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Compound Detail

CHEMBL588641

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COc1cc(F)c2ncc(C#N)c(CCN3CCC(NCc4ccc5c(c4)OCCO5)CC3)c2c1.Cl

Basic Information

ChEMBL ID CHEMBL588641
Phase Preclinical
Structure Type MOL
InChI Key IMXHONGQIJILET-UHFFFAOYSA-N
Parent Compound CHEMBL526044
Active Moiety CHEMBL526044
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
3.82
ALogP
7
HBA
1
HBD
79.6
PSA (Ų)
0.56
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 C27H30ClFN4O3
MW 513.01
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.18

Activity Summary

IC50 3 meas. best 6.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexose transporter 1
CHEMBL4697
IC50 6.04 6.04 911.0 1
Solute carrier family 2, facilitated glucose transporter member 1
CHEMBL2535
IC50 5.81 5.81 1549.0 1
Glucose transporter
CHEMBL3431938
IC50 5.76 5.76 1731.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
- 10.6019/CHEMBL3433997 Hexose transporter 1 2
- 10.6019/CHEMBL3433997 Glucose transporter 2
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 2
20485427 10.1038/nature09107 Unchecked 1
20485427 10.1038/nature09107 HepG2 1

Data from ChEMBL 36 via Core Engine