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Compound Detail

CHEMBL4787891

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COc1cn2ncc(-c3ccnc(OC4CCC4)c3)c2nc1-c1cnn(C)c1

Basic Information

ChEMBL ID CHEMBL4787891
Phase Preclinical
Structure Type MOL
InChI Key OORSHIMWGADFIS-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

376.4
MW (Da)
3.13
ALogP
8
HBA
0
HBD
79.4
PSA (Ų)
0.53
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 C20H20N6O2
MW 376.42
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.24

Activity Summary

IC50 3 meas. best 9.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-2
CHEMBL4267
IC50 9.21 9.21 0.6 1
Unchecked
CHEMBL612545
IC50 7.85 7.85 14.0 1
Activin receptor type-2A
CHEMBL5616
IC50 5.62 5.62 2400.0 1

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-2 1
34055221 10.1021/acsmedchemlett.0c00679 Activin receptor type-2A 1

Data from ChEMBL 36 via Core Engine