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Compound Detail

CHEMBL4635959

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Cc1cc(NC2CCN(C(=O)O[C@H]3CCN(C(=O)/C=C/CN(C)C)C3)CC2)n2ncc(C(C)C)c2n1

Basic Information

ChEMBL ID CHEMBL4635959
Phase Preclinical
Structure Type MOL
InChI Key GRDAHPJRLCTJNA-BXKJMJEDSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

497.6
MW (Da)
2.89
ALogP
8
HBA
1
HBD
95.3
PSA (Ų)
0.59
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 C26H39N7O3
MW 497.64
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -1.15

Activity Summary

IC50 3 meas. best 6.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 7
CHEMBL3055
IC50 6.83 6.83 148.0 1
Cyclin-dependent kinase 4
CHEMBL331
IC50 5.55 5.55 2830.0 1
Cyclin-dependent kinase 9
CHEMBL3116
IC50 5.2 5.2 6320.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 9 2
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 7 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 1 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 2 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 4 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 6 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 8 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 12 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 13 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 18 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 19 1

Data from ChEMBL 36 via Core Engine