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Compound Detail

CHEMBL4159574

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COCCOc1cnc(C(=O)Nc2ccc(F)c([C@@]3(C)N=C(N)CO[C@H]3C(F)(F)F)c2)cn1

Basic Information

ChEMBL ID CHEMBL4159574
Phase Preclinical
Structure Type MOL
InChI Key AANLQBIDWIHDGD-RTBURBONSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

471.4
MW (Da)
2.43
ALogP
8
HBA
2
HBD
121.0
PSA (Ų)
0.47
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21F4N5O4
MW 471.41
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.24

Activity Summary

IC50 2 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-secretase 1
CHEMBL4822
IC50 7.9 7.645 12.5 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29809004 10.1021/acs.jmedchem.8b00304 Beta-secretase 1 2
29809004 10.1021/acs.jmedchem.8b00304 ADMET 2

Data from ChEMBL 36 via Core Engine