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Compound Detail

CHEMBL1783263

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CCC(C)NC(=O)c1nnc2c(-c3cc(OC)ccc3OC)cccc2c1N

Basic Information

ChEMBL ID CHEMBL1783263
Phase Preclinical
Structure Type MOL
InChI Key RMNTXVHSVPDCSC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

380.4
MW (Da)
3.42
ALogP
6
HBA
2
HBD
99.4
PSA (Ų)
0.68
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24N4O3
MW 380.45
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.83

Activity Summary

Ki 1 meas. best 6.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-2/beta-3/gamma-2
CHEMBL2094130
Ki 6.27 6.27 537.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 9.4 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21498079 10.1016/j.bmc.2011.03.035 GABA-A receptor; alpha-2/beta-3/gamma-2 1
21498079 10.1016/j.bmc.2011.03.035 No relevant target 1
21498079 10.1016/j.bmc.2011.03.035 Liver microsomes 1

Data from ChEMBL 36 via Core Engine