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Compound Detail

CHEMBL53662

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COc1ccc2c(c1)nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12

Basic Information

ChEMBL ID CHEMBL53662
Phase Preclinical
Structure Type MOL
InChI Key ACSDLURGGYXLSE-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

390.5
MW (Da)
3.96
ALogP
5
HBA
0
HBD
33.0
PSA (Ų)
0.53
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23FN4O
MW 390.46
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.69

Activity Summary

IC50 3 meas. best 8.18
EC50 1 meas. best 6.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serotonin 3 (5-HT3) receptor
CHEMBL2094132
IC50 8.18 8.18 6.6 1
NG108-15
CHEMBL613828
EC50 6.98 6.98 104.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
IC50 4.38 4.38 41686.9 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 4.16 4.16 69183.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9191957 10.1021/jm960501o Rattus norvegicus 2
9191957 10.1021/jm960501o 5-hydroxytryptamine receptor 1A 1
9191957 10.1021/jm960501o 5-hydroxytryptamine receptor 1B 1
9191957 10.1021/jm960501o 5-hydroxytryptamine receptor 1D 1
9191957 10.1021/jm960501o 5-hydroxytryptamine receptor 2A 1
9191957 10.1021/jm960501o 5-hydroxytryptamine receptor 2C 1
9191957 10.1021/jm960501o Serotonin 3 (5-HT3) receptor 1
9191957 10.1021/jm960501o NG108-15 1

Data from ChEMBL 36 via Core Engine