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Compound Detail

CHEMBL4062553

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COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)C1

Basic Information

ChEMBL ID CHEMBL4062553
Phase Preclinical
Structure Type MOL
InChI Key AKUFOSYLIYVIGY-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

477.7
MW (Da)
4.97
ALogP
7
HBA
0
HBD
46.4
PSA (Ų)
0.34
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H35N5OS
MW 477.68
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.61

Activity Summary

Ki 5 meas. best 7.71

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 7.71 7.71 19.6 2
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.14 6.14 724.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.21 5.21 6168.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29125762 10.1021/acs.jmedchem.7b01248 D(3) dopamine receptor 3
29125762 10.1021/acs.jmedchem.7b01248 D(2) dopamine receptor 1
29125762 10.1021/acs.jmedchem.7b01248 Unchecked 1
29125762 10.1021/acs.jmedchem.7b01248 5-hydroxytryptamine receptor 1A 1
29125762 10.1021/acs.jmedchem.7b01248 5-hydroxytryptamine receptor 2A 1
29125762 10.1021/acs.jmedchem.7b01248 5-hydroxytryptamine receptor 2C 1
31021617 10.1021/acs.jmedchem.9b00412 D(3) dopamine receptor 1
31021617 10.1021/acs.jmedchem.9b00412 D(2) dopamine receptor 1
31021617 10.1021/acs.jmedchem.9b00412 Unchecked 1

Data from ChEMBL 36 via Core Engine