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Compound Detail

CHEMBL4068924

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OCc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1Cl

Basic Information

ChEMBL ID CHEMBL4068924
Phase Preclinical
Structure Type MOL
InChI Key HGMLOQOHAYKVJN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

356.9
MW (Da)
3.03
ALogP
4
HBA
2
HBD
55.4
PSA (Ų)
0.75
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21ClN4O
MW 356.86
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.70

Activity Summary

Ki 1 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.44 8.44 3.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 3.6 nM 8.44 Inhibition of human dopamine D4.2 receptor 28489950

Literature References

PubMed DOI Target Context # Activities
28489950 10.1021/acs.jmedchem.7b00151 D(3) dopamine receptor 1
28489950 10.1021/acs.jmedchem.7b00151 5-hydroxytryptamine receptor 1A 1
28489950 10.1021/acs.jmedchem.7b00151 5-hydroxytryptamine receptor 2A 1
28489950 10.1021/acs.jmedchem.7b00151 Alpha-2A adrenergic receptor 1
28489950 10.1021/acs.jmedchem.7b00151 Unchecked 1
33422983 10.1016/j.ejmech.2020.113141 D(4) dopamine receptor 1
33422983 10.1016/j.ejmech.2020.113141 D(2) dopamine receptor 1
33422983 10.1016/j.ejmech.2020.113141 D(3) dopamine receptor 1

Data from ChEMBL 36 via Core Engine