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Compound Detail

CHEMBL4453866

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Cc1ccc2oc(-c3ccc(C)s3)c(O)c(=O)c2c1

Basic Information

ChEMBL ID CHEMBL4453866
Phase Preclinical
Structure Type MOL
InChI Key CWDVDIDTPJCYHQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

272.3
MW (Da)
3.84
ALogP
4
HBA
1
HBD
50.4
PSA (Ų)
0.73
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H12O3S
MW 272.32
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -0.17

Activity Summary

EC50 1 meas. best 5.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
EC50 5.48 5.48 3300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei EC50 = 3300.0 nM 5.48 Antitrypanosomal activity against Trypanosoma brucei bloodstream form assessed a... 31542713

Literature References

PubMed DOI Target Context # Activities
31542713 10.1016/j.ejmech.2019.111676 Unchecked 1
31542713 10.1016/j.ejmech.2019.111676 786-0 1
31542713 10.1016/j.ejmech.2019.111676 A549 1
31542713 10.1016/j.ejmech.2019.111676 Voltage-gated inwardly rectifying potassium channel KCNH2 1
31542713 10.1016/j.ejmech.2019.111676 Cytochrome P450 1A2 1
31542713 10.1016/j.ejmech.2019.111676 Cytochrome P450 2C9 1
31542713 10.1016/j.ejmech.2019.111676 Cytochrome P450 2C19 1
31542713 10.1016/j.ejmech.2019.111676 Cytochrome P450 2D6 1
31542713 10.1016/j.ejmech.2019.111676 Cytochrome P450 3A4 1
31542713 10.1016/j.ejmech.2019.111676 Trypanosoma brucei 1
31542713 10.1016/j.ejmech.2019.111676 THP-1 1

Data from ChEMBL 36 via Core Engine