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Assay Detail

CHEMBL4431994

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

Binding
Inhibition of Trypanosoma brucei PTR1 using H2B as substrate incubated for 10 mins followed by addition of NADPH measured for 10 to 50 mins
7
Total Activities
7
Compounds Tested
2
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

Profiling of Flavonol Derivatives for the Development of Antitrypanosomatidic Drugs.
Borsari C, Luciani R, Pozzi C, Poehner I, Henrich S, Trande M, Cordeiro-da-Silva A, Santarem N, Baptista C, Tait A, Di Pisa F, Dello Iacono L, Landi G, Gul S, Wolf M, Kuzikov M, Ellinger B, Reinshagen J, Witt G, Gribbon P, Kohler M, Keminer O, Behrens B, Costantino L, Tejera Nevado P, Bifeld E, Eick J, Clos J, Torrado J, Jiménez-Antón MD, Corral MJ, Alunda JM, Pellati F, Wade RC, Ferrari S, Mangani S, Costi MP.
J Med Chem (2016) 59 : 7598 -7616
PubMed 27411733 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.76 5.37
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464764 1 5.37
CHEMBL294009 FLAVONOL 1 4.89
CHEMBL379064 ISORHAMNETIN 1 4.86
CHEMBL150 KAEMPFEROL 1.0 1 4.55
CHEMBL503168 DATISCETIN 1 4.11
CHEMBL1520590 1 -
CHEMBL1883743 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464764 IC50 = 4300.0 nM 5.37
CHEMBL294009 FLAVONOL IC50 = 12800.0 nM 4.89
CHEMBL379064 ISORHAMNETIN IC50 = 13900.0 nM 4.86
CHEMBL150 KAEMPFEROL IC50 = 28000.0 nM 4.55
CHEMBL503168 DATISCETIN IC50 = 76900.0 nM 4.11
CHEMBL1520590 Inhibition - % -
CHEMBL1883743 Inhibition - % -