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Compound Detail

CHEMBL1382868

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c1ccc2c(CSc3[nH]cnc4ncnc3-4)cccc2c1

Basic Information

ChEMBL ID CHEMBL1382868
Phase Preclinical
Structure Type MOL
InChI Key BGMSTNYJYPSLHN-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

292.4
MW (Da)
3.75
ALogP
4
HBA
1
HBD
54.5
PSA (Ų)
0.46
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 C16H12N4S
MW 292.37
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -0.93

Activity Summary

IC50 4 meas. best 6.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serotonin 3 (5-HT3) receptor
CHEMBL2111332
IC50 6.37 6.37 430.0 1
5-hydroxytryptamine receptor 3A
CHEMBL1899
IC50 6.21 6.21 620.0 1
5-hydroxytryptamine receptor 3A/3E
CHEMBL4296087
IC50 6.15 6.15 710.0 1
5-hydroxytryptamine receptor 3A/3C
CHEMBL4296091
IC50 6.08 6.08 840.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28606760 10.1016/j.bmcl.2017.04.073 5-hydroxytryptamine receptor 3A/3E 1
28606760 10.1016/j.bmcl.2017.04.073 5-hydroxytryptamine receptor 3A/3C 1
28606760 10.1016/j.bmcl.2017.04.073 Serotonin 3 (5-HT3) receptor 1
28606760 10.1016/j.bmcl.2017.04.073 5-hydroxytryptamine receptor 3A 1

Data from ChEMBL 36 via Core Engine