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Compound Detail

CHEMBL65710

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c1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)cc1

Basic Information

ChEMBL ID CHEMBL65710
Phase Preclinical
Structure Type MOL
InChI Key OYASVWZGKNBLSA-UHFFFAOYSA-N
8
Targets
8
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

348.5
MW (Da)
3.87
ALogP
5
HBA
0
HBD
23.8
PSA (Ų)
0.56
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 C20H20N4S
MW 348.48
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.92

Activity Summary

IC50 7 meas. best 8.34
EC50 1 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serotonin 3 (5-HT3) receptor
CHEMBL2094116
IC50 8.34 8.34 4.6 1
Serotonin 3 (5-HT3) receptor
CHEMBL2094132
IC50 8.34 8.34 4.6 1
NG108-15
CHEMBL613828
EC50 7.52 7.52 30.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
IC50 5.43 5.43 3715.3 1
5-hydroxytryptamine receptor 1A
CHEMBL214
IC50 5.23 5.23 5888.4 1
5-hydroxytryptamine receptor 2A
CHEMBL3446
IC50 4.71 4.71 19498.5 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 4.04 4.04 91201.1 1
5-hydroxytryptamine receptor 1D
CHEMBL4105
IC50 4.03 4.03 93325.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8642566 10.1021/jm950543x Serotonin 3 (5-HT3) receptor 3
8642566 10.1021/jm950543x 5-hydroxytryptamine receptor 1A 1
8642566 10.1021/jm950543x 5-hydroxytryptamine receptor 1B 1
8642566 10.1021/jm950543x 5-hydroxytryptamine receptor 1D 1
8642566 10.1021/jm950543x 5-hydroxytryptamine receptor 2A 1
8642566 10.1021/jm950543x 5-hydroxytryptamine receptor 2C 1
8642566 10.1021/jm950543x NG108-15 1
11229746 10.1016/s0960-894x(00)00691-0 Serotonin 3 (5-HT3) receptor 1

Data from ChEMBL 36 via Core Engine