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Compound Detail

CHEMBL66307

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Clc1ccc(C(c2ccccc2)N2CCN(c3nc4ccsc4n4cccc34)CC2)cc1

Basic Information

ChEMBL ID CHEMBL66307
Phase Preclinical
Structure Type MOL
InChI Key DFXLNCRNORESIF-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

459.0
MW (Da)
6.11
ALogP
5
HBA
0
HBD
23.8
PSA (Ų)
0.32
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23ClN4S
MW 459.02
Aromatic Rings 5
Heavy Atoms 32
NP-Likeness -1.61

Activity Summary

IC50 3 meas. best 5.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serotonin 3 (5-HT3) receptor
CHEMBL2094116
IC50 5.86 5.86 1380.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serotonin 3 (5-HT3) receptor IC50 = 1380.38 nM 5.86 Binding affinity towards 5-hydroxytryptamine 3 receptor 8642566

Literature References

PubMed DOI Target Context # Activities
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 Serotonin 3 (5-HT3) receptor 1

Data from ChEMBL 36 via Core Engine