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Compound Detail

CHEMBL4519186

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CCNC1=N[C@@H]2[C@@H](OC)[C@H](O)[C@@H](CO)O[C@@H]2S1

Basic Information

ChEMBL ID CHEMBL4519186
Phase Preclinical
Structure Type MOL
InChI Key JRZSXVZVOPYSIU-JGKVKWKGSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

262.3
MW (Da)
-0.84
ALogP
7
HBA
3
HBD
83.3
PSA (Ų)
0.62
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H18N2O4S
MW 262.33
Aromatic Rings 0
Heavy Atoms 17
NP-Likeness 1.12

Activity Summary

Ki 1 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein O-GlcNAcase
CHEMBL5921
Ki 6.57 6.57 270.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein O-GlcNAcase Ki = 270.0 nM 6.57 Inhibition of recombinant human OGA 31487175

Literature References

PubMed DOI Target Context # Activities
31487175 10.1021/acs.jmedchem.9b01090 Protein O-GlcNAcase 1
31487175 10.1021/acs.jmedchem.9b01090 Beta-hexosaminidase subunit beta 1
31487175 10.1021/acs.jmedchem.9b01090 Voltage-gated inwardly rectifying potassium channel KCNH2 1
31487175 10.1021/acs.jmedchem.9b01090 Sodium channel protein type 5 subunit alpha 1
31487175 10.1021/acs.jmedchem.9b01090 Voltage-dependent L-type calcium channel subunit alpha-1C 1
31487175 10.1021/acs.jmedchem.9b01090 Cytochrome P450 3A4 1
31487175 10.1021/acs.jmedchem.9b01090 Cytochrome P450 2D6 1
31487175 10.1021/acs.jmedchem.9b01090 Cytochrome P450 2C9 1
31487175 10.1021/acs.jmedchem.9b01090 Nuclear receptor subfamily 1 group I member 2 1

Data from ChEMBL 36 via Core Engine