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Compound Detail

CHEMBL4225326

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CC1(C)[C@H]2CC=C(CCOC(=O)Cc3ccc(OC/C=C/S(=O)(=O)c4ccccc4)c(Cl)c3)[C@@H]1C2

Basic Information

ChEMBL ID CHEMBL4225326
Phase Preclinical
Structure Type MOL
InChI Key RVJMVDHAZHFEHW-WZHOGVQSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

515.1
MW (Da)
6.17
ALogP
5
HBA
0
HBD
69.7
PSA (Ų)
0.28
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31ClO5S
MW 515.07
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness 0.22

Activity Summary

IC50 1 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
IC50 5.52 5.52 3040.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei IC50 = 3040.0 nM 5.52 Antitrypanosomal activity against Trypanosoma brucei 427 bloodstream forms asses... 29609908

Literature References

PubMed DOI Target Context # Activities
29609908 10.1016/j.bmcl.2018.03.039 Trypanosoma brucei 1
29609908 10.1016/j.bmcl.2018.03.039 HepG2 1
29609908 10.1016/j.bmcl.2018.03.039 Rhodesain 1

Data from ChEMBL 36 via Core Engine