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Assay Detail

CHEMBL2406867

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

Binding
Inhibition of Trypanosoma brucei recombinant rhodesain
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.
Ettari R, Tamborini L, Angelo IC, Micale N, Pinto A, De Micheli C, Conti P.
J Med Chem (2013) 56 : 5637 -5658
PubMed 23611656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 9.08 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2402112 1 10.22
CHEMBL594719 1 10.22
CHEMBL2402192 1 10.22
CHEMBL2402193 1 9.85
CHEMBL2402188 1 9.85
CHEMBL604078 1 9.72
CHEMBL2402196 1 9.62
CHEMBL2401743 1 9.48
CHEMBL2402189 1 9.48
CHEMBL91704 K-777 2.0 1 9.46
CHEMBL327624 1 9.44
CHEMBL604281 1 9.40
CHEMBL2402194 1 9.29
CHEMBL2402113 1 9.15
CHEMBL604079 1 9.09
CHEMBL2402197 1 8.87
CHEMBL2402195 1 8.73
CHEMBL2402190 1 8.70
CHEMBL2402198 1 8.27
CHEMBL2402199 1 7.80
CHEMBL2402200 1 7.46
CHEMBL2402201 1 7.27
CHEMBL2402111 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2402112 IC50 = 0.06 nM 10.22
CHEMBL594719 IC50 = 0.06 nM 10.22
CHEMBL2402192 IC50 = 0.06 nM 10.22
CHEMBL2402193 IC50 = 0.14 nM 9.85
CHEMBL2402188 IC50 = 0.14 nM 9.85
CHEMBL604078 IC50 = 0.19 nM 9.72
CHEMBL2402196 IC50 = 0.24 nM 9.62
CHEMBL2401743 IC50 = 0.33 nM 9.48
CHEMBL2402189 IC50 = 0.33 nM 9.48
CHEMBL91704 K-777 IC50 = 0.35 nM 9.46
CHEMBL327624 IC50 = 0.36 nM 9.44
CHEMBL604281 IC50 = 0.4 nM 9.40
CHEMBL2402194 IC50 = 0.51 nM 9.29
CHEMBL2402113 IC50 = 0.71 nM 9.15
CHEMBL604079 IC50 = 0.81 nM 9.09
CHEMBL2402197 IC50 = 1.34 nM 8.87
CHEMBL2402195 IC50 = 1.86 nM 8.73
CHEMBL2402190 IC50 = 2.0 nM 8.70
CHEMBL2402198 IC50 = 5.4 nM 8.27
CHEMBL2402199 IC50 = 15.8 nM 7.80
CHEMBL2402200 IC50 = 35.1 nM 7.46
CHEMBL2402201 IC50 = 54.0 nM 7.27
CHEMBL2402111 IC50 = 54.6 nM 7.26