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Compound Detail

CHEMBL418347

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COc1cc(Cc2cnc(N)nc2N)cc(OCCCC(=O)O)c1OC

Basic Information

ChEMBL ID CHEMBL418347
Phase Preclinical
Structure Type MOL
InChI Key ZPHWDXVBIFAFRT-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

362.4
MW (Da)
1.49
ALogP
8
HBA
3
HBD
142.8
PSA (Ų)
0.57
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H22N4O5
MW 362.39
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.06

Activity Summary

Ki 3 meas. best 10.46
IC50 2 meas. best 5.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1809
Ki 10.46 10.46 0.0 3
Dihydrofolate reductase
CHEMBL2363
IC50 5.01 5.01 9700.0 1
Dihydrofolate reductase
CHEMBL2575
IC50 4.66 4.66 22000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3973902 10.1021/jm00381a008 Dihydrofolate reductase 4
20485427 10.1038/nature09107 Plasmodium falciparum 4
6754932 10.1021/jm00352a002 ADMET 1
6754932 10.1021/jm00352a002 Dihydrofolate reductase 1
3973902 10.1021/jm00381a008 Staphylococcus aureus 1
3973902 10.1021/jm00381a008 Escherichia coli 1
3973902 10.1021/jm00381a008 NON-PROTEIN TARGET 1
3973902 10.1021/jm00381a008 Proteus vulgaris 1
3290487 10.1021/jm00402a025 Dihydrofolate reductase 1
20485427 10.1038/nature09107 Unchecked 1
20485427 10.1038/nature09107 HepG2 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1
- 10.6019/CHEMBL3433997 Glucose transporter 1

Data from ChEMBL 36 via Core Engine