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Compound Detail

CHEMBL1095274

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CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1.Cl

Basic Information

ChEMBL ID CHEMBL1095274
Phase Preclinical
Structure Type MOL
InChI Key LFLUHLCPXQWQKW-UHFFFAOYSA-N
Parent Compound CHEMBL1199079
Active Moiety CHEMBL1199079
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

340.4
MW (Da)
3.00
ALogP
4
HBA
0
HBD
42.3
PSA (Ų)
0.72
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21ClN2O2S
MW 376.91
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.03

Activity Summary

IC50 1 meas. best 7.11
Ki 1 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 8.24 8.24 5.7 1
5-hydroxytryptamine receptor 6
CHEMBL3371
IC50 7.11 7.11 78.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19939513 10.1016/j.ejmech.2009.10.035 5-hydroxytryptamine receptor 6 4
19939513 10.1016/j.ejmech.2009.10.035 5-hydroxytryptamine receptor 1A 1
19939513 10.1016/j.ejmech.2009.10.035 5-hydroxytryptamine receptor 2B 1
19939513 10.1016/j.ejmech.2009.10.035 5-hydroxytryptamine receptor 2C 1
19939513 10.1016/j.ejmech.2009.10.035 5-hydroxytryptamine receptor 7 1
19939513 10.1016/j.ejmech.2009.10.035 Alpha-1B adrenergic receptor 1
19939513 10.1016/j.ejmech.2009.10.035 Alpha-1D adrenergic receptor 1
19939513 10.1016/j.ejmech.2009.10.035 Alpha-2A adrenergic receptor 1
19939513 10.1016/j.ejmech.2009.10.035 Alpha-1A adrenergic receptor 1
19939513 10.1016/j.ejmech.2009.10.035 Sodium-dependent dopamine transporter 1
19939513 10.1016/j.ejmech.2009.10.035 Sodium-dependent noradrenaline transporter 1
19939513 10.1016/j.ejmech.2009.10.035 D(3) dopamine receptor 1
19939513 10.1016/j.ejmech.2009.10.035 Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine