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Assay Detail

CHEMBL4350852

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

Functional
Antitrypanosomal activity against Trypanosoma brucei Squib 427 trypomastigotes assessed as reduction in parasite growth incubated for 72 hrs by resazurin dye-based fluorimetric analysis
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).
de Heuvel E, Singh AK, Boronat P, Kooistra AJ, van der Meer T, Sadek P, Blaazer AR, Shaner NC, Bindels DS, Caljon G, Maes L, Sterk GJ, Siderius M, Oberholzer M, de Esch IJP, Brown DG, Leurs R.
Bioorg Med Chem (2019) 27 : 4013 -4029
PubMed 31378593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.58 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265502 SURAMIN 3.0 1 7.40
CHEMBL4436770 1 6.20
CHEMBL4465919 1 6.00
CHEMBL4454951 1 6.00
CHEMBL4521383 1 6.00
CHEMBL4445930 1 5.90
CHEMBL4453045 1 5.80
CHEMBL4439778 1 5.80
CHEMBL4443772 1 5.70
CHEMBL4520014 1 5.70
CHEMBL4445489 1 5.70
CHEMBL4566533 1 5.70
CHEMBL4444414 1 5.60
CHEMBL4439798 1 5.60
CHEMBL4439032 1 5.50
CHEMBL4516631 1 5.30
CHEMBL4463356 1 5.20
CHEMBL4473629 1 5.20
CHEMBL4435831 1 5.10
CHEMBL4583339 1 5.10
CHEMBL4453613 1 5.10
CHEMBL4565967 1 5.10
CHEMBL4522881 1 5.10
CHEMBL4472788 1 5.00
CHEMBL4562476 1 4.60
CHEMBL4471782 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265502 SURAMIN IC50 = 39.81 nM 7.40
CHEMBL4436770 IC50 = 630.96 nM 6.20
CHEMBL4465919 IC50 = 1000.0 nM 6.00
CHEMBL4454951 IC50 = 1000.0 nM 6.00
CHEMBL4521383 IC50 = 1000.0 nM 6.00
CHEMBL4445930 IC50 = 1258.93 nM 5.90
CHEMBL4453045 IC50 = 1584.89 nM 5.80
CHEMBL4439778 IC50 = 1584.89 nM 5.80
CHEMBL4443772 IC50 = 1995.26 nM 5.70
CHEMBL4520014 IC50 = 1995.26 nM 5.70
CHEMBL4445489 IC50 = 1995.26 nM 5.70
CHEMBL4566533 IC50 = 1995.26 nM 5.70
CHEMBL4444414 IC50 = 2511.89 nM 5.60
CHEMBL4439798 IC50 = 2511.89 nM 5.60
CHEMBL4439032 IC50 = 3162.28 nM 5.50
CHEMBL4516631 IC50 = 5011.87 nM 5.30
CHEMBL4463356 IC50 = 6309.57 nM 5.20
CHEMBL4473629 IC50 = 6309.57 nM 5.20
CHEMBL4435831 IC50 = 7943.28 nM 5.10
CHEMBL4583339 IC50 = 7943.28 nM 5.10
CHEMBL4453613 IC50 = 7943.28 nM 5.10
CHEMBL4565967 IC50 = 7943.28 nM 5.10
CHEMBL4522881 IC50 = 7943.28 nM 5.10
CHEMBL4472788 IC50 = 10000.0 nM 5.00
CHEMBL4562476 IC50 = 25118.86 nM 4.60
CHEMBL4471782 IC50 > 63095.73 nM -