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Assay Detail

CHEMBL3364301

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Binding
Inhibition of thymidylate synthase activity of Cryptosporidium hominis bifunctional dihydrofolate reductase-thymidylate synthase assessed as reduction in conversion of dUMP and CH2H4F to products dTMP and H2F
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cryptosporidium hominis
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL2366489)
Type SINGLE PROTEIN
Organism Cryptosporidium parvum

Publication

Structural studies provide clues for analog design of specific inhibitors of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase.
Kumar VP, Cisneros JA, Frey KM, Castellanos-Gonzalez A, Wang Y, Gangjee A, White AC, Jorgensen WL, Anderson KS.
Bioorg Med Chem Lett (2014) 24 : 4158 -4161
PubMed 25127103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.42 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2426247 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2426247 IC50 = 380.0 nM 6.42