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Compound Detail

CHEMBL4091127

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COc1ccc2ncc(/C=C/c3cccc(C(F)(F)F)c3)n2n1

Basic Information

ChEMBL ID CHEMBL4091127
Phase Preclinical
Structure Type MOL
InChI Key JNNGGJDFTJICDZ-AATRIKPKSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

319.3
MW (Da)
3.93
ALogP
4
HBA
0
HBD
39.4
PSA (Ų)
0.73
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H12F3N3O
MW 319.29
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.52

Activity Summary

IC50 4 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase CLK4
CHEMBL1075283
IC50 6.66 6.66 220.0 1
Dual specificity protein kinase CLK1
CHEMBL1075280
IC50 6.29 6.29 510.0 1
Dual specificity protein kinase CLK2
CHEMBL1075281
IC50 6.05 6.05 890.0 1
Unchecked
CHEMBL612545
IC50 5.19 5.19 6400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27721154 10.1016/j.ejmech.2016.09.064 Unchecked 14
27721154 10.1016/j.ejmech.2016.09.064 Leishmania amazonensis 3
27721154 10.1016/j.ejmech.2016.09.064 SH-SY5Y 2
27721154 10.1016/j.ejmech.2016.09.064 CDK2/Cyclin A2 1
27721154 10.1016/j.ejmech.2016.09.064 Cyclin-dependent kinase 5/CDK5 activator 1 1
27721154 10.1016/j.ejmech.2016.09.064 CDK9/cyclin T1 1
27721154 10.1016/j.ejmech.2016.09.064 Dual specificity protein kinase CLK1 1
27721154 10.1016/j.ejmech.2016.09.064 Dual specificity protein kinase CLK2 1
27721154 10.1016/j.ejmech.2016.09.064 Dual specificity protein kinase CLK3 1
27721154 10.1016/j.ejmech.2016.09.064 Dual specificity protein kinase CLK4 1
27721154 10.1016/j.ejmech.2016.09.064 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
27721154 10.1016/j.ejmech.2016.09.064 Dual specificity tyrosine-phosphorylation-regulated kinase 1B 1
27721154 10.1016/j.ejmech.2016.09.064 Dual specificity tyrosine-phosphorylation-regulated kinase 2 1
27721154 10.1016/j.ejmech.2016.09.064 Dual specificity tyrosine-phosphorylation-regulated kinase 3 1

Data from ChEMBL 36 via Core Engine