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Compound Detail

CHEMBL4454044

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CC(C)c1cnn2c(NCc3ccccc3N(C)C)nc(OC3CCN(C)CC3)nc12

Basic Information

ChEMBL ID CHEMBL4454044
Phase Preclinical
Structure Type MOL
InChI Key JYPAWUMVEPMZMD-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

423.6
MW (Da)
3.40
ALogP
8
HBA
1
HBD
70.8
PSA (Ų)
0.62
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 C23H33N7O
MW 423.57
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.09

Activity Summary

IC50 6 meas. best 5.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
BT-549
CHEMBL614072
IC50 5.99 5.99 1030.0 1
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 5.41 5.41 3897.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.41 5.41 3900.0 1
Cyclin-dependent kinase 9
CHEMBL3116
IC50 5.13 5.13 7450.0 1
MDA-MB-468
CHEMBL614335
IC50 5.06 5.06 8780.0 1
MDA-MB-231
CHEMBL400
IC50 4.92 4.92 11890.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 2/cyclin E1 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 7 1
34538051 10.1021/acs.jmedchem.1c01350 MDA-MB-468 1
34538051 10.1021/acs.jmedchem.1c01350 BT-549 1
34538051 10.1021/acs.jmedchem.1c01350 MDA-MB-231 1

Data from ChEMBL 36 via Core Engine