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Assay Detail

CHEMBL5737469

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

Binding
ASK1/2 Biochemical Assays (IMAP Technology): IMAP technology provides a homogeneous assay applicable to a wide variety of kinases, phosphatases, and phosphodiesterases without regard for substrate peptide sequence. The assay is a simple mix-and-read procedure allowing accurate determination of enzyme activity. Based on the specific, high-affinity interaction of phospho groups with trivalent metal-containing nanoparticles (beads), IMAP is a generic, non-antibody-based platform to assess kinase, phosphatase, and phosphodiesterase activity. An enzyme reaction is performed using fluorescently labeled substrate. Addition of the IMAP Binding System stops the enzyme reaction and initiates binding of the beads to phosphorylated substrates. Binding of the substrate to the beads, which correlates to enzyme activity, can be detected using either FP or TR-FRET as a readout.
21
Total Activities
7
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase kinase kinase 5 (CHEMBL5285)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrrolopyrimidine and pyrrolopyridine derivatives
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.37 8.98
kon 7 - -
k_off 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5843273 3 8.98
CHEMBL5746514 3 8.46
CHEMBL5770629 3 8.43
CHEMBL6036447 3 8.24
CHEMBL5776905 3 8.24
CHEMBL5937217 3 8.17
CHEMBL5812512 3 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5843273 IC50 = 1.05 nM 8.98
CHEMBL5746514 IC50 = 3.47 nM 8.46
CHEMBL5770629 IC50 = 3.72 nM 8.43
CHEMBL5776905 IC50 = 5.75 nM 8.24
CHEMBL6036447 IC50 = 5.75 nM 8.24
CHEMBL5937217 IC50 = 6.76 nM 8.17
CHEMBL5812512 IC50 = 8.91 nM 8.05
CHEMBL6036447 kon = - -
CHEMBL6036447 k_off = - s-1 -
CHEMBL5937217 kon = - -
CHEMBL5937217 k_off = - s-1 -
CHEMBL5812512 kon = - -
CHEMBL5812512 k_off = - s-1 -
CHEMBL5746514 k_off = - s-1 -
CHEMBL5770629 kon = - -
CHEMBL5770629 k_off = - s-1 -
CHEMBL5843273 kon = - -
CHEMBL5843273 k_off = - s-1 -
CHEMBL5776905 kon = - -
CHEMBL5776905 k_off = - s-1 -
CHEMBL5746514 kon = - -