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Compound Detail

CHEMBL54338

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O=C(OCC1CC1)c1ncn2c1C1CCN1C(=O)c1c(Cl)cccc1-2

Basic Information

ChEMBL ID CHEMBL54338
Phase Preclinical
Structure Type MOL
InChI Key HFTSPQUXYIMHAN-UHFFFAOYSA-N

Known Names

Ro-171812
1
Targets
3
Activities
2
Assay Types
0
PK Parameters
2
Publications
1
Known Names

Molecular Properties

357.8
MW (Da)
2.99
ALogP
5
HBA
0
HBD
64.4
PSA (Ų)
0.79
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 C18H16ClN3O3
MW 357.80
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.74

Activity Summary

Ki 2 meas. best 10.0
IC50 1 meas. best 8.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 10.0 8.63 0.1 2
GABA-A receptor; anion channel
CHEMBL1907607
IC50 8.38 8.38 4.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8390574 10.1021/jm00065a004 GABA-A receptor; anion channel 3
2552115 10.1021/jm00130a010 GABA-A receptor; anion channel 2

Data from ChEMBL 36 via Core Engine