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Compound Detail

CHEMBL495327

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CCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1

Basic Information

ChEMBL ID CHEMBL495327
Phase Preclinical
Structure Type MOL
InChI Key QKVIHOUAEYBMIJ-OPXMRZJTSA-N
4
Targets
7
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

490.7
MW (Da)
5.83
ALogP
5
HBA
2
HBD
71.2
PSA (Ų)
0.42
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H38N4OS
MW 490.72
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.21

Activity Summary

Ki 7 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL3138
Ki 9.4 9.1533 0.4 3
D(2) dopamine receptor
CHEMBL339
Ki 7.04 6.775 92.0 2
Unchecked
CHEMBL612545
Ki 6.73 6.73 185.0 1
D(1A) dopamine receptor
CHEMBL265
Ki 5.47 5.47 3400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22871578 10.1016/j.bmcl.2012.07.003 Unchecked 3
22125662 10.1021/ml200100t Unchecked 3
18785726 10.1021/jm800471h Unchecked 2
18785726 10.1021/jm800471h D(3) dopamine receptor 1
18785726 10.1021/jm800471h D(2) dopamine receptor 1
18785726 10.1021/jm800471h D(1A) dopamine receptor 1
18785726 10.1021/jm800471h Rattus norvegicus 1
22871578 10.1016/j.bmcl.2012.07.003 D(3) dopamine receptor 1
22871578 10.1016/j.bmcl.2012.07.003 Dopamine receptor D2 and D3 1
22125662 10.1021/ml200100t No relevant target 1
22125662 10.1021/ml200100t D(2) dopamine receptor 1
22125662 10.1021/ml200100t D(3) dopamine receptor 1

Data from ChEMBL 36 via Core Engine