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Compound Detail

CHEMBL93076

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CCOC(=O)c1nc2c(O)nc3cc(C(F)(F)F)c(-n4ccc(C=O)c4)cc3n2n1

Basic Information

ChEMBL ID CHEMBL93076
Phase Preclinical
Structure Type MOL
InChI Key AAMJVMJIQRQTEE-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

419.3
MW (Da)
2.78
ALogP
9
HBA
1
HBD
111.6
PSA (Ų)
0.40
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H12F3N5O4
MW 419.32
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.13

Activity Summary

IC50 2 meas. best 5.11
Ki 2 meas. best 6.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, AMPA
CHEMBL2093871
Ki 6.43 6.43 370.0 1
Mus musculus
CHEMBL375
IC50 5.11 5.11 7800.0 1
Glutamate receptor ionotropic, kainate
CHEMBL2094119
IC50 4.51 4.51 31200.0 1
Glutamate receptor ionotropic, NMDA 1
CHEMBL330
Ki 4.15 4.15 71000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14695840 10.1021/jm030906q Mus musculus 2
14695840 10.1021/jm030906q Rattus norvegicus 2
14695840 10.1021/jm030906q Glutamate receptor ionotropic, AMPA 1
14695840 10.1021/jm030906q Glutamate receptor ionotropic, NMDA 1 1
14695840 10.1021/jm030906q Glutamate receptor ionotropic, kainate 1

Data from ChEMBL 36 via Core Engine