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Compound Detail

CHEMBL458147

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Cn1c(=O)c2cc(Cl)ccc2n2cnc(C(=O)OC(C)(C)C)c12

Basic Information

ChEMBL ID CHEMBL458147
Phase Preclinical
Structure Type MOL
InChI Key OVFRNPXWYQUNHR-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

333.8
MW (Da)
2.79
ALogP
6
HBA
0
HBD
65.6
PSA (Ų)
0.64
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 C16H16ClN3O3
MW 333.78
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.06

Activity Summary

Ki 2 meas. best 9.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid receptor subunit alpha-5
CHEMBL5112
Ki 9.19 9.19 0.7 1
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 7.76 7.76 17.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18537233 10.1021/jm701433b GABA-A receptor; alpha-1/beta-3/gamma-2 1
18537233 10.1021/jm701433b Gamma-aminobutyric acid receptor subunit alpha-5 1

Data from ChEMBL 36 via Core Engine