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Compound Detail

CHEMBL3910843

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Nc1nc(N)c(-c2c[nH]c3ccccc23)c(C2CC2)n1

Basic Information

ChEMBL ID CHEMBL3910843
Phase Preclinical
Structure Type MOL
InChI Key KVMGHEGICPHZIT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

265.3
MW (Da)
2.67
ALogP
4
HBA
3
HBD
93.6
PSA (Ų)
0.66
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H15N5
MW 265.32
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.10

Activity Summary

IC50 2 meas. best 6.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 6.04 6.04 910.0 1
Dihydrofolate reductase
CHEMBL202
IC50 5.6 5.6 2500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27994750 10.1021/acsmedchemlett.6b00328 Dihydrofolate reductase 1
27994750 10.1021/acsmedchemlett.6b00328 Bifunctional dihydrofolate reductase-thymidylate synthase 1
27994750 10.1021/acsmedchemlett.6b00328 Unchecked 1

Data from ChEMBL 36 via Core Engine