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Compound Detail

CHEMBL202625

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Cc1cccc(-c2nn3c(c2-c2ccc4c(c2)ncn4CCCOC2CCCCO2)CCC3)n1

Basic Information

ChEMBL ID CHEMBL202625
Phase Preclinical
Structure Type MOL
InChI Key FEZFMQOPZJEIEX-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

457.6
MW (Da)
5.15
ALogP
7
HBA
0
HBD
67.0
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31N5O2
MW 457.58
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.04

Activity Summary

IC50 3 meas. best 5.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-1
CHEMBL4439
IC50 5.74 5.675 1830.0 2
TGF-beta receptor type-2
CHEMBL4267
IC50 4.84 4.84 14540.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16539403 10.1021/jm058209g TGF-beta receptor type-1 2
16539403 10.1021/jm058209g TGF-beta receptor type-2 1
16539403 10.1021/jm058209g Mitogen-activated protein kinase kinase kinase 20 1
16539403 10.1021/jm058209g Unchecked 1

Data from ChEMBL 36 via Core Engine