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Compound Detail

CHEMBL252672

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Oc1ccc2[nH]c3c(C4=C[C@@]5(O)CC/C=C\CCCCN6CCC4[C@]4(C[C@@H]7/C=C\CCCCN7[C@H]45)C6)nccc3c2c1

Basic Information

ChEMBL ID CHEMBL252672
Phase Preclinical
Structure Type MOL
InChI Key CANRNZBVKKQKEQ-DIFNJBIASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

564.8
MW (Da)
6.56
ALogP
5
HBA
3
HBD
75.6
PSA (Ų)
0.29
QED
2
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C36H44N4O2
MW 564.77
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness 2.17

Activity Summary

IC50 1 meas. best 4.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 4.78 4.78 16600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glycogen synthase kinase-3 beta IC50 = 16600.0 nM 4.78 Inhibition of human recombinant GSKbeta 17708655

Literature References

PubMed DOI Target Context # Activities
17708655 10.1021/np060092r Glycogen synthase kinase-3 beta 2
7714542 10.1021/np50114a021 Micrococcus luteus 1
7714542 10.1021/np50114a021 L1210 1
7714542 10.1021/np50114a021 KB 1
23665143 10.1016/j.bmc.2013.04.025 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine