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Compound Detail

CHEMBL4434694

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COc1cc(-c2cncc(-c3ccc(N4CCNCC4)cc3)c2C)cc(Cl)c1C(N)=O

Basic Information

ChEMBL ID CHEMBL4434694
Phase Preclinical
Structure Type MOL
InChI Key LQWXPQRLAHKASJ-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

436.9
MW (Da)
3.89
ALogP
5
HBA
2
HBD
80.5
PSA (Ų)
0.63
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25ClN4O2
MW 436.94
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.62

Activity Summary

IC50 5 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Activin receptor type-1
CHEMBL5903
IC50 8.4 7.945 4.0 4
TGF-beta receptor type-1
CHEMBL4439
IC50 5.68 5.68 2080.0 1

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 2

Data from ChEMBL 36 via Core Engine