Target Information
| Target General Information | Top | |||||
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| Target ID |
T30823
(Former ID: TTDR00202)
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| Target Name |
M-phase inducer phosphatase 1 (MPIP1)
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| Synonyms |
Dual specificity phosphatase Cdc25A; Cdc25A phosphatase
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| Gene Name |
CDC25A
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| Target Type |
Literature-reported target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Asthma [ICD-11: CA23] | |||||
| 2 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
Directly dephosphorylates CDK1 and stimulates its kinase activity. Also dephosphorylates CDK2 in complex with cyclin E, in vitro. Tyrosine protein phosphatase which functions as a dosage-dependent inducer of mitotic progression.
Click to Show/Hide
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| BioChemical Class |
Phosphoric monoester hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.1.3.48
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| Sequence |
MELGPEPPHRRRLLFACSPPPASQPVVKALFGASAAGGLSPVTNLTVTMDQLQGLGSDYE
QPLEVKNNSNLQRMGSSESTDSGFCLDSPGPLDSKENLENPMRRIHSLPQKLLGCSPALK RSHSDSLDHDIFQLIDPDENKENEAFEFKKPVRPVSRGCLHSHGLQEGKDLFTQRQNSAP ARMLSSNERDSSEPGNFIPLFTPQSPVTATLSDEDDGFVDLLDGENLKNEEETPSCMASL WTAPLVMRTTNLDNRCKLFDSPSLCSSSTRSVLKRPERSQEESPPGSTKRRKSMSGASPK ESTNPEKAHETLHQSLSLASSPKGTIENILDNDPRDLIGDFSKGYLFHTVAGKHQDLKYI SPEIMASVLNGKFANLIKEFVIIDCRYPYEYEGGHIKGAVNLHMEEEVEDFLLKKPIVPT DGKRVIVVFHCEFSSERGPRMCRYVRERDRLGNEYPKLHYPELYVLKGGYKEFFMKCQSY CEPPSYRPMHHEDFKEDLKKFRTKSRTWAGEKSKREMYSRLKKL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T08B2M | |||||
| Drugs and Modes of Action | Top | |||||
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| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | MX-7065 | Drug Info | Terminated | Solid tumour/cancer | [2] | |
| 2 | Ro 20-1724 | Drug Info | Terminated | Asthma | [3], [4] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 12 Inhibitor drugs | + | ||||
| 1 | MX-7065 | Drug Info | [1] | |||
| 2 | Ro 20-1724 | Drug Info | [5] | |||
| 3 | (E)-2-(1-decyl-2-oxoindolin-3-ylidene)acetic acid | Drug Info | [6] | |||
| 4 | (Z)-2-(1-decyl-2-oxoindolin-3-ylidene)acetic acid | Drug Info | [6] | |||
| 5 | 1-dodecyl-1H-indole-2,3-dione | Drug Info | [6] | |||
| 6 | 2-(1-dodecyl-1H-indol-3-yl)acetic acid | Drug Info | [6] | |||
| 7 | 3-isopropyl-4-(phenylamino)naphthalene-1,2-dione | Drug Info | [7] | |||
| 8 | 3-isopropyl-4-(phenylthio)naphthalene-1,2-dione | Drug Info | [7] | |||
| 9 | 3-isopropyl-4-phenylnaphthalene-1,2-dione | Drug Info | [7] | |||
| 10 | 3-isopropylnaphthalene-1,2-dione | Drug Info | [7] | |||
| 11 | 4-(p-toluidino)-3-isopropylnaphthalene-1,2-dione | Drug Info | [7] | |||
| 12 | NSC-95397 | Drug Info | [8] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (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 Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Handbook of Assay Development in Drug Discovery, Lisa K. Minor, 2013. Page(11). | |||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016615) | |||||
| REF 3 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5258). | |||||
| 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 800003923) | |||||
| REF 5 | Role of the Cdc25A phosphatase in human breast cancer. J Clin Invest. 2000 Sep;106(6):753-61. | |||||
| REF 6 | Design and synthesis of N-alkyl oxindolylidene acetic acids as a new class of potent Cdc25A inhibitors. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3350-3. | |||||
| REF 7 | Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1905-8. | |||||
| REF 8 | Structure-based de novo design and biochemical evaluation of novel Cdc25 phosphatase inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4330-4. | |||||
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