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Assay Detail

CHEMBL3889073

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

Binding
Competitive Binding Assay: For tau imaging probes other than THK-5105, binding to K18-ΔK280 aggregates was evaluated with a competitive binding test using [18F] THK-5105 as a radioactive competitor. In the binding test, [18F] THK-5105 (at a final concentration of 1.76 nM) and a tested compound (at final concentrations of from 0.1 to 1000 nM) coexisted in the reaction system, to which K18-ΔK280 aggregates (at a final concentration of 200 nM) was then added and the mixtures were incubated at room temperature for one hour. The radioactivity of [18F] THK-5105 binding to the aggregates was determined in a similar way as in the saturation binding test of THK-5105. The percentage of [18F] THK-5105 bonding in the absence of each tested compound was set to be 100%, and percentages of [18F] THK-5105 bonding at various concentrations of each of the tested compounds were determined.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Microtubule-associated protein tau (CHEMBL1293224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tau imaging probe
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.48 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3893272 1 8.04
CHEMBL3985550 1 7.98
CHEMBL3973145 1 7.67
CHEMBL3939385 1 7.46
CHEMBL3953540 1 7.44
CHEMBL3947029 1 7.40
CHEMBL2219511 1 7.23
CHEMBL207649 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3893272 Ki = 9.2 nM 8.04
CHEMBL3985550 Ki = 10.5 nM 7.98
CHEMBL3973145 Ki = 21.4 nM 7.67
CHEMBL3939385 Ki = 34.9 nM 7.46
CHEMBL3953540 Ki = 36.0 nM 7.44
CHEMBL3947029 Ki = 40.1 nM 7.40
CHEMBL2219511 Ki = 59.3 nM 7.23
CHEMBL207649 Ki = 256.0 nM 6.59