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Compound Detail

CHEMBL4744964

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CN1CC[C@]2(O)c3ccccc3N(C)[C@]12c1ccccc1

Basic Information

ChEMBL ID CHEMBL4744964
Phase Preclinical
Structure Type MOL
InChI Key BMDBRSCYSSXTIY-ROUUACIJSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

280.4
MW (Da)
2.51
ALogP
3
HBA
1
HBD
26.7
PSA (Ų)
0.87
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20N2O
MW 280.37
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness 0.78

Activity Summary

EC50 2 meas. best 4.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; GABA-A site (alpha1/beta2 interface)
CHEMBL1907597
EC50 4.89 4.89 13000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33214830 10.1021/acsmedchemlett.0c00340 GABA-A receptor; alpha-1/beta-2/gamma-2 6
33214830 10.1021/acsmedchemlett.0c00340 Unchecked 4
33214830 10.1021/acsmedchemlett.0c00340 GABA-A receptor; GABA-A site (alpha1/beta2 interface) 3

Data from ChEMBL 36 via Core Engine