | Drug Info | [5] | |||
| 14 | 6-p-Tolylamino-1H-pyrimidine-2,4-dione | Drug Info | [6] | |||
| 15 | N*4*-Benzyl-6-chloro-pyrimidine-2,4-diamine | Drug Info | [5] | |||
| 16 | TOPOSTATIN | Drug Info | [7] | |||
| 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 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | ClinicalTrials.gov (NCT00477282) Karenitecin Versus Topotecan in Patients With Advanced Epithelial Ovarian Cancer. U.S. National Institutes of Health. | |||||
| REF 3 | Efficacy, plasma pharmacokinetics, and safety of icofungipen, an inhibitor of Candida isoleucyl-tRNA synthetase, in treatment of experimental disseminated candidiasis in persistently neutropenic rabbits. Antimicrob Agents Chemother. 2005 May;49(5):2084-92. | |||||
| REF 4 | Crystallization and preliminary X-ray analysis of anti-cancer agent 3-(9-acridinylamino)-5-(hydroxymethyl)aniline complexed with the DNA hexamer d(CGTACG)2. Biochim Biophys Acta. 2003 Jan 3;1625(1):27-9. | |||||
| REF 5 | Inhibitors of Bacillus subtilis DNA polymerase III. Influence of modifications in the pyrimidine ring of anilino- and (benzylamino)pyrimidines. J Med Chem. 1986 May;29(5):676-81. | |||||
| REF 6 | Inhibitors of Bacillus subtilis DNA polymerase III. 6-Anilinouracils and 6-(alkylamino)uracils. J Med Chem. 1980 Jan;23(1):34-8. | |||||
| REF 7 | Isoaurostatin, a novel topoisomerase inhibitor produced by Thermomonospora alba. J Nat Prod. 2001 Feb;64(2):204-7. | |||||
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