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Compound Detail

CHEMBL3329813

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CC(C(=O)O)c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1

Basic Information

ChEMBL ID CHEMBL3329813
Phase Preclinical
Structure Type MOL
InChI Key RPITWOWTHILVSI-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
4.68
ALogP
6
HBA
1
HBD
81.0
PSA (Ų)
0.50
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N2O5
MW 476.57
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.52

Activity Summary

IC50 1 meas. best 4.6
Ki 1 meas. best 9.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 9.5 9.5 0.3 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.6 4.6 25000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25149506 10.1016/j.bmcl.2014.06.083 5-hydroxytryptamine receptor 4 2
25149506 10.1016/j.bmcl.2014.06.083 Voltage-gated inwardly rectifying potassium channel KCNH2 1
25149506 10.1016/j.bmcl.2014.06.083 No relevant target 1

Data from ChEMBL 36 via Core Engine