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Compound Detail

CHEMBL4207270

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CCOC(=O)N1CCc2nc(NC(=O)c3cc(Oc4ccc(C(=O)N5CCC5)cc4)cc(O[C@@H](C)COC)c3)sc2C1

Basic Information

ChEMBL ID CHEMBL4207270
Phase Preclinical
Structure Type MOL
InChI Key VBAKJOSCGIWNTC-IBGZPJMESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

594.7
MW (Da)
4.96
ALogP
9
HBA
1
HBD
119.5
PSA (Ų)
0.35
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H34N4O7S
MW 594.69
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.69

Activity Summary

EC50 1 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexokinase-4
CHEMBL3820
EC50 6.64 6.64 230.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hexokinase-4 EC50 = 230.0 nM 6.64 Activation of recombinant human liver glucokinase 2 assessed as reduction in NAD... 28800453

Literature References

PubMed DOI Target Context # Activities
28800453 10.1016/j.ejmech.2017.07.051 Hexokinase-4 3
28800453 10.1016/j.ejmech.2017.07.051 Hepatocyte 1

Data from ChEMBL 36 via Core Engine