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Compound Detail

CHEMBL302447

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c1ccc(CN2CCN(c3nc4scc(-c5ccccc5)c4n4cccc34)CC2)cc1

Basic Information

ChEMBL ID CHEMBL302447
Phase Preclinical
Structure Type MOL
InChI Key RQPNBYPBNQHGRL-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

424.6
MW (Da)
5.54
ALogP
5
HBA
0
HBD
23.8
PSA (Ų)
0.38
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 C26H24N4S
MW 424.57
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -1.46

Activity Summary

IC50 6 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
IC50 5.58 5.58 2630.3 1
Serotonin 3 (5-HT3) receptor
CHEMBL2094116
IC50 5.17 5.17 6760.8 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 4.62 4.62 23988.3 1
5-hydroxytryptamine receptor 1A
CHEMBL214
IC50 4.59 4.59 25704.0 1
5-hydroxytryptamine receptor 1D
CHEMBL4105
IC50 4.51 4.51 30903.0 1
5-hydroxytryptamine receptor 2A
CHEMBL3446
IC50 4.2 4.2 63095.7 1

Activity Data Samples

Top measurements by pChEMBL value

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