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Compound Detail

CHEMBL3319525

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COc1cc(C(O)(C(F)(F)F)C(F)(F)F)cnc1N1CCN(S(=O)(=O)c2ccc(N)nc2)CC1

Basic Information

ChEMBL ID CHEMBL3319525
Phase Preclinical
Structure Type MOL
InChI Key HXCTZGRWJSQPPB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

515.4
MW (Da)
1.89
ALogP
8
HBA
2
HBD
121.9
PSA (Ų)
0.58
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H19F6N5O4S
MW 515.44
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.04

Activity Summary

IC50 1 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexokinase-4
CHEMBL3820
IC50 5.96 5.96 1110.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.0 mL.min-1.g-1 Homo sapiens
CL 14.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hexokinase-4 IC50 = 1110.0 nM 5.96 Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human... 25001129

Literature References

PubMed DOI Target Context # Activities
25001129 10.1021/jm5001979 Liver microsome 2
25001129 10.1021/jm5001979 Hexokinase-4 1

Data from ChEMBL 36 via Core Engine