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Assay Detail

CHEMBL5626795

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

Binding
Inhibition of human recombinant RIPK1 using MBP as substrate preincubated for 15 mins followed by substrate addition and measured after 120 mins in presence of ATP by ADP-Glo kinase assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Receptor-interacting serine/threonine-protein kinase 1 (CHEMBL5464)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Pyrido[3,4-d]pyrimidine derivatives as RIPK3-Mediated necroptosis inhibitors.
Kim N, Park CJ, Kim Y, Ryu S, Cho H, Nam Y, Han M, Shin JS, Sim T.
Eur J Med Chem (2023) 259 : 115635 -115635
PubMed 37494773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.93 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195008 NECROSTATIN 1 6.57
CHEMBL5632937 1 6.16
CHEMBL4779280 1 6.03
CHEMBL5632140 1 5.78
CHEMBL5629959 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195008 NECROSTATIN IC50 = 268.0 nM 6.57
CHEMBL5632937 IC50 = 700.0 nM 6.16
CHEMBL4779280 IC50 = 929.0 nM 6.03
CHEMBL5632140 IC50 = 1665.0 nM 5.78
CHEMBL5629959 IC50 = 8210.0 nM 5.09