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Compound Detail

CHEMBL4800575

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COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(Cl)c(Cl)c2)CC1

Basic Information

ChEMBL ID CHEMBL4800575
Phase Preclinical
Structure Type MOL
InChI Key WWQYGUPGPQFXAD-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

455.4
MW (Da)
4.61
ALogP
4
HBA
1
HBD
50.8
PSA (Ų)
0.59
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25Cl2FN2O3
MW 455.36
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.05

Activity Summary

Ki 6 meas. best 9.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 9.42 9.42 0.4 2
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.34 7.34 45.7 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 7.34 7.34 46.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.47 6.41 338.8 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32883072 10.1021/acs.jmedchem.0c00814 5-hydroxytryptamine receptor 1A 1
32883072 10.1021/acs.jmedchem.0c00814 Adrenergic receptor alpha-1 1
32883072 10.1021/acs.jmedchem.0c00814 D(2) dopamine receptor 1
32883072 10.1021/acs.jmedchem.0c00814 Unchecked 1

Data from ChEMBL 36 via Core Engine