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Compound Detail

CHEMBL203768

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FC(F)(F)c1ccn2c(-c3cccc(Br)n3)cnc2n1

Basic Information

ChEMBL ID CHEMBL203768
Phase Preclinical
Structure Type MOL
InChI Key KMGQMDWTLIZLHG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

343.1
MW (Da)
3.57
ALogP
4
HBA
0
HBD
43.1
PSA (Ų)
0.63
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 C12H6BrF3N4
MW 343.11
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -1.67

Activity Summary

Ki 2 meas. best 9.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 9.51 9.51 0.3 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 9.17 9.17 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16406613 10.1016/j.bmcl.2005.11.112 GABA-A receptor; alpha-1/beta-3/gamma-2 2
16406613 10.1016/j.bmcl.2005.11.112 GABA-A receptor; alpha-3/beta-3/gamma-2 2

Data from ChEMBL 36 via Core Engine