Assay Detail

CHEMBL4352240

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Binding

Inhibition of RIP1 in human whole blood assessed as reduction in TNFalpha/zVAD-fmk/SMAC-induced MIP1alpha production measured after 6 hrs by ELISA

ChEMBL ↗

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Target

Receptor-interacting serine/threonine-protein kinase 1 (CHEMBL5464) ↗

Open DB target context

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Receptor-interacting serine/threonine-protein kinase 1 (CHEMBL5464) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Receptor-interacting serine/threonine-protein kinase 1

CHEMBL5464

Anchored from Assay target.

Protein identity Receptor-interacting serine/threonine-protein kinase 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

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	1	8.07	8.07

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4545939	—	—	1	8.07

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4545939	—	IC50	=	8.5	nM	8.07