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Assay Detail

CHEMBL2045551

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

Binding
Inhibition of Trypanosoma brucei brucei LAPT1 assessed as [3H]-pentamidine uptake after 120 secs by scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
Taladriz A, Healy A, Flores Pérez EJ, Herrero García V, Ríos Martínez C, Alkhaldi AA, Eze AA, Kaiser M, de Koning HP, Chana A, Dardonville C.
J Med Chem (2012) 55 : 2606 -2622
PubMed 22390399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 4.80 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539632 1 5.66
CHEMBL2041828 1 5.44
CHEMBL2041805 1 5.14
CHEMBL2041806 1 5.02
CHEMBL2041796 1 4.72
CHEMBL2041795 1 4.70
CHEMBL2041807 1 4.60
CHEMBL2041841 1 4.60
CHEMBL601708 1 4.41
CHEMBL601066 1 4.31
CHEMBL55 PENTAMIDINE 4.0 1 4.25
CHEMBL596746 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539632 Ki = 2200.0 nM 5.66
CHEMBL2041828 Ki = 3600.0 nM 5.44
CHEMBL2041805 Ki = 7200.0 nM 5.14
CHEMBL2041806 Ki = 9500.0 nM 5.02
CHEMBL2041796 Ki = 19000.0 nM 4.72
CHEMBL2041795 Ki = 20000.0 nM 4.70
CHEMBL2041807 Ki = 25000.0 nM 4.60
CHEMBL2041841 Ki = 25000.0 nM 4.60
CHEMBL601708 Ki = 39000.0 nM 4.41
CHEMBL601066 Ki = 49000.0 nM 4.31
CHEMBL55 PENTAMIDINE Ki = 56200.0 nM 4.25
CHEMBL596746 Ki > 250000.0 nM -