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Assay Detail

CHEMBL815219

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

Functional
Inhibition of Trypanosoma brucei rhodesiense growth
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei
Confidence 1 — Organism
Curated By Expert

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.
Chowdhury SF, Villamor VB, Guerrero RH, Leal I, Brun R, Croft SL, Goodman JM, Maes L, Ruiz-Perez LM, Pacanowska DG, Gilbert IH.
J Med Chem (1999) 42 : 4300 -4312
PubMed 10543874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.25 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL137641 1 6.00
CHEMBL138230 1 6.00
CHEMBL334695 1 6.00
CHEMBL31547 1 5.70
CHEMBL31235 1 5.70
CHEMBL137305 1 5.40
CHEMBL31946 1 5.30
CHEMBL274031 1 5.30
CHEMBL285209 1 5.30
CHEMBL36 PYRIMETHAMINE 4.0 1 5.16
CHEMBL326989 1 5.00
CHEMBL343127 1 4.89
CHEMBL334919 1 4.85
CHEMBL137448 1 4.68
CHEMBL343271 1 4.62
CHEMBL30734 1 4.11
CHEMBL22 TRIMETHOPRIM 4.0 1 -
CHEMBL18967 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL137641 IC50 = 1000.0 nM 6.00
CHEMBL138230 IC50 = 1000.0 nM 6.00
CHEMBL334695 IC50 = 1000.0 nM 6.00
CHEMBL31547 IC50 = 2000.0 nM 5.70
CHEMBL31235 IC50 = 2000.0 nM 5.70
CHEMBL137305 IC50 = 4000.0 nM 5.40
CHEMBL31946 IC50 = 5000.0 nM 5.30
CHEMBL274031 IC50 = 5000.0 nM 5.30
CHEMBL285209 IC50 = 5000.0 nM 5.30
CHEMBL36 PYRIMETHAMINE IC50 = 7000.0 nM 5.16
CHEMBL326989 IC50 = 10000.0 nM 5.00
CHEMBL343127 IC50 = 13000.0 nM 4.89
CHEMBL334919 IC50 = 14000.0 nM 4.85
CHEMBL137448 IC50 = 21000.0 nM 4.68
CHEMBL343271 IC50 = 24000.0 nM 4.62
CHEMBL30734 IC50 = 78000.0 nM 4.11
CHEMBL22 TRIMETHOPRIM IC50 = 148000.0 nM -
CHEMBL18967 IC50 = 204000.0 nM -