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Compound Detail

CHEMBL299634

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Clc1ccc2c(c1)nc(N1CCN(Cc3ccccc3)CC1)c1cccn12

Basic Information

ChEMBL ID CHEMBL299634
Phase Preclinical
Structure Type MOL
InChI Key SEYPHWUAVBLMMR-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

376.9
MW (Da)
4.46
ALogP
4
HBA
0
HBD
23.8
PSA (Ų)
0.53
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21ClN4
MW 376.89
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.74

Activity Summary

IC50 3 meas. best 9.54
EC50 1 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serotonin 3 (5-HT3) receptor
CHEMBL2094132
IC50 9.54 9.54 0.3 1
NG108-15
CHEMBL613828
EC50 7.28 7.28 52.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
IC50 5.28 5.28 5248.1 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 4.72 4.72 19054.6 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