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Compound Detail

CHEMBL2171657

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COc1ccc(CCOc2cc(C3=NN(C(C)C)C(=O)C3(C)C)ccc2OC)cc1

Basic Information

ChEMBL ID CHEMBL2171657
Phase Preclinical
Structure Type MOL
InChI Key ZISXSDNULHNXTK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

410.5
MW (Da)
4.31
ALogP
5
HBA
0
HBD
60.4
PSA (Ų)
0.65
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N2O4
MW 410.51
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.13

Activity Summary

IC50 2 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Class 1 phosphodiesterase PDEB1
CHEMBL2010636
IC50 6.08 6.08 830.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 4.5 4.5 32000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22963052 10.1021/jm301059b MRC5 1
22963052 10.1021/jm301059b Trypanosoma brucei brucei 1
22963052 10.1021/jm301059b Class 1 phosphodiesterase PDEB1 1

Data from ChEMBL 36 via Core Engine