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Compound Detail

CHEMBL236994

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O=c1c2sc3ncc4c(c3c2ncn1-c1ccc(Cl)cc1)NCCO4

Basic Information

ChEMBL ID CHEMBL236994
Phase Preclinical
Structure Type MOL
InChI Key FODONWGPMXPGNC-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

370.8
MW (Da)
3.45
ALogP
7
HBA
1
HBD
69.0
PSA (Ų)
0.56
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H11ClN4O2S
MW 370.82
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.39

Activity Summary

IC50 1 meas. best 8.54
Ki 1 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 1
CHEMBL4477
Ki 9.4 9.4 0.4 1
Metabotropic glutamate receptor 1
CHEMBL3772
IC50 8.54 8.54 2.9 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 135.72 ng.hr.mL-1 Rattus norvegicus
Cmax 198.0 nM Rattus norvegicus
Tmax 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17929793 10.1021/jm070590c Rattus norvegicus 6
17929793 10.1021/jm070590c Metabotropic glutamate receptor 1 2
17929793 10.1021/jm070590c Metabotropic glutamate receptor 5 1

Data from ChEMBL 36 via Core Engine