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Assay Detail

CHEMBL4135616

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

Binding
Inhibition of RIPK2 in human whole blood assessed as reduction in MDP-stimulated TNFalpha secretion pretreated for 30 mins followed by MDP stimulation measured after 20 hrs
1
Total Activities
1
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 2 (CHEMBL5014)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.
He X, Da Ros S, Nelson J, Zhu X, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S, Jia Y, Bursulaya B, Kreusch A, Gao MY, Spraggon G, Baaten J, Clemmer L, Meeusen S, Huang D, Hill R, Nguyen-Tran V, Fathman J, Liu B, Tuntland T, Gordon P, Hollenbeck T, Ng K, Shi J, Bordone L, Liu H.
ACS Med Chem Lett (2017) 8 : 1048 -1053
PubMed 29057049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.52 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161327 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161327 IC50 = 30.0 nM 7.52