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Compound Detail

CHEMBL82833

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COc1cc(N)c(Cl)cc1C(=O)CCC1CCNCC1

Basic Information

ChEMBL ID CHEMBL82833
Phase Preclinical
Structure Type MOL
InChI Key BHUVUNZKZDLBRF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

296.8
MW (Da)
2.89
ALogP
4
HBA
2
HBD
64.3
PSA (Ų)
0.65
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H21ClN2O2
MW 296.80
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -0.25

Activity Summary

EC50 1 meas. best 6.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
EC50 6.9 6.9 125.9 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.34 - Sepia officinalis

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 4 EC50 = 125.89 nM 6.9 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
30398862 10.1021/acs.jmedchem.8b01281 Unchecked 1
30398862 10.1021/acs.jmedchem.8b01281 No relevant target 1

Data from ChEMBL 36 via Core Engine