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Compound Detail

CHEMBL277584

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C[C@@H]1CN(C(=O)N2c3cc(Cl)ccc3-n3cnc(C(=O)OC(C)(C)C)c3C2(C)C)C[C@H](C)N1

Basic Information

ChEMBL ID CHEMBL277584
Phase Preclinical
Structure Type MOL
InChI Key RJCIQNZZLSAFJT-GASCZTMLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

474.0
MW (Da)
4.34
ALogP
6
HBA
1
HBD
79.7
PSA (Ų)
0.62
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H32ClN5O3
MW 474.01
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.41

Activity Summary

Ki 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 7.7 7.7 19.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10197957 10.1021/jm9801307 GABA-A receptor; anion channel 3
10197957 10.1021/jm9801307 Mus musculus 2
10197957 10.1021/jm9801307 Rattus norvegicus 1
10197957 10.1021/jm9801307 GABA-A receptor; alpha-1/beta-2/gamma-2 1
10197957 10.1021/jm9801307 GABA A receptor alpha-3/beta-2/gamma-2 1

Data from ChEMBL 36 via Core Engine