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Compound Detail

CHEMBL4562323

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CC(C)c1cnn2c(NCc3ccccc3-n3cccn3)nc(OC3CCCNC3)nc12

Basic Information

ChEMBL ID CHEMBL4562323
Phase Preclinical
Structure Type MOL
InChI Key LSGRZENCFIIHNV-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
3.18
ALogP
9
HBA
2
HBD
94.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28N8O
MW 432.53
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.51

Activity Summary

IC50 4 meas. best 9.89
EC50 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 7
CHEMBL3055
IC50 9.89 9.89 0.1 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 8.19 8.19 6.4 1
Human betaherpesvirus 5
CHEMBL371
EC50 7.62 7.62 24.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 7.28 7.28 53.0 1
Cyclin-dependent kinase 9
CHEMBL3116
IC50 5.77 5.77 1711.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33539089 10.1021/acs.jmedchem.0c01467 Cyclin-dependent kinase 7 2
31514062 10.1016/j.ejmech.2019.111641 Cyclin-dependent kinase 7 1
31514062 10.1016/j.ejmech.2019.111641 Cyclin-dependent kinase 1 1
31514062 10.1016/j.ejmech.2019.111641 Cyclin-dependent kinase 2 1
31514062 10.1016/j.ejmech.2019.111641 Cyclin-dependent kinase 4 1
31514062 10.1016/j.ejmech.2019.111641 Cyclin-dependent kinase 6 1
31514062 10.1016/j.ejmech.2019.111641 Cyclin-dependent kinase 9 1
33539089 10.1021/acs.jmedchem.0c01467 Human betaherpesvirus 5 1
33539089 10.1021/acs.jmedchem.0c01467 HFF 1

Data from ChEMBL 36 via Core Engine