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Compound Detail

CHEMBL3219107

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C[C@@H](CO)Oc1cc(Oc2ccc(C(=O)N3CCC3)cc2)cc(C(=O)Nc2cc[nH]n2)c1

Basic Information

ChEMBL ID CHEMBL3219107
Phase Preclinical
Structure Type MOL
InChI Key KIPZZZALTNYLEP-HNNXBMFYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
3.06
ALogP
6
HBA
3
HBD
116.8
PSA (Ų)
0.50
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24N4O5
MW 436.47
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.35

Activity Summary

EC50 1 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexokinase-4
CHEMBL3820
EC50 7.28 7.28 53.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hexokinase-4 EC50 = 53.0 nM 7.28 Inhibition of recombinant human pancreatic glucokinase by G-6-P dehydrogenase as... -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C2MD20077E No relevant target 2
- 10.1039/C2MD20077E Hexokinase-4 1
- 10.1039/C2MD20077E MDCK 1
- 10.1039/C2MD20077E Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine