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Compound Detail

CHEMBL368645

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COc1cc(N2C=Cc3c(cnc4nc(N)nc(N)c34)C2)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL368645
Phase Preclinical
Structure Type MOL
InChI Key BIGRVUZNHBDRLI-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

380.4
MW (Da)
2.21
ALogP
9
HBA
2
HBD
121.6
PSA (Ų)
0.70
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 C19H20N6O3
MW 380.41
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.08

Activity Summary

IC50 6 meas. best 6.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL2363
IC50 6.33 6.33 469.9 2
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 6.12 6.12 760.0 2
Dihydrofolate reductase
CHEMBL1926
IC50 5.34 5.34 4600.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15743188 10.1021/jm040153n Dihydrofolate reductase 4
15743188 10.1021/jm040153n Bifunctional dihydrofolate reductase-thymidylate synthase 2

Data from ChEMBL 36 via Core Engine