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Compound Detail

CHEMBL83899

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COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(C)(=O)=O)CC1

Basic Information

ChEMBL ID CHEMBL83899
Phase Preclinical
Structure Type MOL
InChI Key UATDVRSFFGFTAI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

418.0
MW (Da)
2.15
ALogP
6
HBA
2
HBD
101.7
PSA (Ų)
0.47
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H28ClN3O4S
MW 417.96
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -1.19

Activity Summary

EC50 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
EC50 8.6 8.6 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 4 EC50 = 2.512 nM 8.6 Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(01)80413-3 5-hydroxytryptamine receptor 4 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
12540230 10.1021/jm020099f 5-hydroxytryptamine receptor 4 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1

Data from ChEMBL 36 via Core Engine