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Compound Detail

CHEMBL492414

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C=CCOc1cc(OC)c(C(=O)/C=C/c2ccccn2)c(OCC=C)c1

Basic Information

ChEMBL ID CHEMBL492414
Phase Preclinical
Structure Type MOL
InChI Key YUGPSTFHGKEVHQ-MDZDMXLPSA-N
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

351.4
MW (Da)
4.12
ALogP
5
HBA
0
HBD
57.6
PSA (Ų)
0.37
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21NO4
MW 351.40
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.29

Activity Summary

IC50 7 meas. best 6.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Leishmania amazonensis
CHEMBL612877
IC50 6.05 6.005 900.0 2
Leishmania braziliensis
CHEMBL612878
IC50 5.85 5.85 1400.0 1
Trypanosoma cruzi
CHEMBL368
IC50 5.72 5.72 1900.0 1
Vero
CHEMBL391
IC50 5.55 5.55 2800.0 1
Leishmania peruviana
CHEMBL613215
IC50 5.4 5.4 4000.0 1
ADMET
CHEMBL612558
IC50 4.9 4.9 12500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19962891 10.1016/j.bmcl.2009.11.033 Leishmania amazonensis 4
18798609 10.1021/jm800812k Trypanosoma cruzi 1
18798609 10.1021/jm800812k Unchecked 1
18798609 10.1021/jm800812k Vero 1
19962891 10.1016/j.bmcl.2009.11.033 Unchecked 1
19962891 10.1016/j.bmcl.2009.11.033 ADMET 1
19962891 10.1016/j.bmcl.2009.11.033 Leishmania peruviana 1
19962891 10.1016/j.bmcl.2009.11.033 Leishmania braziliensis 1

Data from ChEMBL 36 via Core Engine