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Compound Detail

CHEMBL48648

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Nc1nc(N)c2c(CNc3cccc4c3CCCC4)c[nH]c2n1

Basic Information

ChEMBL ID CHEMBL48648
Phase Preclinical
Structure Type MOL
InChI Key CAYFHAJGILGDLV-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

308.4
MW (Da)
2.61
ALogP
5
HBA
4
HBD
105.6
PSA (Ų)
0.59
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H20N6
MW 308.39
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.83

Activity Summary

IC50 4 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 5.96 5.96 1096.5 3
Dihydrofolate reductase
CHEMBL2363
IC50 4.23 4.23 59300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20117005 10.1016/j.bmc.2009.12.066 Bifunctional dihydrofolate reductase-thymidylate synthase 2
12699390 10.1021/jm020466n Bifunctional dihydrofolate reductase-thymidylate synthase 1
12699390 10.1021/jm020466n Dihydrofolate reductase; T. gondii vs rat 1
20117005 10.1016/j.bmc.2009.12.066 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine