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Compound Detail

CHEMBL5595457

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

Basic Information

ChEMBL ID CHEMBL5595457
Phase Preclinical
Structure Type MOL
InChI Key JJUYPUPBWHCOQR-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

516.6
MW (Da)
5.25
ALogP
5
HBA
1
HBD
61.3
PSA (Ų)
0.32
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29FN4O2S
MW 516.64
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.37

Activity Summary

Ki 2 meas. best 7.38
IC50 1 meas. best 5.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 7.38 7.185 42.0 2
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.54 5.54 2900.0 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 4
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