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Compound Detail

CHEMBL236047

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CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(Cl)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL236047
Phase Preclinical
Structure Type MOL
InChI Key GTLCRPKCYIDHGJ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

419.4
MW (Da)
4.58
ALogP
4
HBA
1
HBD
33.7
PSA (Ų)
0.70
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 C22H24Cl2N2O2
MW 419.35
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.09

Activity Summary

Ki 3 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.74 8.74 1.8 1
Sodium-dependent serotonin transporter
CHEMBL313
Ki 8.62 8.62 2.4 1
Histamine H3 receptor
CHEMBL264
Ki 7.96 7.96 11.0 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 1

Data from ChEMBL 36 via Core Engine