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Compound Detail

CHEMBL3753782

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COc1cccc2[nH]cc(/C(C#N)=C/c3cccnc3)c12

Basic Information

ChEMBL ID CHEMBL3753782
Phase Preclinical
Structure Type MOL
InChI Key YEKNWHPJYYLTRW-MDWZMJQESA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

275.3
MW (Da)
3.64
ALogP
3
HBA
1
HBD
61.7
PSA (Ų)
0.74
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 C17H13N3O
MW 275.31
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -0.88

Activity Summary

IC50 4 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase CLK1
CHEMBL4224
IC50 5.52 5.52 3000.0 1
Kinesin-like protein KIF20A
CHEMBL2021753
IC50 5.48 5.43 3300.0 2
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
IC50 5.22 5.22 6000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26778612 10.1016/j.bmc.2015.12.042 Kinesin-like protein KIF20A 4
26778612 10.1016/j.bmc.2015.12.042 Unchecked 2
26778612 10.1016/j.bmc.2015.12.042 KB 2
26778612 10.1016/j.bmc.2015.12.042 Centromere-associated protein E 1
26778612 10.1016/j.bmc.2015.12.042 Chromosome-associated kinesin KIF4A 1
26778612 10.1016/j.bmc.2015.12.042 Kinesin-like protein KIF11 1
26778612 10.1016/j.bmc.2015.12.042 Kinesin-like protein KIFC3 1
26778612 10.1016/j.bmc.2015.12.042 Kinesin-like protein KIF3C 1
26778612 10.1016/j.bmc.2015.12.042 Kinesin-like protein KIF23 1
26778612 10.1016/j.bmc.2015.12.042 Kinesin-1 heavy chain 1
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

Data from ChEMBL 36 via Core Engine