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Compound Detail

CHEMBL468083

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O=S1(=O)N[C@@]2(CN1CC(F)(F)F)[C@@H]1CC[C@H]2Cc2ccc(-c3cn(-c4ccc(F)cc4)cn3)cc2C1

Basic Information

ChEMBL ID CHEMBL468083
Phase Preclinical
Structure Type MOL
InChI Key IPBZZTDOABSBMR-DCLXLUIPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

520.5
MW (Da)
4.25
ALogP
4
HBA
1
HBD
67.2
PSA (Ų)
0.53
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 C25H24F4N4O2S
MW 520.55
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.77

Activity Summary

IC50 1 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-secretase
CHEMBL2094135
IC50 10.52 10.52 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gamma-secretase IC50 = 0.03 nM 10.52 Inhibition of gamma secretase in human SH-SY5Y cells by HTRF assay 19432431

Literature References

PubMed DOI Target Context # Activities
19432431 10.1021/jm900056p Gamma-secretase 1
19432431 10.1021/jm900056p Mus musculus 1

Data from ChEMBL 36 via Core Engine