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Compound Detail

CHEMBL4076516

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COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)C2)C1

Basic Information

ChEMBL ID CHEMBL4076516
Phase Preclinical
Structure Type MOL
InChI Key ICBYLQHTUDFHNY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

463.6
MW (Da)
4.58
ALogP
7
HBA
0
HBD
46.4
PSA (Ų)
0.36
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 C26H33N5OS
MW 463.65
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.69

Activity Summary

Ki 2 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 7.62 7.62 24.2 1
D(2) dopamine receptor
CHEMBL217
Ki 5.2 5.2 6370.0 1

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

Data from ChEMBL 36 via Core Engine