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Compound Detail

CHEMBL418499

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Cn1c(=O)sc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21

Basic Information

ChEMBL ID CHEMBL418499
Phase Preclinical
Structure Type MOL
InChI Key YURVPEXVKWCAQY-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
3.98
ALogP
5
HBA
0
HBD
28.5
PSA (Ų)
0.64
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 C21H22F3N3OS
MW 421.49
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.82

Activity Summary

IC50 5 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL214
IC50 9.0 9.0 1.0 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 7.16 7.16 70.0 1
D(2) dopamine receptor
CHEMBL3998
IC50 6.7 6.7 200.0 1
Alpha-1A adrenergic receptor
CHEMBL4892
IC50 6.4 6.4 400.0 1
5-hydroxytryptamine receptor 2A
CHEMBL3446
IC50 6.22 6.22 600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9622542 10.1021/jm970298c 5-hydroxytryptamine receptor 1A 1
9622542 10.1021/jm970298c 5-hydroxytryptamine receptor 1B 1
9622542 10.1021/jm970298c 5-hydroxytryptamine receptor 2A 1
9622542 10.1021/jm970298c 5-hydroxytryptamine receptor 2C 1
9622542 10.1021/jm970298c D(2) dopamine receptor 1
9622542 10.1021/jm970298c Alpha-1A adrenergic receptor 1

Data from ChEMBL 36 via Core Engine