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Compound Detail

CHEMBL4104272

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c1ccc(OCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1

Basic Information

ChEMBL ID CHEMBL4104272
Phase Preclinical
Structure Type MOL
InChI Key HVYFBECSQURUQP-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

322.4
MW (Da)
3.45
ALogP
3
HBA
1
HBD
37.5
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22N2O2
MW 322.41
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.91

Activity Summary

Ki 3 meas. best 8.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL219
Ki 8.25 8.25 5.6 1
D(2) dopamine receptor
CHEMBL217
Ki 6.4 6.4 400.0 1
D(3) dopamine receptor
CHEMBL234
Ki 5.83 5.83 1480.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 40.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28489950 10.1021/acs.jmedchem.7b00151 D(2) dopamine receptor 1
28489950 10.1021/acs.jmedchem.7b00151 D(3) dopamine receptor 1
28489950 10.1021/acs.jmedchem.7b00151 D(4) dopamine receptor 1
28489950 10.1021/acs.jmedchem.7b00151 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine