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Compound Detail

CHEMBL2179676

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Cl.Cn1cc2c(OCC3CCN(CCN4CCOCC4)CC3)nc3ccccc3c2c1

Basic Information

ChEMBL ID CHEMBL2179676
Phase Preclinical
Structure Type MOL
InChI Key ITWQLJSVTWOWID-UHFFFAOYSA-N
Parent Compound CHEMBL2220954
Active Moiety CHEMBL2220954
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

408.6
MW (Da)
3.15
ALogP
6
HBA
0
HBD
42.8
PSA (Ų)
0.63
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H33ClN4O2
MW 445.01
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.09

Activity Summary

IC50 1 meas. best 5.91
Ki 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 8.6 8.6 2.5 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.91 5.91 1220.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23043420 10.1021/jm300573d Voltage-gated inwardly rectifying potassium channel KCNH2 1
23043420 10.1021/jm300573d 5-hydroxytryptamine receptor 2A 1
23043420 10.1021/jm300573d 5-hydroxytryptamine receptor 4 1

Data from ChEMBL 36 via Core Engine