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Compound Detail

CHEMBL4291439

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Cc1cccc(-c2nn3c(c2-c2ccc(O)cc2)CC(C)(C)C3)n1

Basic Information

ChEMBL ID CHEMBL4291439
Phase Preclinical
Structure Type MOL
InChI Key KUZGRQRALYQLGV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

319.4
MW (Da)
4.21
ALogP
4
HBA
1
HBD
50.9
PSA (Ų)
0.77
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21N3O
MW 319.41
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.27

Activity Summary

IC50 2 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-1
CHEMBL4439
IC50 6.64 6.64 229.0 1
Tyrosine-protein kinase ABL1
CHEMBL3099
IC50 4.7 4.7 20000.0 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