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Compound Detail

CHEMBL5193862

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O=C(Nn1c(=O)c(=O)[nH]c2cc(C(F)(F)F)c(F)cc21)c1ccccc1O

Basic Information

ChEMBL ID CHEMBL5193862
Phase Preclinical
Structure Type MOL
InChI Key MCKOVZZCGOMMIB-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

383.3
MW (Da)
1.94
ALogP
5
HBA
3
HBD
104.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H9F4N3O4
MW 383.26
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.12

Activity Summary

Ki 6 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, kainate 3
CHEMBL3684
Ki 6.85 6.85 142.0 1
Glutamate receptor ionotropic, kainate 2
CHEMBL3683
Ki 6.04 6.04 908.0 1
Glutamate receptor ionotropic AMPA
CHEMBL2096670
Ki 6.02 6.02 960.0 1
Glutamate receptor ionotropic, kainate 1
CHEMBL1918
Ki 5.95 5.95 1120.0 1
Glutamate receptor 2
CHEMBL4016
Ki 5.38 5.38 4120.0 1
Glutamate receptor ionotropic, kainate 5
CHEMBL2675
Ki 4.58 4.58 26400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34998058 10.1016/j.ejmech.2021.114085 Glutamate receptor ionotropic AMPA 1
34998058 10.1016/j.ejmech.2021.114085 Glutamate receptor 2 1
34998058 10.1016/j.ejmech.2021.114085 Glutamate receptor ionotropic, kainate 1 1
34998058 10.1016/j.ejmech.2021.114085 Glutamate receptor ionotropic, kainate 2 1
34998058 10.1016/j.ejmech.2021.114085 Glutamate receptor ionotropic, kainate 3 1
34998058 10.1016/j.ejmech.2021.114085 Glutamate receptor ionotropic, kainate 5 1

Data from ChEMBL 36 via Core Engine