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Compound Detail

CHEMBL461556

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CC[C@H](CO)Nc1nc(NCc2ccc(-c3ccncc3)cc2)c2ncn(C(C)C)c2n1

Basic Information

ChEMBL ID CHEMBL461556
Phase Preclinical
Structure Type MOL
InChI Key UQRBOMYWGJFNEB-HXUWFJFHSA-N
5
Targets
7
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

431.5
MW (Da)
4.26
ALogP
8
HBA
3
HBD
100.8
PSA (Ų)
0.36
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N7O
MW 431.54
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.73

Activity Summary

IC50 6 meas. best 5.96
EC50 1 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK12/Cyclin K
CHEMBL4106169
EC50 7.44 7.44 36.0 1
Unchecked
CHEMBL612545
IC50 5.96 5.7533 1100.0 3
HEK293
CHEMBL614818
IC50 5.81 5.81 1540.0 1
SH-SY5Y
CHEMBL614910
IC50 5.77 5.77 1690.0 1
Glycogen synthase kinase-3
CHEMBL2366565
IC50 4.45 4.45 35500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18698753 10.1021/jm800109e Unchecked 3
18698753 10.1021/jm800109e Glycogen synthase kinase-3 1
18698753 10.1021/jm800109e SH-SY5Y 1
18698753 10.1021/jm800109e HEK293 1
38579492 10.1016/j.bmc.2024.117653 CDK12/Cyclin K 1

Data from ChEMBL 36 via Core Engine