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Assay Detail

CHEMBL3789353

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

Binding
Inhibition of mouse RIP1 in mouse L929 cells assessed as inhibition of TNF/zVAD.fmk induced necroptosis by Cell titer-Glo luminescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type L929
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ.
J Med Chem (2016) 59 : 2163 -2178
PubMed 26854747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.80 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3109202 1 6.40
CHEMBL3785703 1 5.50
CHEMBL3786078 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3109202 IC50 = 400.0 nM 6.40
CHEMBL3785703 IC50 = 3200.0 nM 5.50
CHEMBL3786078 IC50 = 3200.0 nM 5.50