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Assay Detail

CHEMBL4024002

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

Binding
Inhibition of fluorescent-labeled 3-(3-((3-(4-amino-5-(4-(3-(2-fluoro-5-(trifluoromethyl)phenyl)ureido)-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)propyl)amino)-3-oxopropyl)-5,5-difluoro-7,9-dimethyl-5H-dipyrrolo[1,2-c:2',1'-f]-[1,3,2]diazaborinin-4-ium-5-uide binding to mouse RIPK1 by TR-FRET assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of 7-Oxo-2,4,5,7-tetrahydro-6 H-pyrazolo[3,4- c]pyridine Derivatives as Potent, Orally Available, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure-Kinetic Relationships.
Yoshikawa M, Saitoh M, Katoh T, Seki T, Bigi SV, Shimizu Y, Ishii T, Okai T, Kuno M, Hattori H, Watanabe E, Saikatendu KS, Zou H, Nakakariya M, Tatamiya T, Nakada Y, Yogo T.
J Med Chem (2018) 61 : 2384 -2409
PubMed 29485864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.09 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100398 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100398 Ki = 81.28 nM 7.09