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Compound Detail

CHEMBL4790446

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Cl.Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL4790446
Phase Preclinical
Structure Type MOL
InChI Key CZTKLVZDFSUICK-UHFFFAOYSA-N
Parent Compound CHEMBL4803723
Active Moiety CHEMBL4803723
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

317.2
MW (Da)
4.71
ALogP
1
HBA
2
HBD
27.8
PSA (Ų)
0.67
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H15Cl3N2
MW 353.68
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -0.31

Activity Summary

EC50 5 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 7.9 7.9 12.6 2
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 7.89 7.89 12.8 2
Plasmodium falciparum
CHEMBL364
EC50 5.71 5.71 1940.0 1

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
32822760 10.1016/j.bmcl.2020.127502 ADMET 1
32822760 10.1016/j.bmcl.2020.127502 BJ 1
32822760 10.1016/j.bmcl.2020.127502 Plasmodium falciparum 1
35450369 10.1021/acsmedchemlett.1c00694 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1

Data from ChEMBL 36 via Core Engine