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Compound Detail

CHEMBL213762

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CC(C)COc1cc(OC2CCN(C)CC2)c2c(Nc3c(Cl)ccc4c3OCO4)ncnc2c1

Basic Information

ChEMBL ID CHEMBL213762
Phase Preclinical
Structure Type MOL
InChI Key CFEJJQZWMZTARJ-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

485.0
MW (Da)
5.26
ALogP
8
HBA
1
HBD
78.0
PSA (Ų)
0.49
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29ClN4O4
MW 484.98
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.48

Activity Summary

IC50 3 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 8.15 7.575 7.0 2
A549
CHEMBL392
IC50 6.7 6.7 200.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 600.0 ng.hr.mL-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17064066 10.1021/jm060434q Proto-oncogene tyrosine-protein kinase Src 2
17064066 10.1021/jm060434q Vascular endothelial growth factor receptor 2 1
17064066 10.1021/jm060434q A549 1
17064066 10.1021/jm060434q Mus musculus 1

Data from ChEMBL 36 via Core Engine