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Compound Detail

CHEMBL3752465

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Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OC(CCN(C)C)c3ccccc3)cc1)CC2

Basic Information

ChEMBL ID CHEMBL3752465
Phase Preclinical
Structure Type MOL
InChI Key LEZYBQCQNUONFW-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

464.0
MW (Da)
6.31
ALogP
3
HBA
1
HBD
44.8
PSA (Ų)
0.45
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30ClN3O2
MW 464.01
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.22

Activity Summary

Ki 3 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL324
Ki 9.22 9.22 0.6 1
Sodium-dependent serotonin transporter
CHEMBL313
Ki 7.18 7.18 65.5 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.86 6.86 138.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26748694 10.1016/j.bmcl.2015.12.071 5-hydroxytryptamine receptor 2C 1
26748694 10.1016/j.bmcl.2015.12.071 Sodium-dependent serotonin transporter 1
26748694 10.1016/j.bmcl.2015.12.071 5-hydroxytryptamine receptor 2A 1
26748694 10.1016/j.bmcl.2015.12.071 Mus musculus 1
26748694 10.1016/j.bmcl.2015.12.071 Liver microsome 1
26748694 10.1016/j.bmcl.2015.12.071 ADMET 1

Data from ChEMBL 36 via Core Engine