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Compound Detail

CHEMBL1161069

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CCCCS(=O)(=O)N(C)Cc1ccc(CN2CCN(c3ccccc3OC)CC2)n1C.O=C(O)CCC(=O)O

Basic Information

ChEMBL ID CHEMBL1161069
Phase Preclinical
Structure Type MOL
InChI Key ZPNFRIUEGZMXEB-UHFFFAOYSA-N
Parent Compound CHEMBL1199969
Active Moiety CHEMBL1199969
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

448.6
MW (Da)
2.92
ALogP
6
HBA
0
HBD
58.0
PSA (Ų)
0.56
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H42N4O7S
MW 566.72
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.39

Activity Summary

Ki 2 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 8.15 8.15 7.1 1
D(2) dopamine receptor
CHEMBL339
Ki 6.0 6.0 1000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 3.7 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7473547 10.1021/jm00021a009 Rattus norvegicus 2
7473547 10.1021/jm00021a009 D(2) dopamine receptor 1
7473547 10.1021/jm00021a009 5-hydroxytryptamine receptor 1A 1
7473547 10.1021/jm00021a009 No relevant target 1

Data from ChEMBL 36 via Core Engine