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Compound Detail

CHEMBL301010

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COc1ccc(-c2cc(C#N)c(=O)n(C)c2-c2ccc(N(C)C)cc2)cc1

Basic Information

ChEMBL ID CHEMBL301010
Phase Preclinical
Structure Type MOL
InChI Key XBMDFRQPTGJXHL-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

359.4
MW (Da)
3.67
ALogP
5
HBA
0
HBD
58.3
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21N3O2
MW 359.43
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.76

Activity Summary

Ki 3 meas. best 6.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 6.07 6.07 860.0 1
GABA-A receptor; alpha-2/beta-3/gamma-2
CHEMBL2094130
Ki 5.75 5.75 1800.0 1
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 5.16 5.16 7000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11960500 10.1021/jm0110789 GABA-A receptor; alpha-1/beta-3/gamma-2 2
11960500 10.1021/jm0110789 GABA-A receptor; alpha-2/beta-3/gamma-2 2
11960500 10.1021/jm0110789 GABA-A receptor; alpha-3/beta-3/gamma-2 2
11960500 10.1021/jm0110789 GABA-A receptor; alpha-5/beta-3/gamma-2 1

Data from ChEMBL 36 via Core Engine