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Compound Detail

CHEMBL4781323

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C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C4CC4)c4ccccc34)n2)c(OC)cc1OCCN(C)C

Basic Information

ChEMBL ID CHEMBL4781323
Phase Preclinical
Structure Type MOL
InChI Key FSUIAZJSIDRSAY-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

512.6
MW (Da)
5.25
ALogP
8
HBA
2
HBD
93.5
PSA (Ų)
0.27
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32N6O3
MW 512.61
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.00

Activity Summary

IC50 3 meas. best 9.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NCI-H292
CHEMBL614733
IC50 9.37 9.37 0.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NCI-H292 IC50 = 0.432 nM 9.37 Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR... 33429247

Literature References

Data from ChEMBL 36 via Core Engine