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Compound Detail

CHEMBL135201

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Nc1cc(OCCCNCC2CCc3ccc(O)cc3O2)ccc1Cl.O=C(O)C(=O)O

Basic Information

ChEMBL ID CHEMBL135201
Phase Preclinical
Structure Type MOL
InChI Key OLZKSNVYTOYFEH-UHFFFAOYSA-N
Parent Compound CHEMBL1180616
Active Moiety CHEMBL1180616
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

362.9
MW (Da)
3.38
ALogP
5
HBA
3
HBD
76.7
PSA (Ų)
0.52
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25ClN2O7
MW 452.89
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.05

Activity Summary

Ki 4 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL339
Ki 9.52 8.655 0.3 2
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 8.72 8.72 1.9 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.75 7.75 18.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9435894 10.1021/jm9703653 D(2) dopamine receptor 3
9435894 10.1021/jm9703653 5-hydroxytryptamine receptor 1A 1
9435894 10.1021/jm9703653 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine