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Compound Detail

CHEMBL427826

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CC1(C)N=C(N)N=C(N)N1c1ccc(C(F)(F)F)cc1

Basic Information

ChEMBL ID CHEMBL427826
Phase Preclinical
Structure Type MOL
InChI Key ROTRAHDYGVFVQU-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

285.3
MW (Da)
1.89
ALogP
5
HBA
2
HBD
80.0
PSA (Ų)
0.83
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H14F3N5
MW 285.27
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -0.70

Activity Summary

Ki 3 meas. best 6.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1926
Ki 6.88 6.88 131.8 1
Dihydrofolate reductase
CHEMBL2575
Ki 6.77 6.77 169.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7241512 10.1021/jm00137a013 Dihydrofolate reductase 2
6699880 10.1021/jm00369a019 Dihydrofolate reductase 2
6420569 10.1021/jm00368a006 Dihydrofolate reductase 2
7699713 10.1021/jm00006a016 Dihydrofolate reductase 1
6694162 10.1021/jm00368a007 Dihydrofolate reductase 1
6737433 10.1021/jm00373a016 Dihydrofolate reductase 1
6864738 10.1021/jm00361a012 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine