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Compound Detail

CHEMBL339058

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COc1cc(Cc2c(C)nc(N)nc2N)cc(OC)c1O

Basic Information

ChEMBL ID CHEMBL339058
Phase Preclinical
Structure Type MOL
InChI Key OWESLNUTAHNAGR-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

290.3
MW (Da)
1.26
ALogP
7
HBA
3
HBD
116.5
PSA (Ų)
0.78
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H18N4O3
MW 290.32
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness 0.01

Activity Summary

IC50 5 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1809
IC50 6.52 6.52 300.0 3
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL3963
IC50 6.32 6.32 480.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8941396 10.1021/jm960491r Dihydrofolate reductase 1
8941396 10.1021/jm960491r No relevant target 1
6991695 10.1021/jm00179a012 Dihydrofolate reductase 1
6991695 10.1021/jm00179a012 Bifunctional dihydrofolate reductase-thymidylate synthase 1
6991692 10.1021/jm00178a007 Dihydrofolate reductase 1
6991692 10.1021/jm00178a007 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine