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Compound Detail

CHEMBL278261

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CN(Cc1c[nH]c2nc(N)nc(N)c12)c1cccc2ccccc12

Basic Information

ChEMBL ID CHEMBL278261
Phase Preclinical
Structure Type MOL
InChI Key VGMMWZWEERBTOC-UHFFFAOYSA-N
2
Targets
9
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

318.4
MW (Da)
2.91
ALogP
5
HBA
3
HBD
96.8
PSA (Ų)
0.54
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 C18H18N6
MW 318.38
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -0.91

Activity Summary

IC50 9 meas. best 6.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 6.06 6.06 870.0 3
Dihydrofolate reductase
CHEMBL2363
IC50 5.09 5.09 8200.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15743188 10.1021/jm040153n Dihydrofolate reductase 4
9089339 10.1021/jm960717q Dihydrofolate reductase 2
15743188 10.1021/jm040153n Bifunctional dihydrofolate reductase-thymidylate synthase 2
9089339 10.1021/jm960717q Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine