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Assay Detail

CHEMBL4434086

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

Binding
Inhibition of human 6His-TEV-TNIK(1 to 325) expressed in baculovirus-infected sf21 cells using LRRKtide as substrate preincubated for 30 mins followed by substrate addition and measured after 75 to 90 mins by ADP-Glo Reagent based method
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

TRAF2 and NCK-interacting protein kinase (CHEMBL4527)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase.
Read J, Collie IT, Nguyen-McCarty M, Lucaj C, Robinson J, Conway L, Mukherjee J, McCall E, Donohoe G, Flavell E, Peciak K, Warwicker J, Dix C, Van den Hoven BG, Madin A, Brown DG, Moss S, Haggarty SJ, Brandon NJ, Bürli RW.
Bioorg Med Chem Lett (2019) 29 : 1962 -1967
PubMed 31153805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.48 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3754283 1 8.00
CHEMBL4471729 1 7.90
CHEMBL4558962 1 7.10
CHEMBL4527085 1 6.90
CHEMBL3262590 2 6.82
CHEMBL4451091 1 5.40
CHEMBL4558988 1 4.80
CHEMBL4465524 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3754283 IC50 = 10.0 nM 8.00
CHEMBL4471729 IC50 = 12.59 nM 7.90
CHEMBL4558962 IC50 = 79.43 nM 7.10
CHEMBL4527085 IC50 = 125.89 nM 6.90
CHEMBL3262590 IC50 = 150.0 nM 6.82
CHEMBL3262590 IC50 = 158.49 nM 6.80
CHEMBL4451091 IC50 = 3981.07 nM 5.40
CHEMBL4558988 IC50 = 15848.93 nM 4.80
CHEMBL4465524 IC50 = 25118.86 nM 4.60