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Compound Detail

CHEMBL379668

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COc1cc2c(c(Cl)c1Cl)C(=O)C(CCN(C)[C@@H](C)C(=O)O)(c1ccccc1)C2=O

Basic Information

ChEMBL ID CHEMBL379668
Phase Preclinical
Structure Type MOL
InChI Key LVLIPXUTHJTYCL-BJDAYTSDSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

450.3
MW (Da)
4.11
ALogP
5
HBA
1
HBD
83.9
PSA (Ų)
0.64
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21Cl2NO5
MW 450.32
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness 0.14

Activity Summary

IC50 1 meas. best 9.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium- and chloride-dependent glycine transporter 1
CHEMBL2337
IC50 9.33 9.33 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16321523 10.1016/j.bmcl.2005.11.041 Sodium- and chloride-dependent glycine transporter 1 1
16321523 10.1016/j.bmcl.2005.11.041 Voltage-gated inwardly rectifying potassium channel KCNH2 1
16321523 10.1016/j.bmcl.2005.11.041 5-hydroxytryptamine receptor 1A 1
16321523 10.1016/j.bmcl.2005.11.041 5-hydroxytryptamine receptor 2A 1
16321523 10.1016/j.bmcl.2005.11.041 D(2) dopamine receptor 1
16321523 10.1016/j.bmcl.2005.11.041 Sodium- and chloride-dependent glycine transporter 2 1

Data from ChEMBL 36 via Core Engine