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Compound Detail

CHEMBL3088055

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COc1cccc(O[C@H]2CC[C@H]3CN[C@H](C(=O)O)C[C@H]3C2)c1-c1nnn[nH]1.Cl

Basic Information

ChEMBL ID CHEMBL3088055
Phase Preclinical
Structure Type MOL
InChI Key DNGURPAMLKIZKQ-BYVSKJIISA-N
Parent Compound CHEMBL3139492
Active Moiety CHEMBL3139492
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

373.4
MW (Da)
1.49
ALogP
7
HBA
3
HBD
122.2
PSA (Ų)
0.72
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H24ClN5O4
MW 409.87
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness 0.28

Activity Summary

Ki 2 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, kainate 1
CHEMBL1918
Ki 5.96 5.96 1100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutamate receptor ionotropic, kainate 1 Ki = 1100.0 nM 5.96 Displacement of [3H]ATPA from human Gluk1 receptor 24140446

Literature References

PubMed DOI Target Context # Activities
24140446 10.1016/j.bmcl.2013.09.045 Glutamate receptor 2 1
24140446 10.1016/j.bmcl.2013.09.045 Glutamate receptor ionotropic, kainate 1 1

Data from ChEMBL 36 via Core Engine