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Compound Detail

CHEMBL331292

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COc1cc(CC2CN=C(N)N=C2N)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL331292
Phase Preclinical
Structure Type MOL
InChI Key POWGIEXWLGAZNH-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

292.3
MW (Da)
0.56
ALogP
7
HBA
2
HBD
104.5
PSA (Ų)
0.82
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H20N4O3
MW 292.34
Aromatic Rings 1
Heavy Atoms 21
NP-Likeness 0.51

Activity Summary

IC50 4 meas. best 6.52
Ki 1 meas. best 8.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1809
Ki 8.87 8.87 1.3 1
Dihydrofolate reductase
CHEMBL5457
IC50 6.52 6.52 300.0 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 5.55 5.55 2800.0 1
Dihydrofolate reductase
CHEMBL1926
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15214795 10.1021/jm0306327 Dihydrofolate reductase 3
15214795 10.1021/jm0306327 Unchecked 3
8784450 10.1021/jm960197z Dihydrofolate reductase 1
15214795 10.1021/jm0306327 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine