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Assay Detail

CHEMBL3789111

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

Binding
Competitive inhibition of human RIP1 (1 to 375 residues) in presence of increasing ATP by ADP-Glo reagent based assay
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 1 (CHEMBL5464)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 1 9.10 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3785703 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3785703 Ki = 0.8 nM 9.10