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Compound Detail

CHEMBL597961

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Nc1nc(N)c2c(CCCc3ccc(OCc4ccccc4)cc3)c[nH]c2n1

Basic Information

ChEMBL ID CHEMBL597961
Phase Preclinical
Structure Type MOL
InChI Key AYHBAWVKXMFVHV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

373.5
MW (Da)
3.88
ALogP
5
HBA
3
HBD
102.8
PSA (Ų)
0.46
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N5O
MW 373.46
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -0.36

Activity Summary

IC50 2 meas. best 6.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL2363
IC50 6.18 6.18 660.0 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20117005 10.1016/j.bmc.2009.12.066 Dihydrofolate reductase 1
20117005 10.1016/j.bmc.2009.12.066 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine