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Assay Detail

CHEMBL5629638

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Functional
Inhibition of necroptosis in human U-937 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 1 — Organism
Curated By Autocuration

Target

U-937 (CHEMBL612794)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel cyclic malonamide derivatives as selective RIPK1 inhibitors.
Petró JL, Bényei G, Bana P, Linke N, Horti F, Szabó JE, Szalai KK, Hornyánszky G, Greiner I, Éles J.
Bioorg Med Chem Lett (2024) 100 : 129643 -129643
PubMed 38316369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.99 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071864 GSK2982772 2.0 1 8.23
CHEMBL5632371 1 7.95
CHEMBL5632067 1 7.44
CHEMBL5633027 1 7.24
CHEMBL5632839 1 7.21
CHEMBL5633468 1 7.20
CHEMBL5632090 1 7.10
CHEMBL5633836 1 6.83
CHEMBL5632042 1 6.37
CHEMBL5633109 1 6.25
CHEMBL5633631 1 6.05
CHEMBL5631547 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071864 GSK2982772 IC50 = 5.888 nM 8.23
CHEMBL5632371 IC50 = 11.22 nM 7.95
CHEMBL5632067 IC50 = 36.31 nM 7.44
CHEMBL5633027 IC50 = 57.54 nM 7.24
CHEMBL5632839 IC50 = 61.66 nM 7.21
CHEMBL5633468 IC50 = 63.1 nM 7.20
CHEMBL5632090 IC50 = 79.43 nM 7.10
CHEMBL5633836 IC50 = 147.91 nM 6.83
CHEMBL5632042 IC50 = 426.58 nM 6.37
CHEMBL5633109 IC50 = 562.34 nM 6.25
CHEMBL5633631 IC50 = 891.25 nM 6.05
CHEMBL5631547 IC50 = 1096.48 nM 5.96