Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMC7W6R)

Drug Name
Selumetinib Drug Info
Synonyms
Selumetinib; AZD-6244; ARRY142886; AZD6244; ARRY142886; AZD 6244; AZD-6244; 6UH91I579U; ARRY 142886; ARRY-142886; AZD6244 (Selumetinib); AZD6244(Selumetinib); CHEBI:90227; CHEMBL1614701; MEK inhibitors; Selumetinib (AZD6244); UNII-6UH91I579U
Indication
Disease Entry ICD 11 Status REF
Neurofibromatosis type 1 LD2D.10 Approved [1]
Melanoma 2C30 Phase 3 [2]
Thyroid cancer 2D10 Phase 3 [3]
Non-small-cell lung cancer 2C25.Y Phase 2 [4]
Middle East Respiratory Syndrome (MERS) 1D64 Investigative [5]
Severe acute respiratory syndrome (SARS) 1D65 Investigative [5]
Solid tumour/cancer 2A00-2F9Z Investigative [6]
Cross-matching ID
PubChem CID
10127622
ChEBI ID
CHEBI:90227
CAS Number
CAS 606143-52-6
TTD Drug ID
DMC7W6R
ACDINA Drug ID
D01422

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
ERK activator kinase 1 (MEK1) TTIDAPM MP2K1_HUMAN Inhibitor [3]
ERK activator kinase 2 (MEK2) TTTW2NY MP2K2_HUMAN Inhibitor [3]
MAPK/ERK kinase kinase (MAP3K) TTROQ37 NOUNIPROTAC Modulator [7]
HUMAN ERK activator kinase 1 (MEK1) TTAW3TO MP2K1_HUMAN Inhibitor [5]
HUMAN ERK activator kinase 2 (MEK2) TTWX403 MP2K2_HUMAN Inhibitor [5]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
ERK activator kinase 2 (MEK2) DTT MAP2K2 4.372 6.068 6.352 6.894
ERK activator kinase 1 (MEK1) DTT MAP2K1 8.617 7.493 7.334 6.969
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

ICD Disease Classification 02 Neoplasm
Disease Class ICD-11: 2C82 Prostate cancer
The Studied Tissue Skin
The Studied Disease Melanoma [ICD-11:2C82]
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
ERK activator kinase 2 (MEK2) DTT MAP2K2 2.87E-01 0.91 0.61
ERK activator kinase 1 (MEK1) DTT MAP2K1 8.00E-01 -0.07 -0.15
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 ClinicalTrials.gov (NCT01933932) Assess Efficacy & Safety of Selumetinib in Combination With Docetaxel in Patients Receiving 2nd Line Treatment for v-Ki-ras2 Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) Positive NSCLC (SELECT-1)
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 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: 5665).
5 Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47.
6 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. (Target id: 1479).
7 Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells.Br J Cancer.2012 May 8;106(10):1648-59.