Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5736379

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

Binding
In Vitro Direct Determination By Fluorescence: Table 6 & 7: Fresh solutions of each test compound (2.5 mM in DMSO) are diluted in PBS pH=7.4 at concentrations between 0.5 nM and 5 μM in the presence or absence of α-syn (200 nM), Aβ1-42 (500 nM) or Tau (200 nM) fibers in a final 2 mL volume. After 1 h of incubation at RT, the binding of each compound to α-syn, A131-42 or Tau fibers is measured by fluorescence using the spectral changes of the compounds during their binding to the fibers, using the appropriate excitation/emission wavelengths (those giving the highest fluorescence variation during binding to the fibres). For each concentration of compound added to the fibres, the bound and free fractions are measured by fluorescence according to the following equation:F m =F B B+F F×(T−B).
24
Total Activities
8
Compounds Tested
3
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

Compounds for using in imaging and particularly for the diagnosis of neurodegenerative diseases
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 8.77 9.89
kon 8 - -
k_off 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6001659 3 9.89
CHEMBL5771524 3 9.36
CHEMBL6035240 3 9.31
CHEMBL6034599 3 9.01
CHEMBL5896450 3 8.78
CHEMBL5843281 3 8.62
CHEMBL1908919 FLORBETAPIR 4.0 3 7.71
CHEMBL207649 3 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6001659 Kd = 0.13 nM 9.89
CHEMBL5771524 Kd = 0.44 nM 9.36
CHEMBL6035240 Kd = 0.49 nM 9.31
CHEMBL6034599 Kd = 0.97 nM 9.01
CHEMBL5896450 Kd = 1.67 nM 8.78
CHEMBL5843281 Kd = 2.4 nM 8.62
CHEMBL1908919 FLORBETAPIR Kd = 19.6 nM 7.71
CHEMBL207649 Kd = 34.9 nM 7.46
CHEMBL1908919 FLORBETAPIR kon = - -
CHEMBL1908919 FLORBETAPIR k_off = - s-1 -
CHEMBL207649 kon = - -
CHEMBL207649 k_off = - s-1 -
CHEMBL5771524 kon = - -
CHEMBL5771524 k_off = - s-1 -
CHEMBL6035240 kon = - -
CHEMBL6035240 k_off = - s-1 -
CHEMBL6001659 kon = - -
CHEMBL6001659 k_off = - s-1 -
CHEMBL5843281 kon = - -
CHEMBL5843281 k_off = - s-1 -
CHEMBL5896450 kon = - -
CHEMBL5896450 k_off = - s-1 -
CHEMBL6034599 kon = - -
CHEMBL6034599 k_off = - s-1 -