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Assay Detail

CHEMBL5733422

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

Binding
Inhibition Assay: The in vitro activity of the compounds described herein in inhibiting TAK1, HCK, and other kinases were obtained using an Invitrogen Select Screening assay as known in the art.
24
Total Activities
8
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methods to treat lymphoplasmacytic lymphoma
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.53 7.64
kon 8 - -
k_off 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5950918 3 7.64
CHEMBL5915826 3 7.60
CHEMBL5827081 3 7.16
CHEMBL5834925 3 6.71
CHEMBL6044253 3 6.34
CHEMBL6014241 3 5.94
CHEMBL5778860 3 5.47
CHEMBL5994443 3 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5950918 IC50 = 22.9 nM 7.64
CHEMBL5915826 IC50 = 25.3 nM 7.60
CHEMBL5827081 IC50 = 69.7 nM 7.16
CHEMBL5834925 IC50 = 196.0 nM 6.71
CHEMBL6044253 IC50 = 459.0 nM 6.34
CHEMBL6014241 IC50 = 1150.0 nM 5.94
CHEMBL5778860 IC50 = 3420.0 nM 5.47
CHEMBL5994443 IC50 = 3910.0 nM 5.41
CHEMBL5950918 kon = - -
CHEMBL5950918 k_off = - s-1 -
CHEMBL5834925 kon = - -
CHEMBL5834925 k_off = - s-1 -
CHEMBL6044253 kon = - -
CHEMBL6044253 k_off = - s-1 -
CHEMBL5994443 kon = - -
CHEMBL5994443 k_off = - s-1 -
CHEMBL6014241 kon = - -
CHEMBL6014241 k_off = - s-1 -
CHEMBL5778860 kon = - -
CHEMBL5778860 k_off = - s-1 -
CHEMBL5827081 kon = - -
CHEMBL5827081 k_off = - s-1 -
CHEMBL5915826 kon = - -
CHEMBL5915826 k_off = - s-1 -