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Compound Detail

CHEMBL34641

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COc1ccc(/C=C/COc2ccccc2C(=O)O)cc1Cc1cnc(N)nc1N

Basic Information

ChEMBL ID CHEMBL34641
Phase Preclinical
Structure Type MOL
InChI Key DINWCFBBTDJSMT-SNAWJCMRSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

406.4
MW (Da)
3.03
ALogP
7
HBA
3
HBD
133.6
PSA (Ų)
0.52
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22N4O4
MW 406.44
Aromatic Rings 3
Heavy Atoms 30

Activity Summary

IC50 4 meas. best 6.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL5457
IC50 6.42 6.42 380.0 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 5.6 5.6 2500.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 5.19 5.19 6400.0 1
Dihydrofolate reductase
CHEMBL1926
IC50 5.07 5.07 8600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14998335 10.1021/jm030438k Dihydrofolate reductase 6
14998335 10.1021/jm030438k Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine