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Compound Detail

CHEMBL383677

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CC(C)(O)c1ccn2c(-c3ccc(F)c(-c4ccncc4C#N)c3)cnc2n1

Basic Information

ChEMBL ID CHEMBL383677
Phase Preclinical
Structure Type MOL
InChI Key IQKMZIHHJYCEKH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

373.4
MW (Da)
3.70
ALogP
6
HBA
1
HBD
87.1
PSA (Ų)
0.59
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16FN5O
MW 373.39
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.21

Activity Summary

Ki 3 meas. best 9.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 9.85 9.85 0.1 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 9.55 9.55 0.3 1
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 9.22 9.22 0.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16386900 10.1016/j.bmcl.2005.12.044 GABA-A receptor; alpha-1/beta-3/gamma-2 2
16386900 10.1016/j.bmcl.2005.12.044 GABA-A receptor; alpha-3/beta-3/gamma-2 2
16386900 10.1016/j.bmcl.2005.12.044 GABA-A receptor; alpha-5/beta-3/gamma-2 1

Data from ChEMBL 36 via Core Engine