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Compound Detail

CHEMBL393036

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CNCc1cc(C#CCCN2CCCCC2)ccc1Oc1ccc(SC)cc1

Basic Information

ChEMBL ID CHEMBL393036
Phase Preclinical
Structure Type MOL
InChI Key WTAQICPSTMPTOD-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

394.6
MW (Da)
5.15
ALogP
4
HBA
1
HBD
24.5
PSA (Ų)
0.52
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N2OS
MW 394.58
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.89

Activity Summary

Ki 3 meas. best 9.15
Kd 1 meas. best 8.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL228
Ki 9.15 9.15 0.7 1
Sodium-dependent serotonin transporter
CHEMBL313
Ki 9.15 9.15 0.7 1
Histamine H3 receptor
CHEMBL264
Ki 8.77 8.77 1.7 1
Histamine H3 receptor
CHEMBL264
Kd 8.61 8.61 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17616397 10.1016/j.bmcl.2007.06.061 Sodium-dependent serotonin transporter 2
17616397 10.1016/j.bmcl.2007.06.061 Histamine H3 receptor 2

Data from ChEMBL 36 via Core Engine