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Compound Detail

CHEMBL411901

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CCn1cnc2c(N)nc(N(c3cccc(Cl)c3)[C@@H]3CCCC[C@@H]3N)nc21

Basic Information

ChEMBL ID CHEMBL411901
Phase Preclinical
Structure Type MOL
InChI Key JHLFDBSTLNYPFS-LSDHHAIUSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

385.9
MW (Da)
3.49
ALogP
7
HBA
2
HBD
98.9
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H24ClN7
MW 385.90
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.89

Activity Summary

IC50 3 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.6 7.6 25.0 1
Protein kinase C alpha type
CHEMBL299
IC50 5.21 5.21 6100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 25.0 nM 7.6 Inhibition of Cdk1/cyclin B 18077363
Protein kinase C alpha type IC50 = 6100.0 nM 5.21 Inhibition of PKCalpha 18077363

Literature References

PubMed DOI Target Context # Activities
18077363 10.1073/pnas.0708800104 Serine/threonine-protein kinase 26 2
18077363 10.1073/pnas.0708800104 Ribosomal protein S6 kinase alpha-3 2
18077363 10.1073/pnas.0708800104 Unchecked 2
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit beta 1
18077363 10.1073/pnas.0708800104 Serine/threonine-protein kinase Chk2 1
18077363 10.1073/pnas.0708800104 Cyclin-dependent kinase-like 1 1
18077363 10.1073/pnas.0708800104 Serine/threonine-protein kinase 25 1
18077363 10.1073/pnas.0708800104 Cyclin-dependent kinase 2 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase kinase 2 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type IV 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit gamma 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit delta 1
10633033 10.1021/jm991182e Cyclin-dependent kinase 1/cyclin B 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit alpha 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type 1G 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type 1D 1
18077363 10.1073/pnas.0708800104 5'-AMP-activated protein kinase catalytic subunit alpha-2 1
18077363 10.1073/pnas.0708800104 Protein kinase C alpha type 1
18077363 10.1073/pnas.0708800104 Epidermal growth factor receptor 1
10633033 10.1021/jm991182e Cyclin-dependent kinase 4/cyclin D 1

Data from ChEMBL 36 via Core Engine