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Compound Detail

CHEMBL4073330

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O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2o1

Basic Information

ChEMBL ID CHEMBL4073330
Phase Preclinical
Structure Type MOL
InChI Key FSLWZIRTOUAUNP-UHFFFAOYSA-N
5
Targets
7
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
3.13
ALogP
8
HBA
1
HBD
83.5
PSA (Ų)
0.35
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 C24H26N4O4
MW 434.50
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.70

Activity Summary

Ki 7 meas. best 8.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 8.07 8.07 8.5 1
Unchecked
CHEMBL612545
Ki 7.77 7.285 17.0 2
D(2) dopamine receptor
CHEMBL217
Ki 7.72 7.56 19.0 2
D(4) dopamine receptor
CHEMBL219
Ki 6.57 6.57 270.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.55 5.55 2800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28489379 10.1021/acs.jmedchem.7b00363 D(2) dopamine receptor 4
28489379 10.1021/acs.jmedchem.7b00363 Unchecked 2
28489379 10.1021/acs.jmedchem.7b00363 D(1A) dopamine receptor 1
28489379 10.1021/acs.jmedchem.7b00363 D(3) dopamine receptor 1
28489379 10.1021/acs.jmedchem.7b00363 D(4) dopamine receptor 1
28489379 10.1021/acs.jmedchem.7b00363 D(1B) dopamine receptor 1
28489379 10.1021/acs.jmedchem.7b00363 5-hydroxytryptamine receptor 2A 1
28489379 10.1021/acs.jmedchem.7b00363 HEK293 1

Data from ChEMBL 36 via Core Engine