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Compound Detail

CHEMBL428024

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CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccccc1

Basic Information

ChEMBL ID CHEMBL428024
Phase Preclinical
Structure Type MOL
InChI Key OICXGVDCXUDGKS-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

350.5
MW (Da)
3.27
ALogP
4
HBA
1
HBD
33.7
PSA (Ų)
0.81
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 C22H26N2O2
MW 350.46
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.87

Activity Summary

Ki 3 meas. best 8.24
Kd 1 meas. best 8.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 8.24 8.24 5.7 1
Histamine H3 receptor
CHEMBL264
Kd 8.14 8.14 7.2 1
Sodium-dependent serotonin transporter
CHEMBL313
Ki 7.96 7.96 11.0 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 7.52 7.52 30.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17616397 10.1016/j.bmcl.2007.06.061 Sodium-dependent serotonin transporter 2
17616397 10.1016/j.bmcl.2007.06.061 Histamine H3 receptor 2

Data from ChEMBL 36 via Core Engine