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Compound Detail

CHEMBL1722444

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Cc1ccc(-n2nc(C)c3c2C(Br)C(C)(C)CC3=O)nc1

Basic Information

ChEMBL ID CHEMBL1722444
Phase Preclinical
Structure Type MOL
InChI Key RTCMKAHTBJUOFR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

348.2
MW (Da)
3.93
ALogP
4
HBA
0
HBD
47.8
PSA (Ų)
0.73
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H18BrN3O
MW 348.24
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -0.79

Activity Summary

IC50 1 meas. best 5.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK2/Cyclin A2
CHEMBL3038469
IC50 5.12 5.12 7500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK2/Cyclin A2 IC50 = 7500.0 nM 5.12 Inhibition of human N-terminal GST-tagged CDK2 (1 to 298 residues)/Cyclin A (174... 33550184

Literature References

PubMed DOI Target Context # Activities
33550184 10.1016/j.ejmech.2021.113232 CDK2/Cyclin A2 1

Data from ChEMBL 36 via Core Engine