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Compound Detail

CHEMBL3930739

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Nc1ncc(CN2CCN(c3cccc(C(F)(F)F)c3)CC2)c(N)n1

Basic Information

ChEMBL ID CHEMBL3930739
Phase Preclinical
Structure Type MOL
InChI Key RXKNPXKSCJSKNO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

352.4
MW (Da)
1.98
ALogP
6
HBA
2
HBD
84.3
PSA (Ų)
0.88
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 C16H19F3N6
MW 352.36
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.65

Activity Summary

IC50 2 meas. best 5.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL202
IC50 5.04 5.04 9200.0 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 4.1 4.1 80000.0 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