Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL1271703

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CC(C)[C@@H]1COC[C@H](C2(OC(=O)N3CCNCC3)CC2)N1S(=O)(=O)c1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL1271703
Phase Preclinical
Structure Type MOL
InChI Key MELKFGZURAGNSX-RBUKOAKNSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

472.0
MW (Da)
2.33
ALogP
6
HBA
1
HBD
88.2
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H30ClN3O5S
MW 472.01
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness -0.42

Activity Summary

IC50 2 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 3A4
CHEMBL340
IC50 9.52 9.52 0.3 1
Unchecked
CHEMBL612545
IC50 7.84 7.84 14.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1854.06 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 3A4 IC50 = 0.3 nM 9.52 Inhibition of CYP3A4 after 30 mins 20933414
Unchecked IC50 = 14.5 nM 7.84 Inhibition of gamma-secretase-mediated amyloid beta-40 production 20933414

Literature References

PubMed DOI Target Context # Activities
20933414 10.1016/j.bmcl.2010.09.028 Unchecked 1
20933414 10.1016/j.bmcl.2010.09.028 Cytochrome P450 3A4 1
20933414 10.1016/j.bmcl.2010.09.028 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine