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Compound Detail

CHEMBL52415

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COc1cc(Cc2cnc(N)nc2N)cc(C#Cc2ccc(C(=O)O)cc2)c1OC

Basic Information

ChEMBL ID CHEMBL52415
Phase Preclinical
Structure Type MOL
InChI Key KZSFROFZPJXGFV-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

404.4
MW (Da)
2.35
ALogP
7
HBA
3
HBD
133.6
PSA (Ų)
0.55
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 C22H20N4O4
MW 404.43
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.17

Activity Summary

IC50 4 meas. best 8.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL5457
IC50 8.09 8.09 8.2 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 6.38 6.38 420.0 1
Dihydrofolate reductase
CHEMBL1926
IC50 5.92 5.92 1200.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 4.06 4.06 88000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15026078 10.1016/j.bmcl.2003.12.103 Dihydrofolate reductase 3
15026078 10.1016/j.bmcl.2003.12.103 Unchecked 3
15026078 10.1016/j.bmcl.2003.12.103 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine