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Assay Detail

CHEMBL4352202

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

Binding
Inhibition of RIP1 in mouse L929 cells assessed as reduction in TNF/zVAD.fmk-induced necrotic death measured after 24 hrs by cell titer-glo luminescent cell viability 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

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW.
J Med Chem (2019) 62 : 5096 -5110
PubMed 31013427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.06 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4545939 1 8.49
CHEMBL4514271 1 7.50
CHEMBL4474320 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4545939 IC50 = 3.2 nM 8.49
CHEMBL4514271 IC50 = 32.0 nM 7.50
CHEMBL4474320 IC50 = 6300.0 nM 5.20