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Compound Detail

CHEMBL1087152

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CC(C)c1ccc(NC(=O)Oc2ccc3c(c2)[C@]2(C)CCN(CCCc4ccccc4)[C@@H]2N3C)cc1

Basic Information

ChEMBL ID CHEMBL1087152
Phase Preclinical
Structure Type MOL
InChI Key UNNLLMSJDOVFCG-SMCANUKXSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

483.7
MW (Da)
6.79
ALogP
4
HBA
1
HBD
44.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H37N3O2
MW 483.66
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.09

Activity Summary

IC50 1 meas. best 6.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL2528
IC50 6.29 6.29 510.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 510.0 nM 6.29 Inhibition of mouse serum BChE after 1 hr by modified Ellman's colorimetric meth... 20137934

Literature References

PubMed DOI Target Context # Activities
20137934 10.1016/j.bmcl.2010.01.057 Acetylcholinesterase 1
20137934 10.1016/j.bmcl.2010.01.057 Cholinesterase 1
20137934 10.1016/j.bmcl.2010.01.057 Unchecked 1

Data from ChEMBL 36 via Core Engine