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Compound Detail

CHEMBL3657428

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CC1=N[C@]2(N=C1N)c1cc(-c3cc(F)cc(C#N)c3)ccc1C[C@]21CC[C@@H](OC(F)F)CC1

Basic Information

ChEMBL ID CHEMBL3657428
Phase Preclinical
Structure Type MOL
InChI Key PGKOVKXDONQGMH-OPXMRZJTSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

452.5
MW (Da)
5.07
ALogP
5
HBA
1
HBD
83.8
PSA (Ų)
0.71
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 C25H23F3N4O
MW 452.48
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.15

Activity Summary

IC50 1 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-secretase 1
CHEMBL4822
IC50 7.66 7.66 22.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-secretase 1 IC50 = 22.0 nM 7.66 TR-FRET Assay: The beta-secretase enzyme used in the TR-FRET is prepared as foll... -

Data from ChEMBL 36 via Core Engine