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Compound Detail

CHEMBL523435

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COc1cccc2c(C3=C(c4cn(C)c5cc(I)c(F)cc45)C(=O)NC3=O)coc12

Basic Information

ChEMBL ID CHEMBL523435
Phase Preclinical
Structure Type MOL
InChI Key JBKILIGSDAQHSL-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

516.3
MW (Da)
4.24
ALogP
5
HBA
1
HBD
73.5
PSA (Ų)
0.33
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H14FIN2O4
MW 516.27
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.19

Activity Summary

IC50 5 meas. best 6.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 6.61 6.61 247.0 2
HuP-T3
CHEMBL1075477
IC50 6.22 6.22 600.0 1
MIA PaCa-2
CHEMBL614725
IC50 6.22 6.22 600.0 1
BXPC-3
CHEMBL614530
IC50 6.05 6.05 900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19338355 10.1021/jm801317h BXPC-3 3
19338355 10.1021/jm801317h Glycogen synthase kinase-3 beta 2
19338355 10.1021/jm801317h Cyclin-dependent kinase 2 2
19338355 10.1021/jm801317h MIA PaCa-2 1
19338355 10.1021/jm801317h HuP-T3 1
19338355 10.1021/jm801317h Cyclin-dependent kinase 1/cyclin B1 1
19338355 10.1021/jm801317h RAC-gamma serine/threonine-protein kinase 1
19338355 10.1021/jm801317h Serine/threonine-protein kinase Chk1 1
19338355 10.1021/jm801317h RAF proto-oncogene serine/threonine-protein kinase 1
19338355 10.1021/jm801317h Mitogen-activated protein kinase 3 1
19338355 10.1021/jm801317h Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
19338355 10.1021/jm801317h Inhibitor of nuclear factor kappa-B kinase subunit beta 1
37536264 10.1016/j.bmc.2023.117406 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine