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Compound Detail

CHEMBL3218478

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COCc1ccc(Oc2cc3[nH]c(-c4ccccn4)nc3cc2[C@H]2CCCN2C(C)=O)cn1

Basic Information

ChEMBL ID CHEMBL3218478
Phase Preclinical
Structure Type MOL
InChI Key KNZIMOVBOPUPJI-HSZRJFAPSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

443.5
MW (Da)
4.64
ALogP
6
HBA
1
HBD
93.2
PSA (Ų)
0.47
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25N5O3
MW 443.51
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.98

Activity Summary

EC50 2 meas. best 7.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexokinase-4
CHEMBL3820
EC50 7.06 7.06 88.0 1
Hexokinase-4
CHEMBL3882
EC50 6.73 6.73 187.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hexokinase-4 EC50 = 88.0 nM 7.06 Activation of recombinant human glucokinase assessed as formation of glucose-6-p... -
Hexokinase-4 EC50 = 187.0 nM 6.73 Activation of rat glucokinase -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C1MD00116G Hexokinase-4 2
- 10.1039/C1MD00116G Unchecked 1

Data from ChEMBL 36 via Core Engine