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Compound Detail

CHEMBL4752410

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O=C(Nc1ccccc1)c1ccc(-c2cc(-c3c[nH]nc3-c3ccccn3)ccn2)cc1

Basic Information

ChEMBL ID CHEMBL4752410
Phase Preclinical
Structure Type MOL
InChI Key RSEGOHMKRVRWOE-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

417.5
MW (Da)
5.45
ALogP
4
HBA
2
HBD
83.6
PSA (Ų)
0.40
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H19N5O
MW 417.47
Aromatic Rings 5
Heavy Atoms 32
NP-Likeness -1.32

Activity Summary

IC50 3 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-1
CHEMBL4439
IC50 7.75 7.75 18.0 1
Unchecked
CHEMBL612545
IC50 6.55 6.415 280.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34055221 10.1021/acsmedchemlett.0c00679 Unchecked 2
34055221 10.1021/acsmedchemlett.0c00679 TGF-beta receptor type-1 1

Data from ChEMBL 36 via Core Engine