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Compound Detail

CHEMBL180210

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CCCCN(C)C(=O)Cc1c(-c2ccc(Cl)cc2)nc2c(Cl)cc(Cl)cn12

Basic Information

ChEMBL ID CHEMBL180210
Phase Preclinical
Structure Type MOL
InChI Key DMYKDDKHSWCLSJ-UHFFFAOYSA-N
2
Targets
6
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

424.8
MW (Da)
5.76
ALogP
3
HBA
0
HBD
37.6
PSA (Ų)
0.50
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20Cl3N3O
MW 424.76
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.70

Activity Summary

IC50 3 meas. best 9.35
Ki 3 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Translocator protein
CHEMBL4552
Ki 9.52 9.065 0.3 2
Translocator protein
CHEMBL4552
IC50 9.35 8.915 0.4 2
GABA-A receptor; anion channel
CHEMBL1907607
Ki 5.16 5.16 6880.0 1
GABA-A receptor; anion channel
CHEMBL1907607
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15634024 10.1021/jm049610q Rattus norvegicus 6
15634024 10.1021/jm049610q Translocator protein 4
15634024 10.1021/jm049610q GABA-A receptor; anion channel 2
15634024 10.1021/jm049610q Benzodiazepine receptors; peripheral & central 2

Data from ChEMBL 36 via Core Engine