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Compound Detail

CHEMBL5594139

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CC(=O)Nc1ncc(CN2CCC(C#Cc3cnc(OC(C)C)nc3)CC2)s1

Basic Information

ChEMBL ID CHEMBL5594139
Phase Preclinical
Structure Type MOL
InChI Key VUJPFYQQOBGWFC-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

399.5
MW (Da)
2.94
ALogP
7
HBA
1
HBD
80.2
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25N5O2S
MW 399.52
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.56

Activity Summary

EC50 1 meas. best 7.68
IC50 1 meas. best 7.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein O-GlcNAcase
CHEMBL5921
IC50 7.97 7.97 10.8 1
Protein O-GlcNAcase
CHEMBL3351213
EC50 7.68 7.68 20.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
39109492 10.1021/acs.jmedchem.4c01132 Protein O-GlcNAcase 2

Data from ChEMBL 36 via Core Engine