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Compound Detail

CHEMBL5413185

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O=C1CCCN1c1ccc(S(=O)(=O)c2ccccc2CO)c(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL5413185
Phase Preclinical
Structure Type MOL
InChI Key QHMYYSZDAFKICE-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
3
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
3.16
ALogP
4
HBA
1
HBD
74.7
PSA (Ų)
0.86
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H16F3NO4S
MW 399.39
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.20

Activity Summary

IC50 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 6.6 6.6 251.2 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 208.0 ng.hr.mL-1 Mus musculus
CL 20.0 mL.min-1.g-1 Mus musculus
CL 12.5 mL.min-1.g-1 Homo sapiens
Cmax 438.17 nM Mus musculus
T1/2 0.07317 hr Mus musculus
T1/2 0.05533 hr Homo sapiens
Tmax 0.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma cruzi IC50 = 251.19 nM 6.6 Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigotes ass... 36626662

Literature References

PubMed DOI Target Context # Activities
36626662 10.1021/acs.jmedchem.2c01725 ADMET 7
36626662 10.1021/acs.jmedchem.2c01725 H9c2 1
36626662 10.1021/acs.jmedchem.2c01725 Trypanosoma cruzi 1

Data from ChEMBL 36 via Core Engine