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Compound Detail

CHEMBL5395058

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O=C1CCCN1c1ccc(Sc2ccccc2CO)c(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL5395058
Phase Preclinical
Structure Type MOL
InChI Key AMBVMYANOKPCMK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
3
Publications
0
Known Names

Molecular Properties

367.4
MW (Da)
4.48
ALogP
3
HBA
1
HBD
40.5
PSA (Ų)
0.87
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H16F3NO2S
MW 367.39
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.04

Activity Summary

IC50 1 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 7.5 7.5 31.6 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 485.0 ng.hr.mL-1 Mus musculus
AUC 530.0 ng.hr.mL-1 Mus musculus
CL 31.49 mL.min-1.g-1 Mus musculus
CL 11.51 mL.min-1.g-1 Homo sapiens
Cmax 819.29 nM Mus musculus
T1/2 0.07967 hr Mus musculus
T1/2 0.03517 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 = 31.62 nM 7.5 Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigotes ass... 36626662

Literature References

PubMed DOI Target Context # Activities
36626662 10.1021/acs.jmedchem.2c01725 ADMET 9
36626662 10.1021/acs.jmedchem.2c01725 Trypanosoma cruzi 2
36626662 10.1021/acs.jmedchem.2c01725 H9c2 1

Data from ChEMBL 36 via Core Engine