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Compound Detail

CHEMBL4649500

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Fc1ccc(C2CCCn3nc(N[C@@H]4[C@@H]5CC[C@H]4CN(c4ccnc(C(F)(F)F)c4)C5)nc32)c(F)c1F

Basic Information

ChEMBL ID CHEMBL4649500
Phase Preclinical
Structure Type MOL
InChI Key KXIPKBDNWGDNKQ-XYQMTRTISA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

522.5
MW (Da)
5.36
ALogP
6
HBA
1
HBD
58.9
PSA (Ų)
0.37
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24F6N6
MW 522.50
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.97

Activity Summary

IC50 1 meas. best 7.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-secretase
CHEMBL2094135
IC50 7.36 7.36 44.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gamma-secretase IC50 = 44.0 nM 7.36 Modulation of gamma secretase in human H4 cells overexpressing human APP695 harb... 32551009

Literature References

PubMed DOI Target Context # Activities
32551009 10.1021/acsmedchemlett.0c00109 Gamma-secretase 1

Data from ChEMBL 36 via Core Engine