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Compound Detail

CHEMBL102469

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O=C(O)CC[C@H](NC(=O)c1ccc(N(CCF)Cc2ccc3nc(CF)[nH]c(=O)c3c2)cc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL102469
Phase Preclinical
Structure Type MOL
InChI Key XRNHFJOBXRIIHD-IBGZPJMESA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

502.5
MW (Da)
2.42
ALogP
6
HBA
4
HBD
152.7
PSA (Ų)
0.29
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24F2N4O6
MW 502.47
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.90

Activity Summary

IC50 3 meas. best 6.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL1952
IC50 6.47 6.47 338.8 1
Thymidylate synthase
CHEMBL3160
IC50 6.47 6.47 340.0 1
L1210
CHEMBL386
IC50 5.92 5.92 1200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2231606 10.1021/jm00173a024 Thymidylate synthase 1
2231606 10.1021/jm00173a024 L1210 1
20153089 10.1016/j.ejmech.2009.12.065 Thymidylate synthase 1

Data from ChEMBL 36 via Core Engine