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Compound Detail

CHEMBL3763352

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COCCOc1cc(C2=NN(C3CCCCCC3)C(=O)[C@@H]3CC=CC[C@H]23)ccc1OC

Basic Information

ChEMBL ID CHEMBL3763352
Phase Preclinical
Structure Type MOL
InChI Key VZBSYCDYSSJMAN-LEWJYISDSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

426.6
MW (Da)
4.57
ALogP
5
HBA
0
HBD
60.4
PSA (Ų)
0.36
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H34N2O4
MW 426.56
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness -0.44

Activity Summary

EC50 1 meas. best 6.1
IC50 1 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Class 1 phosphodiesterase PDEB1
CHEMBL2010636
IC50 7.1 7.1 79.4 1
Trypanosoma brucei brucei
CHEMBL612851
EC50 6.1 6.1 794.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26935942 10.1016/j.bmc.2016.02.032 Class 1 phosphodiesterase PDEB1 1
26935942 10.1016/j.bmc.2016.02.032 Trypanosoma brucei brucei 1
26935942 10.1016/j.bmc.2016.02.032 MRC5 1
26935942 10.1016/j.bmc.2016.02.032 Unchecked 1

Data from ChEMBL 36 via Core Engine