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Compound Detail

CHEMBL1946744

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O=C(CCCCN1[C@@H]2CC[C@H]1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL1946744
Phase Preclinical
Structure Type MOL
InChI Key SGGMEYGWAJEGIP-WPUZRXDDSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

455.0
MW (Da)
5.82
ALogP
5
HBA
1
HBD
53.4
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27ClN2O2S
MW 455.02
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.91

Activity Summary

Ki 3 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 7.8 7.8 16.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.75 6.75 180.0 1
D(4) dopamine receptor
CHEMBL3361
Ki 6.29 6.29 508.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22336245 10.1016/j.bmc.2012.01.022 Unchecked 2
22336245 10.1016/j.bmc.2012.01.022 5-hydroxytryptamine receptor 2A 1
22336245 10.1016/j.bmc.2012.01.022 5-hydroxytryptamine receptor 1A 1
22336245 10.1016/j.bmc.2012.01.022 D(2) dopamine receptor 1
22336245 10.1016/j.bmc.2012.01.022 D(3) dopamine receptor 1
22336245 10.1016/j.bmc.2012.01.022 D(4) dopamine receptor 1
22336245 10.1016/j.bmc.2012.01.022 Histamine H1 receptor 1
22336245 10.1016/j.bmc.2012.01.022 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine