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Compound Detail

CHEMBL3330811

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COc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1

Basic Information

ChEMBL ID CHEMBL3330811
Phase Preclinical
Structure Type MOL
InChI Key FROKPIIZKWCIFC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

334.4
MW (Da)
4.12
ALogP
5
HBA
0
HBD
44.1
PSA (Ų)
0.57
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 C19H14N2O2S
MW 334.40
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.20

Activity Summary

IC50 2 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 1
CHEMBL3772
IC50 7.3 7.3 50.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.97 4.97 10800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25127154 10.1016/j.ejmech.2014.08.027 Metabotropic glutamate receptor 1 3
25127154 10.1016/j.ejmech.2014.08.027 Metabotropic glutamate receptor 5 2
25127154 10.1016/j.ejmech.2014.08.027 Voltage-gated inwardly rectifying potassium channel KCNH2 2
25127154 10.1016/j.ejmech.2014.08.027 Liver microsome 1
25127154 10.1016/j.ejmech.2014.08.027 Cytochrome P450 1A2 1
25127154 10.1016/j.ejmech.2014.08.027 Cytochrome P450 2C9 1
25127154 10.1016/j.ejmech.2014.08.027 Cytochrome P450 2C19 1
25127154 10.1016/j.ejmech.2014.08.027 Cytochrome P450 2D6 1
25127154 10.1016/j.ejmech.2014.08.027 Cytochrome P450 3A4 1
25127154 10.1016/j.ejmech.2014.08.027 ADMET 1

Data from ChEMBL 36 via Core Engine