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Compound Detail

CHEMBL4793443

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C=CC(=O)Nc1ccc(OC)c(Nc2cc(-n3c(CCCO)nnc3-c3ccc(F)cc3)ccn2)c1

Basic Information

ChEMBL ID CHEMBL4793443
Phase Preclinical
Structure Type MOL
InChI Key NJHBBUOCKSUYLO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

488.5
MW (Da)
4.27
ALogP
8
HBA
3
HBD
114.2
PSA (Ų)
0.29
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25FN6O3
MW 488.52
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.44

Activity Summary

IC50 1 meas. best 4.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
A-431
CHEMBL614069
IC50 4.05 4.05 88600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
A-431 IC50 = 88600.0 nM 4.05 Antiproliferative activity against human A-431 cells harboring wild type EGFR as... 31869655

Literature References

PubMed DOI Target Context # Activities
31869655 10.1016/j.ejmech.2019.111966 Epidermal growth factor receptor 2
31869655 10.1016/j.ejmech.2019.111966 A-431 1
31869655 10.1016/j.ejmech.2019.111966 NCI-H1975 1
31869655 10.1016/j.ejmech.2019.111966 U-87 MG 1
31869655 10.1016/j.ejmech.2019.111966 Unchecked 1

Data from ChEMBL 36 via Core Engine