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Compound Detail

CHEMBL14805

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CC(C)(C)OC(=O)c1ncn2c1CN(C(=O)N1CCCC1)c1cc(Cl)ccc1-2.CCCC(=O)O

Basic Information

ChEMBL ID CHEMBL14805
Phase Preclinical
Structure Type MOL
InChI Key MCGVESKBPTWUNU-UHFFFAOYSA-N
Parent Compound CHEMBL1178194
Active Moiety CHEMBL1178194
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

402.9
MW (Da)
4.02
ALogP
5
HBA
0
HBD
67.7
PSA (Ų)
0.68
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 C24H31ClN4O5
MW 490.99
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.86

Activity Summary

Ki 1 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 8.59 8.59 2.6 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3680.0 ng.hr.mL-1 Rattus norvegicus
Cmax 819.1 nM Rattus norvegicus
T1/2 7.6 hr Rattus norvegicus
Tmax 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10197957 10.1021/jm9801307 Rattus norvegicus 5
10197957 10.1021/jm9801307 Mus musculus 3
10197957 10.1021/jm9801307 GABA-A receptor; anion channel 2
10197957 10.1021/jm9801307 GABA-A receptor; alpha-1/beta-2/gamma-2 1

Data from ChEMBL 36 via Core Engine