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Compound Detail

CHEMBL557400

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CC(C)c1ccc(NC(=O)Oc2ccc3c(c2)[C@]2(C)CC[N@@+](C)([O-])[C@@H]2N3C)cc1.Cl

Basic Information

ChEMBL ID CHEMBL557400
Phase Preclinical
Structure Type MOL
InChI Key IETHGPWOHFZAIP-OUOGWCTJSA-N
Parent Compound CHEMBL1196559
Active Moiety CHEMBL1196559
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

395.5
MW (Da)
4.80
ALogP
4
HBA
1
HBD
64.6
PSA (Ų)
0.60
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 C23H30ClN3O3
MW 431.96
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness 0.11

Activity Summary

IC50 1 meas. best 5.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 5.28 5.28 5200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 5200.0 nM 5.28 Ex vivo inhibition of human plasma Butyrylcholinesterase. 12166941

Literature References

PubMed DOI Target Context # Activities
12166941 10.1021/jm010491d Acetylcholinesterase 1
12166941 10.1021/jm010491d Cholinesterase 1
12166941 10.1021/jm010491d Cholinesterases; ACHE & BCHE 1

Data from ChEMBL 36 via Core Engine