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Compound Detail

CHEMBL268453

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C#CCN(Cc1cc2c(O)nc(C)nc2cc1C)c1ccc(C(=O)NCc2cccc([N+](=O)[O-])c2)c(F)c1

Basic Information

ChEMBL ID CHEMBL268453
Phase Preclinical
Structure Type MOL
InChI Key QDONLEJFIXLJSK-UHFFFAOYSA-N
3
Targets
7
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

513.5
MW (Da)
4.57
ALogP
7
HBA
2
HBD
121.5
PSA (Ų)
0.20
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H24FN5O4
MW 513.53
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.89

Activity Summary

IC50 7 meas. best 7.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL3160
IC50 7.36 7.36 44.0 2
L1210 (1565)
CHEMBL614000
IC50 6.75 6.41 180.0 2
L1210
CHEMBL386
IC50 6.68 5.8133 210.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7699716 10.1021/jm00006a019 L1210 2
7699716 10.1021/jm00006a019 L1210 (1565) 2
8576912 10.1021/jm950645n L1210 2
7699716 10.1021/jm00006a019 Thymidylate synthase 1
8576912 10.1021/jm950645n Thymidylate synthase 1
8576912 10.1021/jm950645n Unchecked 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine