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Compound Detail

CHEMBL432715

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O=C1NC(=O)c2c1c1c3ccccc3[nH]c1c1[nH]c3c(Br)cccc3c21

Basic Information

ChEMBL ID CHEMBL432715
Phase Preclinical
Structure Type MOL
InChI Key KYWAFRQKAIEBNH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

404.2
MW (Da)
4.60
ALogP
2
HBA
3
HBD
77.8
PSA (Ų)
0.33
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H10BrN3O2
MW 404.22
Aromatic Rings 5
Heavy Atoms 26
NP-Likeness 0.27

Activity Summary

IC50 3 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CaM kinase II
CHEMBL2097164
IC50 4.96 4.96 11100.0 1
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 4.79 4.79 16200.0 1
Cyclin-dependent kinase 2/cyclin E
CHEMBL2094126
IC50 4.71 4.71 19400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12747775 10.1021/jm0256169 Cyclin-dependent kinase 4/cyclin D1 1
12747775 10.1021/jm0256169 Cyclin-dependent kinase 2/cyclin E 1
12747775 10.1021/jm0256169 Cyclin-dependent kinase 1/cyclin B 1
12747775 10.1021/jm0256169 CaM kinase II 1
12747775 10.1021/jm0256169 cAMP-dependent protein kinase (PKA) 1
12747775 10.1021/jm0256169 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine