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Compound Detail

CHEMBL2059819

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N#C[C@H]1C[C@@H]1CN([C@H](CCC(F)(F)F)C(N)=O)S(=O)(=O)c1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL2059819
Phase Preclinical
Structure Type MOL
InChI Key PPBDKFUHZARRNW-JTNHKYCSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

423.8
MW (Da)
2.69
ALogP
4
HBA
1
HBD
104.3
PSA (Ų)
0.69
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H17ClF3N3O3S
MW 423.84
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -1.11

Activity Summary

IC50 1 meas. best 8.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-secretase
CHEMBL2094135
IC50 8.16 8.16 6.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gamma-secretase IC50 = 6.92 nM 8.16 Inhibition of gamma secretase-mediated amyloid beta42 production in human H4 cel... 22420884

Literature References

PubMed DOI Target Context # Activities
22420884 10.1021/jm300094u ADMET 1
22420884 10.1021/jm300094u Liver microsomes 1
22420884 10.1021/jm300094u Gamma-secretase 1

Data from ChEMBL 36 via Core Engine