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Compound Detail

CHEMBL4294411

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CCOC(=O)c1ccc(-c2c(-c3cccc(C)n3)nn3c2C(C)C(C)(C)C3)cc1

Basic Information

ChEMBL ID CHEMBL4294411
Phase Preclinical
Structure Type MOL
InChI Key TUQJLUVEHCATLN-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

389.5
MW (Da)
5.24
ALogP
5
HBA
0
HBD
57.0
PSA (Ų)
0.57
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27N3O2
MW 389.50
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.37

Activity Summary

IC50 3 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-1
CHEMBL4439
IC50 5.7 5.7 2008.0 1
MCF7
CHEMBL387
IC50 4.54 4.54 29000.0 1
K562
CHEMBL385
IC50 4.35 4.35 45000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28135685 10.1016/j.ejmech.2017.01.018 TGF-beta receptor type-1 1
28135685 10.1016/j.ejmech.2017.01.018 Cyclin-dependent kinase 2/cyclin E1 1
28135685 10.1016/j.ejmech.2017.01.018 Tyrosine-protein kinase ABL1 1
28135685 10.1016/j.ejmech.2017.01.018 K562 1
28135685 10.1016/j.ejmech.2017.01.018 MCF7 1

Data from ChEMBL 36 via Core Engine