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Compound Detail

CHEMBL3758932

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COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cccc2)C[C@H]1OC

Basic Information

ChEMBL ID CHEMBL3758932
Phase Preclinical
Structure Type MOL
InChI Key OBSQRQKRXUFJSA-AZUAARDMSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

420.9
MW (Da)
2.64
ALogP
6
HBA
2
HBD
81.8
PSA (Ų)
0.64
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H29ClN4O3
MW 420.94
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.96

Activity Summary

IC50 2 meas. best 6.19
EC50 1 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
IC50 6.19 6.19 648.0 1
5-hydroxytryptamine receptor 4
CHEMBL4317
EC50 6.17 6.17 676.1 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.17 5.17 6835.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26761776 10.1016/j.ejmech.2015.12.006 5-hydroxytryptamine receptor 4 2
26761776 10.1016/j.ejmech.2015.12.006 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine