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Assay Detail

CHEMBL5050277

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

Functional
Antitrypanosomal activity against bloodstream Trypanosoma congolense IL3000 assessed as parasite growth inhibition incubated for 69 hrs by resazurin dye based fluorescence analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma congolense
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma congolense (CHEMBL4296607)
Type ORGANISM
Organism Trypanosoma congolense

Publication

Repositioning of a Diaminothiazole Series Confirmed to Target the Cyclin-Dependent Kinase CRK12 for Use in the Treatment of African Animal Trypanosomiasis.
Smith A, Wall RJ, Patterson S, Rowan T, Rico Vidal E, Stojanovski L, Huggett M, Hampton SE, Thomas MG, Corpas Lopez V, Gillingwater K, Duke J, Napier G, Peter R, Vitouley HS, Harrison JR, Milne R, Jeacock L, Baker N, Davis SH, Simeons F, Riley J, Horn D, Brun R, Zuccotto F, Witty MJ, Wyllie S, Read KD, Gilbert IH.
J Med Chem (2022) 65 : 5606 -5624
PubMed 35303411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.53 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5088920 1 9.40
CHEMBL5076865 1 9.23
CHEMBL5094897 1 8.89
CHEMBL5084963 1 8.60
CHEMBL5074906 1 8.49
CHEMBL5084432 1 8.08
CHEMBL5072657 1 7.80
CHEMBL5089071 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5088920 EC50 = 0.4 nM 9.40
CHEMBL5076865 EC50 = 0.59 nM 9.23
CHEMBL5094897 EC50 = 1.3 nM 8.89
CHEMBL5084963 EC50 = 2.5 nM 8.60
CHEMBL5074906 EC50 = 3.2 nM 8.49
CHEMBL5084432 EC50 = 8.3 nM 8.08
CHEMBL5072657 EC50 = 16.0 nM 7.80
CHEMBL5089071 EC50 = 18.0 nM 7.75