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Compound Detail

CHEMBL4435010

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COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1.Cl

Basic Information

ChEMBL ID CHEMBL4435010
Phase Preclinical
Structure Type MOL
InChI Key GJDXAYDBLVQEKU-UHFFFAOYSA-N
Parent Compound CHEMBL4596543
Active Moiety CHEMBL4596543
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

368.4
MW (Da)
2.86
ALogP
6
HBA
2
HBD
103.0
PSA (Ų)
0.58
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 C18H17ClN4O3S
MW 404.88
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -0.71

Activity Summary

Ki 4 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 8.7 8.7 2.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.1 6.1 794.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 5.94 5.94 1148.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.92 5.92 1202.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31229883 10.1016/j.ejmech.2019.06.001 Histamine H1 receptor 3
31229883 10.1016/j.ejmech.2019.06.001 5-hydroxytryptamine receptor 2C 3
31229883 10.1016/j.ejmech.2019.06.001 5-hydroxytryptamine receptor 6 2
31229883 10.1016/j.ejmech.2019.06.001 5-hydroxytryptamine receptor 2B 2
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 7 1
31229883 10.1016/j.ejmech.2019.06.001 Alpha-1A adrenergic receptor 1
31229883 10.1016/j.ejmech.2019.06.001 Muscarinic acetylcholine receptor M1 1
31229883 10.1016/j.ejmech.2019.06.001 Muscarinic acetylcholine receptor M5 1
31229883 10.1016/j.ejmech.2019.06.001 Voltage-gated inwardly rectifying potassium channel KCNH2 1
31229883 10.1016/j.ejmech.2019.06.001 No relevant target 1

Data from ChEMBL 36 via Core Engine