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Compound Detail

CHEMBL5619978

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NC(=O)c1cc2cc(N3CCN(CCc4ccc5[nH]c(=O)oc5c4)CC3)ccc2o1

Basic Information

ChEMBL ID CHEMBL5619978
Phase Preclinical
Structure Type MOL
InChI Key CTQNVZIYOJCTSN-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

406.4
MW (Da)
2.33
ALogP
6
HBA
2
HBD
108.7
PSA (Ų)
0.53
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22N4O4
MW 406.44
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.07

Activity Summary

IC50 2 meas. best 7.23
EC50 1 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL238
IC50 7.23 7.23 59.0 1
Sodium-dependent noradrenaline transporter
CHEMBL222
IC50 6.78 6.78 168.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
EC50 4.96 4.96 11000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38875810 10.1016/j.ejmech.2024.116564 5-hydroxytryptamine receptor 1A 2
38875810 10.1016/j.ejmech.2024.116564 Sodium-dependent serotonin transporter 1
38875810 10.1016/j.ejmech.2024.116564 Sodium-dependent noradrenaline transporter 1
38875810 10.1016/j.ejmech.2024.116564 Sodium-dependent dopamine transporter 1

Data from ChEMBL 36 via Core Engine