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Compound Detail

CHEMBL157025

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C#CCN(Cc1cc2c(O)nc(C)nc2cc1C)c1ccc(C(=O)N[C@@H](CCC(=O)N[C@@H](C)c2nnn[nH]2)C(=O)O)c(F)c1

Basic Information

ChEMBL ID CHEMBL157025
Phase Preclinical
Structure Type MOL
InChI Key XPWJYJITPLJYMI-HJPURHCSSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

603.6
MW (Da)
2.08
ALogP
10
HBA
5
HBD
199.2
PSA (Ų)
0.15
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 C29H30FN9O5
MW 603.62
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -1.55

Activity Summary

IC50 5 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL3160
IC50 9.0 9.0 1.0 1
L1210
CHEMBL386
IC50 6.58 6.2467 260.0 3
L1210 (1565)
CHEMBL614000
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00078-9 L1210 3
- 10.1016/0960-894X(96)00078-9 Thymidylate synthase 1
- 10.1016/0960-894X(96)00078-9 L1210 (1565) 1

Data from ChEMBL 36 via Core Engine