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Compound Detail

CHEMBL5201903

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Cl.Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21

Basic Information

ChEMBL ID CHEMBL5201903
Phase Preclinical
Structure Type MOL
InChI Key MNMSWUFXEOYHMY-UHFFFAOYSA-N
Parent Compound CHEMBL5222595
Active Moiety CHEMBL5222595
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

333.2
MW (Da)
4.42
ALogP
2
HBA
3
HBD
48.0
PSA (Ų)
0.62
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H15Cl3N2O
MW 369.68
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness 0.30

Activity Summary

EC50 6 meas. best 7.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 7.61 7.605 24.6 2
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 7.33 7.33 46.8 2
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 7.29 7.285 51.3 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 5-hydroxytryptamine receptor 2B 3
35450369 10.1021/acsmedchemlett.1c00694 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1

Data from ChEMBL 36 via Core Engine