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Compound Detail

CHEMBL322313

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Oc1c(-c2ccsc2)cnc2c(-c3cccc(C(F)(F)F)c3)cnn12

Basic Information

ChEMBL ID CHEMBL322313
Phase Preclinical
Structure Type MOL
InChI Key PEJYYKCLGNUTMG-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

361.4
MW (Da)
4.85
ALogP
5
HBA
1
HBD
50.4
PSA (Ų)
0.56
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H10F3N3OS
MW 361.35
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -2.00

Activity Summary

Ki 5 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL2094107
Ki 8.24 8.24 5.8 1
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095167
Ki 8.0 8.0 10.0 1
GABA A receptor alpha-3/beta-2/gamma-2
CHEMBL2111343
Ki 7.05 7.05 89.0 1
GABA A receptor alpha-5/beta-3/gamma-2
CHEMBL2111374
Ki 6.68 6.68 207.0 1
GABA A receptor alpha-2/beta-2/gamma-2
CHEMBL2111327
Ki 6.27 6.27 540.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12519068 10.1021/jm020999w Mus musculus 10
12519068 10.1021/jm020999w GABA-A receptor; anion channel 3
12519068 10.1021/jm020999w GABA-A receptor; alpha-1/beta-2/gamma-2 1
12519068 10.1021/jm020999w GABA A receptor alpha-2/beta-2/gamma-2 1
12519068 10.1021/jm020999w GABA A receptor alpha-3/beta-2/gamma-2 1
12519068 10.1021/jm020999w GABA A receptor alpha-5/beta-3/gamma-2 1

Data from ChEMBL 36 via Core Engine