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Compound Detail

CHEMBL3759819

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O=S(=O)(NC1CC2CCC(C1)N2CCOc1cccc(-c2ccccc2)c1)c1cccc(Cl)c1

Basic Information

ChEMBL ID CHEMBL3759819
Phase Preclinical
Structure Type MOL
InChI Key FARUXTURXOFRQS-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

497.1
MW (Da)
5.36
ALogP
4
HBA
1
HBD
58.6
PSA (Ų)
0.46
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 C27H29ClN2O3S
MW 497.06
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.35

Activity Summary

Ki 6 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 7.85 7.85 14.0 1
D(2) dopamine receptor
CHEMBL217
Ki 7.03 7.03 94.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.59 6.59 254.0 1
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 6.49 6.49 325.0 1
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 6.13 6.13 742.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.94 5.94 1146.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26698537 10.1016/j.ejmech.2015.11.040 5-hydroxytryptamine receptor 7 4
26698537 10.1016/j.ejmech.2015.11.040 Mus musculus 2
26698537 10.1016/j.ejmech.2015.11.040 5-hydroxytryptamine receptor 1A 1
26698537 10.1016/j.ejmech.2015.11.040 5-hydroxytryptamine receptor 2A 1
26698537 10.1016/j.ejmech.2015.11.040 5-hydroxytryptamine receptor 6 1
26698537 10.1016/j.ejmech.2015.11.040 D(2) dopamine receptor 1
26698537 10.1016/j.ejmech.2015.11.040 Adrenergic receptor alpha-1 1
26698537 10.1016/j.ejmech.2015.11.040 Unchecked 1

Data from ChEMBL 36 via Core Engine