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Compound Detail

CHEMBL210279

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O=S1(=O)NC[C@@H]2C[C@](c3cc(F)ccc3F)(S(=O)(=O)c3ccc(Cl)cc3)CC[C@@H]2N1

Basic Information

ChEMBL ID CHEMBL210279
Phase Preclinical
Structure Type MOL
InChI Key JWBIVRADHWRRRA-YXKWSERDSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

476.9
MW (Da)
2.89
ALogP
4
HBA
2
HBD
92.3
PSA (Ų)
0.71
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H19ClF2N2O4S2
MW 476.95
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.73

Activity Summary

IC50 1 meas. best 8.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-secretase
CHEMBL2094135
IC50 8.21 8.21 6.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gamma-secretase IC50 = 6.18 nM 8.21 Inhibition of gamma secretase 16617016

Literature References

PubMed DOI Target Context # Activities
16617016 10.1016/j.bmcl.2005.12.083 Liver microsomes 1
16617016 10.1016/j.bmcl.2005.12.083 Gamma-secretase 1

Data from ChEMBL 36 via Core Engine