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Compound Detail

CHEMBL210587

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O=S1(=O)N[C@H]2CC[C@@](c3cc(F)ccc3F)(S(=O)(=O)c3ccc(Cl)cc3)C[C@H]2CN1C1CC1

Basic Information

ChEMBL ID CHEMBL210587
Phase Preclinical
Structure Type MOL
InChI Key REFFKKGLZVSMFQ-JQOQJDEVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

517.0
MW (Da)
3.77
ALogP
4
HBA
1
HBD
83.5
PSA (Ų)
0.67
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23ClF2N2O4S2
MW 517.02
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.79

Activity Summary

IC50 1 meas. best 9.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-secretase
CHEMBL2094135
IC50 9.72 9.72 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gamma-secretase IC50 = 0.19 nM 9.72 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