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Assay Detail

CHEMBL4135614

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

Binding
Inhibition of RIPK2 in C57BL/6 mouse BMDM assessed as reduction in MDP/LPS-stimulated IL6 secretion pretreated for 30 mins followed by MDP/LPS stimulation after 18 hrs
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BMDM
Confidence 9 — Direct single protein target
Curated By Intermediate

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
Inhibition 2 - -
IC50 2 8.07 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173493 2 8.22
CHEMBL4161327 2 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173493 IC50 = 6.0 nM 8.22
CHEMBL4161327 IC50 = 12.0 nM 7.92
CHEMBL4173493 Inhibition - % -
CHEMBL4161327 Inhibition - % -