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Assay Detail

CHEMBL4838014

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

Functional
Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei AQP1-3 KO trypomastigotes incubated for 48 hrs by resazurin dye based fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Synthesis, biological, and photophysical studies of molecular rotor-based fluorescent inhibitors of the trypanosome alternative oxidase.
Cueto-Díaz EJ, Ebiloma GU, Alfayez IA, Ungogo MA, Lemgruber L, González-García MC, Giron MD, Salto R, Fueyo-González FJ, Shiba T, González-Vera JA, Ruedas Rama MJ, Orte A, de Koning HP, Dardonville C.
Eur J Med Chem (2021) 220 : 113470 -113470
PubMed 33940464 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.13 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 7.47
CHEMBL4878802 1 6.72
CHEMBL4873996 1 6.47
CHEMBL4857072 1 6.37
CHEMBL4872515 1 6.36
CHEMBL4879019 1 6.18
CHEMBL4846979 1 5.98
CHEMBL4857860 1 4.88
CHEMBL4846671 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE EC50 = 34.0 nM 7.47
CHEMBL4878802 EC50 = 190.0 nM 6.72
CHEMBL4873996 EC50 = 340.0 nM 6.47
CHEMBL4857072 EC50 = 430.0 nM 6.37
CHEMBL4872515 EC50 = 440.0 nM 6.36
CHEMBL4879019 EC50 = 663.0 nM 6.18
CHEMBL4846979 EC50 = 1048.0 nM 5.98
CHEMBL4857860 EC50 = 13100.0 nM 4.88
CHEMBL4846671 EC50 = 16600.0 nM 4.78