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Compound Detail

CHEMBL4514586

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COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C.Cl

Basic Information

ChEMBL ID CHEMBL4514586
Phase Preclinical
Structure Type MOL
InChI Key VYHRVDZNMSGPDZ-UHFFFAOYSA-N
Parent Compound CHEMBL4595727
Active Moiety CHEMBL4595727
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

426.6
MW (Da)
4.51
ALogP
6
HBA
1
HBD
52.0
PSA (Ų)
0.38
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28ClFN4OS
MW 463.02
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.32

Activity Summary

Ki 5 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 7.05 7.05 89.8 1
D(4) dopamine receptor
CHEMBL219
Ki 6.88 6.88 132.8 1
D(2) dopamine receptor
CHEMBL217
Ki 6.6 6.6 253.1 1
D(1A) dopamine receptor
CHEMBL2056
Ki 6.2 6.2 631.0 1
D(1B) dopamine receptor
CHEMBL1850
Ki 6.03 6.03 926.1 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