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Compound Detail

CHEMBL4435320

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COc1cc(-c2cncc(-c3ccc(N4CCN(C)CC4)cc3)c2C)cc(OC)c1C(N)=O

Basic Information

ChEMBL ID CHEMBL4435320
Phase Preclinical
Structure Type MOL
InChI Key XIAQAOWQYMNJJB-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

446.6
MW (Da)
3.59
ALogP
6
HBA
1
HBD
80.9
PSA (Ų)
0.62
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H30N4O3
MW 446.55
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.54

Activity Summary

IC50 4 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Activin receptor type-1
CHEMBL5903
IC50 8.4 8.06 4.0 2
TGF-beta receptor type-1
CHEMBL4439
IC50 7.12 6.86 75.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32369358 10.1021/acs.jmedchem.0c00395 Activin receptor type-1 5
32369358 10.1021/acs.jmedchem.0c00395 TGF-beta receptor type-1 2
32369358 10.1021/acs.jmedchem.0c00395 Unchecked 1

Data from ChEMBL 36 via Core Engine