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Compound Detail

CHEMBL297390

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O=C(O)Cn1ccnc1

Basic Information

ChEMBL ID CHEMBL297390
Phase Preclinical
Structure Type MOL
InChI Key QAFBDRSXXHEXGB-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

126.1
MW (Da)
-0.03
ALogP
3
HBA
1
HBD
55.1
PSA (Ų)
0.60
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C5H6N2O2
MW 126.11
Aromatic Rings 1
Heavy Atoms 9
NP-Likeness -1.42

Activity Summary

IC50 3 meas. best 4.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA transporter 4
CHEMBL3699
IC50 4.37 4.37 42657.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA transporter 4 IC50 = 42657.95 nM 4.37 Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells 21353350

Literature References

PubMed DOI Target Context # Activities
21353350 10.1016/j.ejmech.2011.01.042 Unchecked 4
- 10.1016/S0960-894X(00)80463-1 No relevant target 1
21353350 10.1016/j.ejmech.2011.01.042 Sodium- and chloride-dependent GABA transporter 1 1
21353350 10.1016/j.ejmech.2011.01.042 GABA transporter 3 1
21353350 10.1016/j.ejmech.2011.01.042 GABA transporter 4 1

Data from ChEMBL 36 via Core Engine