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Assay Detail

CHEMBL877966

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory concentration against isolated Lactobacillus casei Thymidylate synthase
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Lacticaseibacillus casei
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Thymidylate synthase (CHEMBL5328)
Type SINGLE PROTEIN
Organism Lactobacillus casei

Publication

Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.
Gangjee A, Yu J, McGuire JJ, Cody V, Galitsky N, Kisliuk RL, Queener SF.
J Med Chem (2000) 43 : 3837 -3851
PubMed 11052789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.72 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL389051 1 7.26
CHEMBL124256 1 6.51
CHEMBL225071 RALTITREXED 4.0 1 5.10
CHEMBL439973 1 5.05
CHEMBL225072 PEMETREXED 4.0 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL389051 IC50 = 55.0 nM 7.26
CHEMBL124256 IC50 = 310.0 nM 6.51
CHEMBL225071 RALTITREXED IC50 = 8000.0 nM 5.10
CHEMBL439973 IC50 = 9000.0 nM 5.05
CHEMBL225072 PEMETREXED IC50 = 20000.0 nM 4.70