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Assay Detail

CHEMBL664356

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

Binding
Inhibitory activity against Trypanosoma cruzi dihydrofolate reductase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma cruzi
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.
Zuccotto F, Brun R, Gonzalez Pacanowska D, Ruiz Perez LM, Gilbert IH.
Bioorg Med Chem Lett (1999) 9 : 1463 -1468
PubMed 10360757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.92 10.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 10.42
CHEMBL35364 1 9.97
CHEMBL284943 1 9.88
CHEMBL35427 1 9.74
CHEMBL285474 1 7.85
CHEMBL35552 1 7.33
CHEMBL265757 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE Ki = 0.038 nM 10.42
CHEMBL35364 Ki = 0.107 nM 9.97
CHEMBL284943 Ki = 0.131 nM 9.88
CHEMBL35427 Ki = 0.183 nM 9.74
CHEMBL285474 Ki = 14.1 nM 7.85
CHEMBL35552 Ki = 46.2 nM 7.33
CHEMBL265757 Ki = 55.7 nM 7.25