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Compound Detail

CHEMBL1783749

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CCS(=O)(=O)c1ccn([C@@H](CC2CCOCC2)C(=O)Nc2ccc(C)cn2)c(=O)c1

Basic Information

ChEMBL ID CHEMBL1783749
Phase Preclinical
Structure Type MOL
InChI Key ZOHCYUHMSMYXBB-SFHVURJKSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
2
Publications
0
Known Names

Molecular Properties

433.5
MW (Da)
2.34
ALogP
7
HBA
1
HBD
107.4
PSA (Ų)
0.72
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H27N3O5S
MW 433.53
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.36

Activity Summary

EC50 1 meas. best 5.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexokinase-4
CHEMBL3820
EC50 5.82 5.82 1500.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 18.0 mL.min-1.kg-1 Rattus norvegicus
CL 5.0 mL.min-1.kg-1 Homo sapiens
T1/2 2.0 hr Rattus norvegicus
T1/2 2.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hexokinase-4 EC50 = 1500.0 nM 5.82 Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophoto... 19435665

Literature References

PubMed DOI Target Context # Activities
19435665 10.1016/j.bmcl.2009.04.107 Liver microsomes 4
19435665 10.1016/j.bmcl.2009.04.107 Hexokinase-4 2

Data from ChEMBL 36 via Core Engine