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Compound Detail

CHEMBL1277401

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O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)CC1

Basic Information

ChEMBL ID CHEMBL1277401
Phase Preclinical
Structure Type MOL
InChI Key OSWDQWCAAIWPDM-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

425.9
MW (Da)
4.92
ALogP
4
HBA
1
HBD
66.8
PSA (Ų)
0.74
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24ClNO4
MW 425.91
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness 0.10

Activity Summary

Ki 2 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.4 6.4 398.1 1
Histamine H1 receptor
CHEMBL231
Ki 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20942472 10.1021/jm100856p 5-hydroxytryptamine receptor 2C 1
20942472 10.1021/jm100856p 5-hydroxytryptamine receptor 2B 1
20942472 10.1021/jm100856p 5-hydroxytryptamine receptor 2A 1
20942472 10.1021/jm100856p Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine