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Compound Detail

CHEMBL5753347

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CC1=N[C@@]2(CC([C@H]3CCOC(C)(C)C3)Oc3ccc(-c4cccc(Cl)c4)cc32)N=C1N

Basic Information

ChEMBL ID CHEMBL5753347
Phase Preclinical
Structure Type MOL
InChI Key PNGMSULGCSIWPT-YHLDMFKXSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

438.0
MW (Da)
5.35
ALogP
5
HBA
1
HBD
69.2
PSA (Ų)
0.69
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H28ClN3O2
MW 437.97
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness 0.16

Activity Summary

IC50 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-secretase 1
CHEMBL4822
IC50 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-secretase 1 IC50 = 5.0 nM 8.3 FRET Assay: The enzyme (truncated form) was diluted to 6 μg/mL (stock 1.3 mg/mL)... -

Data from ChEMBL 36 via Core Engine