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Compound Detail

CHEMBL399696

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CC(=O)Nc1nc(C)c(S(=O)(=O)Oc2cccc3c2[nH]c2c(C4=C[C@@]5(O)CC/C=C\CCCCN6CCC4[C@]4(C[C@@H]7CCC(=O)CCCN7[C@H]45)C6)nccc23)s1

Basic Information

ChEMBL ID CHEMBL399696
Phase Preclinical
Structure Type MOL
InChI Key IMHUMQBLODOEBB-PFZFYGFTSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

799.0
MW (Da)
6.75
ALogP
11
HBA
3
HBD
157.8
PSA (Ų)
0.15
QED
3
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H50N6O6S2
MW 799.03
Aromatic Rings 4
Heavy Atoms 56
NP-Likeness 1.09

Activity Summary

IC50 1 meas. best 5.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 5.07 5.07 8500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glycogen synthase kinase-3 beta IC50 = 8500.0 nM 5.07 Inhibition of human recombinant GSKbeta 17708655

Literature References

PubMed DOI Target Context # Activities
17708655 10.1021/np060092r Glycogen synthase kinase-3 beta 2

Data from ChEMBL 36 via Core Engine