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Compound Detail

CHEMBL4467528

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CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C.Cl

Basic Information

ChEMBL ID CHEMBL4467528
Phase Preclinical
Structure Type MOL
InChI Key OHFDSJPIFZIHFX-UHFFFAOYSA-N
Parent Compound CHEMBL4596340
Active Moiety CHEMBL4596340
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

454.6
MW (Da)
5.24
ALogP
6
HBA
0
HBD
43.2
PSA (Ų)
0.29
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H32ClFN4OS
MW 491.08
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.66

Activity Summary

Ki 3 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 6.26 6.26 549.6 1
D(4) dopamine receptor
CHEMBL219
Ki 6.0 6.0 988.6 1
D(1A) dopamine receptor
CHEMBL2056
Ki 5.95 5.95 1122.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32282200 10.1021/acs.jmedchem.9b01835 D(2) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 D(1A) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 D(3) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 D(4) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 D(1B) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine