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Compound Detail

CHEMBL440334

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CCCCOc1c(CCC)cc(Cc2cnc(N)nc2N)cc1CCC

Basic Information

ChEMBL ID CHEMBL440334
Phase Preclinical
Structure Type MOL
InChI Key OXRGQGLRPYROQW-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

356.5
MW (Da)
4.32
ALogP
5
HBA
2
HBD
87.0
PSA (Ų)
0.62
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H32N4O
MW 356.51
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.05

Activity Summary

IC50 4 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL3963
IC50 8.24 8.24 5.8 1
Dihydrofolate reductase
CHEMBL1809
IC50 7.77 7.77 17.0 1
Dihydrofolate reductase
CHEMBL3565
IC50 6.88 6.88 132.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 4.82 4.82 15000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3100802 10.1021/jm00385a017 Dihydrofolate reductase 3
3100802 10.1021/jm00385a017 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine