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Compound Detail

CHEMBL5595885

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O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCc4c[nH]c5ccc(Cl)cc45)CC3)cccc21

Basic Information

ChEMBL ID CHEMBL5595885
Phase Preclinical
Structure Type MOL
InChI Key XUVAGSBCUVZYBU-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

533.1
MW (Da)
5.77
ALogP
5
HBA
1
HBD
61.3
PSA (Ų)
0.29
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29ClN4O2S
MW 533.10
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.31

Activity Summary

IC50 2 meas. best 6.97
Ki 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 8.3 7.88 5.0 2
5-hydroxytryptamine receptor 6
CHEMBL3371
IC50 6.97 6.97 107.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 6.16 6.16 700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38901106 10.1016/j.ejmech.2024.116601 5-hydroxytryptamine receptor 6 5
38901106 10.1016/j.ejmech.2024.116601 Adrenergic receptor alpha-1 1
38901106 10.1016/j.ejmech.2024.116601 Histamine H1 receptor 1
38901106 10.1016/j.ejmech.2024.116601 Muscarinic acetylcholine receptor M1 1
38901106 10.1016/j.ejmech.2024.116601 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine