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Assay Detail

CHEMBL4815729

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

Binding
Inhibition of recombinant RIPK2 (unknown origin) using RS repeat peptide as substrate preincubated for 5 mins followed by substrate and ATP addition and further incubated for 2 hrs by ADP-Glo reagent based assay
27
Total Activities
27
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 2 (CHEMBL5014)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of pyrido[2,3-d]pyrimidin-7-one inhibitors of receptor interacting protein kinase-2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling.
Nikhar S, Siokas I, Schlicher L, Lee S, Gyrd-Hansen M, Degterev A, Cuny GD.
Eur J Med Chem (2021) 215 : 113252 -113252
PubMed 33601309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.48 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4847211 1 8.30
CHEMBL4864600 1 8.22
CHEMBL4861488 1 8.10
CHEMBL136244 1 7.98
CHEMBL4861447 1 7.96
CHEMBL49120 PD-0166285 1.0 1 7.89
CHEMBL4852860 1 7.89
CHEMBL4868894 1 7.85
CHEMBL4864714 1 7.84
CHEMBL4875011 1 7.82
CHEMBL4849134 1 7.80
CHEMBL4867467 1 7.80
CHEMBL4853179 1 7.77
CHEMBL4867716 1 7.77
CHEMBL4858463 1 7.68
CHEMBL4874031 1 7.68
CHEMBL4852513 1 7.68
CHEMBL4853711 1 7.66
CHEMBL4864576 1 7.60
CHEMBL4870434 1 7.60
CHEMBL4859351 1 7.57
CHEMBL4847571 1 7.47
CHEMBL4856366 1 7.19
CHEMBL4854929 1 6.98
CHEMBL4859716 1 6.89
CHEMBL4871544 1 4.52
CHEMBL136106 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4847211 IC50 = 5.0 nM 8.30
CHEMBL4864600 IC50 = 6.0 nM 8.22
CHEMBL4861488 IC50 = 8.0 nM 8.10
CHEMBL136244 IC50 = 10.5 nM 7.98
CHEMBL4861447 IC50 = 11.0 nM 7.96
CHEMBL49120 PD-0166285 IC50 = 13.0 nM 7.89
CHEMBL4852860 IC50 = 13.0 nM 7.89
CHEMBL4868894 IC50 = 14.0 nM 7.85
CHEMBL4864714 IC50 = 14.6 nM 7.84
CHEMBL4875011 IC50 = 15.0 nM 7.82
CHEMBL4849134 IC50 = 16.0 nM 7.80
CHEMBL4867467 IC50 = 16.0 nM 7.80
CHEMBL4853179 IC50 = 17.0 nM 7.77
CHEMBL4867716 IC50 = 17.0 nM 7.77
CHEMBL4858463 IC50 = 21.0 nM 7.68
CHEMBL4874031 IC50 = 21.0 nM 7.68
CHEMBL4852513 IC50 = 21.0 nM 7.68
CHEMBL4853711 IC50 = 22.0 nM 7.66
CHEMBL4864576 IC50 = 25.0 nM 7.60
CHEMBL4870434 IC50 = 25.0 nM 7.60
CHEMBL4859351 IC50 = 27.0 nM 7.57
CHEMBL4847571 IC50 = 34.0 nM 7.47
CHEMBL4856366 IC50 = 64.7 nM 7.19
CHEMBL4854929 IC50 = 105.0 nM 6.98
CHEMBL4859716 IC50 = 128.0 nM 6.89
CHEMBL4871544 IC50 = 30000.0 nM 4.52
CHEMBL136106 IC50 = 30000.0 nM 4.52