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Assay Detail

CHEMBL3789104

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

Binding
Binding affinity to human RIP1 (1 to 375 residues) preincubated for 10 mins measured after 20 mins by fluorescence polarization assay
7
Total Activities
7
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
IC50 7 7.20 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3785703 1 8.00
CHEMBL3109202 1 7.60
CHEMBL3786293 1 7.50
CHEMBL3786162 1 7.40
CHEMBL3786778 1 6.50
CHEMBL370438 1 6.20
CHEMBL3787216 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3785703 IC50 = 10.0 nM 8.00
CHEMBL3109202 IC50 = 25.0 nM 7.60
CHEMBL3786293 IC50 = 32.0 nM 7.50
CHEMBL3786162 IC50 = 40.0 nM 7.40
CHEMBL3786778 IC50 = 320.0 nM 6.50
CHEMBL370438 IC50 = 630.0 nM 6.20
CHEMBL3787216 IC50 > 10000.0 nM -