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Compound Detail

CHEMBL4534333

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O=C(Nc1ccc2[nH]c(=O)oc2c1)C(=O)N1CCN(c2ccc(C(F)(F)F)c(F)c2)CC1

Basic Information

ChEMBL ID CHEMBL4534333
Phase Preclinical
Structure Type MOL
InChI Key DHOPUVMTPDUDAN-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

452.4
MW (Da)
2.57
ALogP
5
HBA
2
HBD
98.7
PSA (Ų)
0.46
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16F4N4O4
MW 452.36
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.68

Activity Summary

IC50 2 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, NMDA 2B
CHEMBL3442
IC50 9.0 9.0 1.0 1
Glutamate receptor ionotropic, NMDA 2B
CHEMBL311
IC50 7.8 7.8 15.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.6 mL.min-1.kg-1 Rattus norvegicus
F 8.7 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30833109 10.1016/j.bmcl.2019.02.017 Glutamate receptor ionotropic, NMDA 2B 2
30833109 10.1016/j.bmcl.2019.02.017 ADMET 2
30833109 10.1016/j.bmcl.2019.02.017 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine