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Compound Detail

CHEMBL6671

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CC1(C)N=C(N)N=C(N)N1c1cccc(OCCCCOc2cccc(C(F)(F)F)c2)c1

Basic Information

ChEMBL ID CHEMBL6671
Phase Preclinical
Structure Type MOL
InChI Key MMMVJJCCSPZNKF-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

449.5
MW (Da)
4.13
ALogP
7
HBA
2
HBD
98.5
PSA (Ų)
0.59
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26F3N5O2
MW 449.48
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.79

Activity Summary

Ki 4 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1926
Ki 8.24 8.24 5.8 1
Dihydrofolate reductase
CHEMBL2575
Ki 7.54 7.54 28.8 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL4614
Ki 7.12 7.12 75.9 1
Dihydrofolate reductase
CHEMBL2902
Ki 5.87 5.87 1349.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6699880 10.1021/jm00369a019 Dihydrofolate reductase 2
6420569 10.1021/jm00368a006 Dihydrofolate reductase 2
7699713 10.1021/jm00006a016 Dihydrofolate reductase 1
3599028 10.1021/jm00390a017 Bifunctional dihydrofolate reductase-thymidylate synthase 1
6796688 10.1021/jm00144a010 Dihydrofolate reductase 1
6864738 10.1021/jm00361a012 Dihydrofolate reductase 1
7057420 10.1021/jm00344a012 L5178Y 1
7057421 10.1021/jm00344a013 L5178Y 1

Data from ChEMBL 36 via Core Engine