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Compound Detail

CHEMBL198999

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CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCc5ccccc5)CC4)c(=O)c23)C1

Basic Information

ChEMBL ID CHEMBL198999
Phase Preclinical
Structure Type MOL
InChI Key MDXDUERQAFAILI-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

515.7
MW (Da)
3.85
ALogP
8
HBA
0
HBD
53.8
PSA (Ų)
0.37
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 C29H33N5O2S
MW 515.68
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.72

Activity Summary

Ki 3 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1B
CHEMBL1898
Ki 8.92 8.92 1.2 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 8.72 8.72 1.9 1
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16219465 10.1016/j.bmcl.2005.04.077 5-hydroxytryptamine receptor 1A 3
16219465 10.1016/j.bmcl.2005.04.077 5-hydroxytryptamine receptor 1B 3
16219465 10.1016/j.bmcl.2005.04.077 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine