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Compound Detail

CHEMBL324194

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O=C(CC[C@@H]1N=C(c2ccccc2)c2cc([N+](=O)[O-])ccc2NC1=O)OCc1ccccc1

Basic Information

ChEMBL ID CHEMBL324194
Phase Preclinical
Structure Type MOL
InChI Key PTRYBRYZCRKBRP-QFIPXVFZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

443.5
MW (Da)
4.28
ALogP
6
HBA
1
HBD
110.9
PSA (Ų)
0.33
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H21N3O5
MW 443.46
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.47

Activity Summary

Ki 1 meas. best 6.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 6.91 6.91 124.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA-A receptor; anion channel Ki = 124.0 nM 6.91 Binding affinity to rat benzodiazepine receptor 12372537

Literature References

PubMed DOI Target Context # Activities
12372537 10.1016/s0960-894x(02)00512-7 GABA-A receptor; anion channel 2
12372537 10.1016/s0960-894x(02)00512-7 Rattus norvegicus 2

Data from ChEMBL 36 via Core Engine