Target Information
| Target General Information | Top | |||||
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| Target ID |
T99031
(Former ID: TTDC00164)
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| Target Name |
ERK activator kinase (MEK)
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| Synonyms |
MEK; MAPKK; MAP kinase kinase
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Melanoma [ICD-11: 2C30] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | ARRY-162 | Drug Info | Approved | Melanoma | [1] | |
| Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
| 1 | NFX-179 | Drug Info | Phase 2 | Neurofibromatosis 1 | [2] | |
| 2 | HL-085 | Drug Info | Phase 1/2 | Melanoma | [3] | |
| 3 | BI 3011441 | Drug Info | Phase 1 | Solid tumour/cancer | [4] | |
| 4 | GDC-0623 | Drug Info | Phase 1 | Solid tumour/cancer | [5] | |
| 5 | RG7304 | Drug Info | Phase 1 | Solid tumour/cancer | [6] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 18 Inhibitor drugs | + | ||||
| 1 | ARRY-162 | Drug Info | [1] | |||
| 2 | NFX-179 | Drug Info | [7] | |||
| 3 | HL-085 | Drug Info | [8] | |||
| 4 | BI 3011441 | Drug Info | [9] | |||
| 5 | GDC-0623 | Drug Info | [5] | |||
| 6 | Azetidine derivative 2 | Drug Info | [11] | |||
| 7 | Benzoheterocyclic compound 1 | Drug Info | [11] | |||
| 8 | Benzoimidazole derivative 1 | Drug Info | [11] | |||
| 9 | Benzoimidazole derivative 2 | Drug Info | [11] | |||
| 10 | N-(arylamino)sulfonamide derivative 1 | Drug Info | [11] | |||
| 11 | P-toluenesulfonate derivative 1 | Drug Info | [11] | |||
| 12 | PMID28594589-Compound-TABLE3C1 | Drug Info | [11] | |||
| 13 | PMID28594589-Compound-TABLE3C12 | Drug Info | [11] | |||
| 14 | PMID28594589-Compound-TABLE3C14 | Drug Info | [11] | |||
| 15 | PMID28594589-Compound-TABLE3C2 | Drug Info | [11] | |||
| 16 | Pyridinone compound 1 | Drug Info | [11] | |||
| 17 | Pyridopyrimidine derivative 1 | Drug Info | [11] | |||
| 18 | Quinazolines and azaquinazoline derivative 1 | Drug Info | [11] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | RG7304 | Drug Info | [10] | |||
| 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 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| REF 2 | ClinicalTrials.gov (NCT04435665) A Randomized, Double-Blind, Vehicle-Controlled, Parallel Group Phase 2a Study to Determine Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Activity of NFX-179 Gel in Subjects With Cutaneous Neurofibromas. U.S.National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT03973151) Study of HL-085 in NRAS Mutant Advanced Melanoma. U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT04742556) A Study to Test Different Doses of BI 3011441 in Japanese People With Different Types of Advanced Cancer (NRAS/KRAS Mutation Positive). U.S. National Institutes of Health. | |||||
| REF 5 | Clinical pipeline report, company report or official report of Genentech (2011). | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029782) | |||||
| REF 7 | Clinical pipeline report, company report or official report of NFlection Therapeutics | |||||
| REF 8 | Current Development Status of MEK Inhibitors. Molecules. 2017 Sep 26;22(10):1551. | |||||
| REF 9 | Clinical pipeline report, company report or official report of Boehringer Ingelheim. | |||||
| REF 10 | Clinical pipeline report, company report or official report of Roche. | |||||
| REF 11 | MEK inhibitors in oncology: a patent review (2015-Present).Expert Opin Ther Pat. 2017 Aug;27(8):887-906. | |||||
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