Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5584587

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

Binding
Inhibition of N-terminal poly his-tagged recombinant RIPK2 (8 to 310 residues) (unknown origin) expressed in Sf9 cells preincubated for 15 mins followed by ATP addition and measured after 90 mins mins by by ADP-Glo reagent based luminescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
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, synthesis and evaluation of novel thieno[2,3d]pyrimidine derivatives as potent and specific RIPK2 inhibitors.
Misehe M, Šála M, Matoušová M, Hercík K, Kocek H, Chalupská D, Chaloupecká E, Hájek M, Boura E, Mertlíková-Kaiserová H, Nencka R.
Bioorg Med Chem Lett (2024) 97 : 129567 -129567
PubMed 38008339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.02 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5598306 1 8.52
CHEMBL4514780 1 8.40
CHEMBL5596566 1 8.40
CHEMBL5596719 1 8.40
CHEMBL5596475 1 8.30
CHEMBL5597795 1 8.30
CHEMBL5597463 1 8.15
CHEMBL5598474 1 8.10
CHEMBL5596401 1 8.10
CHEMBL5590947 1 8.05
CHEMBL5597680 1 8.00
CHEMBL5598225 1 7.96
CHEMBL5597383 1 7.96
CHEMBL5596824 1 7.96
CHEMBL5596171 1 7.92
CHEMBL5598127 1 7.89
CHEMBL5598037 1 7.85
CHEMBL5597768 1 7.82
CHEMBL5597925 1 7.80
CHEMBL5598319 1 7.77
CHEMBL5597496 1 7.77
CHEMBL5597467 1 7.75
CHEMBL5597059 1 7.68
CHEMBL5597382 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5598306 IC50 = 3.0 nM 8.52
CHEMBL4514780 IC50 = 4.0 nM 8.40
CHEMBL5596566 IC50 = 4.0 nM 8.40
CHEMBL5596719 IC50 = 4.0 nM 8.40
CHEMBL5596475 IC50 = 5.0 nM 8.30
CHEMBL5597795 IC50 = 5.0 nM 8.30
CHEMBL5597463 IC50 = 7.0 nM 8.15
CHEMBL5598474 IC50 = 8.0 nM 8.10
CHEMBL5596401 IC50 = 8.0 nM 8.10
CHEMBL5590947 IC50 = 9.0 nM 8.05
CHEMBL5597680 IC50 = 10.0 nM 8.00
CHEMBL5598225 IC50 = 11.0 nM 7.96
CHEMBL5597383 IC50 = 11.0 nM 7.96
CHEMBL5596824 IC50 = 11.0 nM 7.96
CHEMBL5596171 IC50 = 12.0 nM 7.92
CHEMBL5598127 IC50 = 13.0 nM 7.89
CHEMBL5598037 IC50 = 14.0 nM 7.85
CHEMBL5597768 IC50 = 15.0 nM 7.82
CHEMBL5597925 IC50 = 16.0 nM 7.80
CHEMBL5598319 IC50 = 17.0 nM 7.77
CHEMBL5597496 IC50 = 17.0 nM 7.77
CHEMBL5597467 IC50 = 18.0 nM 7.75
CHEMBL5597059 IC50 = 21.0 nM 7.68
CHEMBL5597382 IC50 = 26.0 nM 7.58