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Compound Detail

CHEMBL3884250

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COc1cccc2[nH]c3c4ccncc4cc(C#N)c3c12

Basic Information

ChEMBL ID CHEMBL3884250
Phase Preclinical
Structure Type MOL
InChI Key DSISPBFCWKLZEA-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

273.3
MW (Da)
3.75
ALogP
3
HBA
1
HBD
61.7
PSA (Ų)
0.57
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H11N3O
MW 273.30
Aromatic Rings 4
Heavy Atoms 21
NP-Likeness -0.44

Activity Summary

IC50 4 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase CLK4
CHEMBL4203
IC50 7.0 7.0 100.0 1
Dual specificity protein kinase CLK1
CHEMBL4224
IC50 6.21 6.21 620.0 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
IC50 6.07 6.07 850.0 1
Dual specificity protein kinase CLK2
CHEMBL4225
IC50 5.4 5.4 4000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27676471 10.1016/j.ejmech.2016.08.069 Unchecked 1
27676471 10.1016/j.ejmech.2016.08.069 Cyclin-dependent kinase 5/CDK5 activator 1 1
27676471 10.1016/j.ejmech.2016.08.069 Glycogen synthase kinase-3 1
27676471 10.1016/j.ejmech.2016.08.069 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
27676471 10.1016/j.ejmech.2016.08.069 Dual specificity protein kinase CLK1 1
27676471 10.1016/j.ejmech.2016.08.069 Dual specificity tyrosine-phosphorylation-regulated kinase 1B 1
27676471 10.1016/j.ejmech.2016.08.069 Dual specificity protein kinase CLK2 1
27676471 10.1016/j.ejmech.2016.08.069 Dual specificity protein kinase CLK3 1
27676471 10.1016/j.ejmech.2016.08.069 Dual specificity protein kinase CLK4 1
27676471 10.1016/j.ejmech.2016.08.069 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine