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Compound Detail

CHEMBL2321961

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COC(=O)c1ccc2c(c1)NC(=C1\C(=O)Nc3c1cccc3C(F)(F)F)/C2=N/O

Basic Information

ChEMBL ID CHEMBL2321961
Phase Preclinical
Structure Type MOL
InChI Key DFJOHBMOVLHZCW-YIYUENNCSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

403.3
MW (Da)
3.46
ALogP
6
HBA
3
HBD
100.0
PSA (Ų)
0.29
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 C19H12F3N3O4
MW 403.32
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.24

Activity Summary

IC50 4 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase 3 beta
CHEMBL1909485
IC50 7.0 7.0 100.0 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL5508
IC50 6.96 6.96 110.0 1
Cyclin-dependent kinase 5
CHEMBL4036
IC50 5.77 5.77 1700.0 1
Casein kinase I isoform alpha
CHEMBL1781858
IC50 5.3 5.3 5000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27726390 10.1021/acs.jnatprod.6b00285 KCL-22 2
23336033 10.1021/ml300207a Dual specificity tyrosine-phosphorylation-regulated kinase 2 1
23336033 10.1021/ml300207a Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
23336033 10.1021/ml300207a Casein kinase I isoform alpha 1
23336033 10.1021/ml300207a Glycogen synthase kinase 3 beta 1
23336033 10.1021/ml300207a Cyclin-dependent kinase 5 1

Data from ChEMBL 36 via Core Engine