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Compound Detail

CHEMBL545488

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Cl.O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL545488
Phase Preclinical
Structure Type MOL
InChI Key FKPGHTCMGZCAEB-UHFFFAOYSA-N
Parent Compound CHEMBL111189
Active Moiety CHEMBL111189
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

428.6
MW (Da)
4.30
ALogP
5
HBA
0
HBD
40.6
PSA (Ų)
0.59
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30ClFN2O2S
MW 465.03
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.02

Activity Summary

Ki 4 meas. best 6.65
Kd 1 meas. best 6.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 6.83 6.83 147.9 1
D(2) dopamine receptor
CHEMBL339
Ki 6.65 6.65 223.9 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.54 6.54 288.4 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.4 6.4 398.1 1
D(1A) dopamine receptor
CHEMBL265
Ki 5.51 5.51 3090.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10425088 10.1021/jm981094e Unchecked 3
10425088 10.1021/jm981094e Mus musculus 2
10425088 10.1021/jm981094e D(1A) dopamine receptor 1
10425088 10.1021/jm981094e D(2) dopamine receptor 1
10425088 10.1021/jm981094e 5-hydroxytryptamine receptor 2A 1
10425088 10.1021/jm981094e 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine