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Compound Detail

CHEMBL4476839

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CNC1=N[C@@H]2[C@H](F)[C@H](O)[C@@H](CF)O[C@@H]2S1

Basic Information

ChEMBL ID CHEMBL4476839
Phase Preclinical
Structure Type MOL
InChI Key XFEVUYIVNQYKSO-IECVIRLLSA-N
2
Targets
2
Activities
2
Assay Types
5
PK Parameters
3
Publications
0
Known Names

Molecular Properties

238.3
MW (Da)
0.07
ALogP
5
HBA
2
HBD
53.9
PSA (Ų)
0.68
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C8H12F2N2O2S
MW 238.26
Aromatic Rings 0
Heavy Atoms 15
NP-Likeness 0.25

Activity Summary

EC50 1 meas. best 6.48
Ki 1 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein O-GlcNAcase
CHEMBL5921
Ki 7.46 7.46 35.0 1
Protein O-GlcNAcase
CHEMBL3351213
EC50 6.48 6.48 328.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.4 mL.min-1.kg-1 Rattus norvegicus
F 60.5 % Rattus norvegicus
Fu 0.99 - Homo sapiens
Fu 0.99 - Rattus norvegicus
T1/2 1.18 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31487175 10.1021/acs.jmedchem.9b01090 ADMET 8
31487175 10.1021/acs.jmedchem.9b01090 Protein O-GlcNAcase 2
31487175 10.1021/acs.jmedchem.9b01090 Beta-hexosaminidase subunit beta 1

Data from ChEMBL 36 via Core Engine