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Compound Detail

CHEMBL248446

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CCc1cc2[nH]c(=O)c(=O)[nH]c2c(N(CCCOC)S(C)(=O)=O)c1Cl

Basic Information

ChEMBL ID CHEMBL248446
Phase Preclinical
Structure Type MOL
InChI Key YIKXBWQRHOAYSJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

389.9
MW (Da)
1.23
ALogP
5
HBA
2
HBD
112.3
PSA (Ų)
0.55
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H20ClN3O5S
MW 389.86
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.92

Activity Summary

IC50 1 meas. best 7.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, NMDA 1
CHEMBL2015
IC50 7.31 7.31 49.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 632.0 ng.hr.mL-1 Rattus norvegicus
F 47.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutamate receptor ionotropic, NMDA 1 IC50 = 49.0 nM 7.31 Antagonist activity at human NMDA NR1 receptor 17562362

Literature References

PubMed DOI Target Context # Activities
17562362 10.1016/j.bmcl.2007.05.083 Rattus norvegicus 2
17562362 10.1016/j.bmcl.2007.05.083 Liver microsomes 2
17562362 10.1016/j.bmcl.2007.05.083 Glutamate receptor ionotropic, NMDA 1 1
17562362 10.1016/j.bmcl.2007.05.083 No relevant target 1
17562362 10.1016/j.bmcl.2007.05.083 Caco-2 1

Data from ChEMBL 36 via Core Engine