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Compound Detail

CHEMBL4442332

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COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12.Cl

Basic Information

ChEMBL ID CHEMBL4442332
Phase Preclinical
Structure Type MOL
InChI Key SJGAYHFYNRZIAG-UHFFFAOYSA-N
Parent Compound CHEMBL4598348
Active Moiety CHEMBL4598348
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
4.32
ALogP
6
HBA
2
HBD
103.0
PSA (Ų)
0.44
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21ClN4O3S
MW 468.97
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -0.70

Activity Summary

Ki 4 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 8.0 8.0 10.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 5.96 5.96 1096.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.88 5.88 1318.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.78 5.78 1660.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31229883 10.1016/j.ejmech.2019.06.001 5-hydroxytryptamine receptor 1A 1
31229883 10.1016/j.ejmech.2019.06.001 5-hydroxytryptamine receptor 2A 1
31229883 10.1016/j.ejmech.2019.06.001 D(2) dopamine receptor 1
31229883 10.1016/j.ejmech.2019.06.001 5-hydroxytryptamine receptor 6 1
31229883 10.1016/j.ejmech.2019.06.001 5-hydroxytryptamine receptor 7 1

Data from ChEMBL 36 via Core Engine