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Compound Detail

CHEMBL5204409

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Cc1ccccc1/C(=C\CCN1CCC[C@@H](C(=O)O)C1)c1sccc1C.Cl

Basic Information

ChEMBL ID CHEMBL5204409
Phase Preclinical
Structure Type MOL
InChI Key KKZCUEUXKVGHAR-NINVZRGFSA-N
Parent Compound CHEMBL5222684
Active Moiety CHEMBL5222684
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

369.5
MW (Da)
4.98
ALogP
3
HBA
1
HBD
40.5
PSA (Ų)
0.78
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28ClNO2S
MW 405.99
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.90

Activity Summary

IC50 1 meas. best 7.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.11 7.11 78.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 78.0 nM 7.11 Inhibition of GAT-mediated [3H]-GABA uptake in rat forebrain synaptosomes preinc... 35306287

Literature References

PubMed DOI Target Context # Activities
35306287 10.1016/j.ejmech.2022.114269 Unchecked 1
35306287 10.1016/j.ejmech.2022.114269 Mus musculus 1

Data from ChEMBL 36 via Core Engine