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Compound Detail

CHEMBL3823441

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CN(c1ccc(O)cc1)c1nc(-c2ccccn2)cs1

Basic Information

ChEMBL ID CHEMBL3823441
Phase Preclinical
Structure Type MOL
InChI Key OXXRMKKAGJYBBX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

283.4
MW (Da)
3.68
ALogP
5
HBA
1
HBD
49.2
PSA (Ų)
0.80
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H13N3OS
MW 283.36
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -1.27

Activity Summary

IC50 1 meas. best 5.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor 1
CHEMBL2009
IC50 5.53 5.53 2970.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 234.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutamate receptor 1 IC50 = 2970.0 nM 5.53 Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cel... 27067148

Literature References

PubMed DOI Target Context # Activities
27067148 10.1021/acs.jmedchem.6b00125 Glutamate receptor 1 5
27067148 10.1021/acs.jmedchem.6b00125 Liver microsome 2
27067148 10.1021/acs.jmedchem.6b00125 ADMET 2
27067148 10.1021/acs.jmedchem.6b00125 Hepatocyte 2
27067148 10.1021/acs.jmedchem.6b00125 Rattus norvegicus 1
27067148 10.1021/acs.jmedchem.6b00125 Cytochrome P450 1A2 1

Data from ChEMBL 36 via Core Engine