Details of the Drug

General Information of Drug (ID: DMRPCF2)

• Drug Name: MGCD265
• Synonyms: MGCD-265; 875337-44-3; MGCD265; MGCD-265 analog; MGCD 265; N-(3-fluoro-4-(2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide; UNII-93M6577H9D; CHEMBL254760; 93M6577H9D; n-(3-fluoro-4-(2-(1-methyl-1h-imidazol-4-yl)thieno(3,2-b)pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide; N-[(3-Fluoro-4-{[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)carbamothioyl]-2-phenylacetamide

Indication

Disease Entry	ICD 11	Status	REF
Non-small-cell lung cancer	2C25.Y	Phase 2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 1:
  Molecular Weight (mw); 517.6
  Logarithm of the Partition Coefficient (xlogp); 4.9
  Rotatable Bond Count (rotbonds); 6
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 7
• Chemical Identifiers:
  Formula: C26H20FN5O2S2
  IUPAC Name: N-[[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-phenylacetamide
  Canonical SMILES: CN1C=C(N=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=CC=C5)F
  InChI: InChI=1S/C26H20FN5O2S2/c1-32-14-20(29-15-32)23-13-19-25(36-23)22(9-10-28-19)34-21-8-7-17(12-18(21)27)30-26(35)31-24(33)11-16-5-3-2-4-6-16/h2-10,12-15H,11H2,1H3,(H2,30,31,33,35)
  InChIKey: UFICVEHDQUKCEA-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 24901704
  ChEBI ID: CHEMBL254760
  CAS Number: 875337-44-3
  TTD ID: D08FDX
• Drug-Molecule Activity Atlas (DMA)NEW: Click to Jump to the Detailed DMA Information of This Drug
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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Protein kinase (PK)	TTU8W4S	NOUNIPROTAC	Inhibitor	[2]
Tyrosine-protein kinase UFO (AXL)	TTZPY6J	UFO_HUMAN	Modulator	[3]

Molecular Expression Atlas of This Drug

• The Studied Disease: Non-small-cell lung cancer
• ICD Disease Classification: 2C25.Y

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Tyrosine-protein kinase UFO (AXL)	DTT	AXL	1.13E-65	-0.53	-2.04

References

• [1] ClinicalTrials.gov (NCT02544633) Phase 2 Study of MGCD265 in Patients With Non-Small Cell Lung Cancer With Activating Genetic Alterations in MET.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Company report (Mirati Therapeutics: formerly MethylGene)