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Assay Detail

CHEMBL4306770

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

Binding
Inhibition of RIP1 in human whole blood assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated MIP-1 beta cytokine overproduction incubated for 6 hrs by sandwich ELISA
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
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

Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
Harris PA, Marinis JM, Lich JD, Berger SB, Chirala A, Cox JA, Eidam PM, Finger JN, Gough PJ, Jeong JU, Kang J, Kasparcova V, Leister LK, Mahajan MK, Miller G, Nagilla R, Ouellette MT, Reilly MA, Rendina AR, Rivera EJ, Sun HH, Thorpe JH, Totoritis RD, Wang W, Wu D, Zhang D, Bertin J, Marquis RW.
ACS Med Chem Lett (2019) 10 : 857 -862
PubMed 31223438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4452233 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4452233 IC50 = 5.0 nM 8.30