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Compound Detail

CHEMBL352357

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C#CCN(Cc1ccc2nc(C)nc(O)c2c1)c1ccc(C(=O)N[C@@H](CCC(=O)NC(Cc2ccccc2)C(=O)O)C(=O)O)cc1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL352357
Phase Preclinical
Structure Type MOL
InChI Key UJKLTVIUCLCNKQ-MKSHZDIXSA-N
Parent Compound CHEMBL1184495
Active Moiety CHEMBL1184495
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

623.7
MW (Da)
3.06
ALogP
8
HBA
5
HBD
182.1
PSA (Ų)
0.13
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H34F3N5O9
MW 737.69
Aromatic Rings 4
Heavy Atoms 46
NP-Likeness -0.84

Activity Summary

IC50 2 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL3160
IC50 7.52 7.52 30.0 1
L1210
CHEMBL386
IC50 5.68 5.68 2100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thymidylate synthase IC50 = 30.0 nM 7.52 Inhibition of Thymidylate synthase activity in L1210 cells 8568829
L1210 IC50 = 2100.0 nM 5.68 Inhibition of L1210 cell growth 8568829

Literature References

PubMed DOI Target Context # Activities
8568829 10.1021/jm950471+ Thymidylate synthase 1
8568829 10.1021/jm950471+ L1210 1
8568829 10.1021/jm950471+ L1210 (1565) 1

Data from ChEMBL 36 via Core Engine