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Compound Detail

CHEMBL1451229

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Cc1nnc2n1-c1ccc(Br)cc1C(c1ccccc1Cl)=NC2

Basic Information

ChEMBL ID CHEMBL1451229
Phase Preclinical
Structure Type MOL
InChI Key BUTCFAZTKZDYCN-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

387.7
MW (Da)
4.34
ALogP
4
HBA
0
HBD
43.1
PSA (Ų)
0.62
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H12BrClN4
MW 387.67
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.84

Activity Summary

Ki 4 meas. best 9.4

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 9.4 9.4 0.4 1
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095172
Ki 9.3 9.3 0.5 1
GABA A receptor alpha-3/beta-2/gamma-2
CHEMBL2111339
Ki 9.22 9.22 0.6 1
GABA A receptor alpha-2/beta-2/gamma-2
CHEMBL2111413
Ki 9.0 9.0 1.0 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

Data from ChEMBL 36 via Core Engine