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Compound Detail

CHEMBL4210471

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O=C(NCCCN1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1

Basic Information

ChEMBL ID CHEMBL4210471
Phase Preclinical
Structure Type MOL
InChI Key WRRIRYQLTJZUKS-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

382.5
MW (Da)
1.75
ALogP
6
HBA
1
HBD
66.9
PSA (Ų)
0.74
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 C21H26N4O3
MW 382.46
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.41

Activity Summary

EC50 1 meas. best 5.19
Ki 1 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 7.34 7.34 45.3 1
5-hydroxytryptamine receptor 2A
CHEMBL322
EC50 5.19 5.19 6480.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28943244 10.1016/j.bmc.2017.09.018 5-hydroxytryptamine receptor 2A 4
28943244 10.1016/j.bmc.2017.09.018 5-hydroxytryptamine receptor 1A 1
28943244 10.1016/j.bmc.2017.09.018 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine