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Compound Detail

CHEMBL5179487

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C[C@@H]1N=C(c2ccccc2)c2cc(Br)ccc2NC1=O

Basic Information

ChEMBL ID CHEMBL5179487
Phase Preclinical
Structure Type MOL
InChI Key GAONFNHSQRTFJA-JTQLQIEISA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

329.2
MW (Da)
3.63
ALogP
2
HBA
1
HBD
41.5
PSA (Ų)
0.85
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H13BrN2O
MW 329.20
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.25

Activity Summary

Ki 4 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2
CHEMBL4523641
Ki 8.72 8.72 1.9 1
GABA A receptor alpha-2/beta-2/gamma-2
CHEMBL2111413
Ki 7.96 7.96 11.0 1
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095172
Ki 7.84 7.84 14.4 1
GABA A receptor alpha-3/beta-2/gamma-2
CHEMBL2111339
Ki 7.72 7.72 19.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35218882 10.1016/j.bmcl.2022.128637 GABA-A receptor; alpha-1/beta-2/gamma-2 1
35218882 10.1016/j.bmcl.2022.128637 GABA A receptor alpha-2/beta-2/gamma-2 1
35218882 10.1016/j.bmcl.2022.128637 GABA A receptor alpha-3/beta-2/gamma-2 1
35218882 10.1016/j.bmcl.2022.128637 Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 1
35218882 10.1016/j.bmcl.2022.128637 Unchecked 1

Data from ChEMBL 36 via Core Engine