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Compound Detail

CHEMBL5178632

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COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC.Cl

Basic Information

ChEMBL ID CHEMBL5178632
Phase Preclinical
Structure Type MOL
InChI Key PVTMHJQDZUKZLW-UHFFFAOYSA-N
Parent Compound CHEMBL5221423
Active Moiety CHEMBL5221423
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

354.4
MW (Da)
3.13
ALogP
5
HBA
3
HBD
75.7
PSA (Ų)
0.67
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H23ClN2O4
MW 390.87
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness 0.66

Activity Summary

EC50 4 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 8.42 8.41 3.8 2
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 8.12 8.11 7.6 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35450369 10.1021/acsmedchemlett.1c00694 5-hydroxytryptamine receptor 2A 3
35450369 10.1021/acsmedchemlett.1c00694 5-hydroxytryptamine receptor 2C 3
35450369 10.1021/acsmedchemlett.1c00694 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1

Data from ChEMBL 36 via Core Engine