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Assay Detail

CHEMBL2406859

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

Binding
Inhibition of Trypanosoma brucei rhodesiense rhodesain
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei rhodesiense
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Rhodesain (CHEMBL4188)
Type SINGLE PROTEIN
Organism Trypanosoma brucei rhodesiense

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
Ki 7 7.84 8.70
IC50 6 6.69 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2402090 1 8.70
CHEMBL2402091 1 8.10
CHEMBL2402094 1 7.96
CHEMBL2402095 1 7.44
CHEMBL181752 1 7.42
CHEMBL181504 1 7.22
CHEMBL183767 1 7.10
CHEMBL2402096 1 7.00
CHEMBL92099 1 6.96
CHEMBL181902 1 5.96
CHEMBL367811 1 5.48
CHEMBL2402093 1 -
CHEMBL2402092 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2402090 Ki = 2.0 nM 8.70
CHEMBL2402091 Ki = 8.0 nM 8.10
CHEMBL2402094 Ki = 11.0 nM 7.96
CHEMBL2402095 Ki = 36.0 nM 7.44
CHEMBL181752 IC50 = 38.0 nM 7.42
CHEMBL181504 IC50 = 60.0 nM 7.22
CHEMBL183767 IC50 = 80.0 nM 7.10
CHEMBL2402096 Ki = 100.0 nM 7.00
CHEMBL92099 IC50 = 110.0 nM 6.96
CHEMBL181902 IC50 = 1100.0 nM 5.96
CHEMBL367811 IC50 = 3330.0 nM 5.48
CHEMBL2402093 Ki - -
CHEMBL2402092 Ki - -