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Compound Detail

CHEMBL2059011

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N#C[C@H]1C[C@@H](CN([C@H](CCC(F)(F)F)C(N)=O)S(=O)(=O)c2ccc(Cl)cc2)C1

Basic Information

ChEMBL ID CHEMBL2059011
Phase Preclinical
Structure Type MOL
InChI Key DMINKKLAOYLYLD-TYNCELHUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

437.9
MW (Da)
3.08
ALogP
4
HBA
1
HBD
104.3
PSA (Ų)
0.67
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 C17H19ClF3N3O3S
MW 437.87
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -1.16

Activity Summary

IC50 1 meas. best 8.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-secretase
CHEMBL2094135
IC50 8.32 8.32 4.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gamma-secretase IC50 = 4.77 nM 8.32 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