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Compound Detail

CHEMBL66114

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COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL66114
Phase Preclinical
Structure Type MOL
InChI Key BKVIWGRFRKLFIO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
9
Publications
0
Known Names

Molecular Properties

554.1
MW (Da)
3.74
ALogP
8
HBA
2
HBD
120.2
PSA (Ų)
0.28
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H36ClN3O6S
MW 554.11
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -1.00

Activity Summary

Ki 1 meas. best 9.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL5017
Ki 9.13 9.13 0.7 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 5.25 hr Sus scrofa

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00358-Z Sus scrofa 2
- 10.1016/S0960-894X(01)80414-5 5-hydroxytryptamine receptor 4 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.1016/0960-894X(95)00358-Z 5-hydroxytryptamine receptor 4 1
- 10.1016/0960-894X(95)00358-Z ADMET 1
12540230 10.1021/jm020099f Rattus norvegicus 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