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Assay Detail

CHEMBL5524326

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

Functional
Anti-necroptic activity against human HT-29 cells assessed as cell viability pretreated with compound followed by TNF-alpha/Smac mimetic/Z-VAD-FMK stimulation for 16 hrs by Cell Titer Glo assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Autocuration

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of novel biaryl benzoxazepinones as dual-mode receptor-interacting protein kinase-1 (RIPK1) inhibitors.
Xin Y, Dai P, Shao H, Zhuang C, Li J.
Bioorg Med Chem (2024) 100 : 117611 -117611
PubMed 38309200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 8.01 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5561756 1 8.77
CHEMBL4071864 GSK2982772 2.0 1 8.54
CHEMBL5561876 1 8.52
CHEMBL5560332 1 8.52
CHEMBL5565428 1 8.48
CHEMBL5556433 1 8.47
CHEMBL5568058 1 8.46
CHEMBL5567676 1 8.42
CHEMBL5562023 1 8.24
CHEMBL5561036 1 8.12
CHEMBL5562395 1 8.08
CHEMBL5566734 1 8.08
CHEMBL5568607 1 8.06
CHEMBL5556292 1 8.01
CHEMBL5558452 1 8.00
CHEMBL5563484 1 7.96
CHEMBL5568551 1 7.93
CHEMBL5561523 1 7.90
CHEMBL5568348 1 7.85
CHEMBL5563478 1 7.69
CHEMBL5564150 1 7.56
CHEMBL5567654 1 7.52
CHEMBL5559956 1 7.48
CHEMBL5562465 1 7.25
CHEMBL5565633 1 7.22
CHEMBL5562035 1 7.08
CHEMBL5561071 1 -
CHEMBL5568096 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5561756 EC50 = 1.7 nM 8.77
CHEMBL4071864 GSK2982772 EC50 = 2.9 nM 8.54
CHEMBL5561876 EC50 = 3.0 nM 8.52
CHEMBL5560332 EC50 = 3.0 nM 8.52
CHEMBL5565428 EC50 = 3.3 nM 8.48
CHEMBL5556433 EC50 = 3.4 nM 8.47
CHEMBL5568058 EC50 = 3.5 nM 8.46
CHEMBL5567676 EC50 = 3.8 nM 8.42
CHEMBL5562023 EC50 = 5.8 nM 8.24
CHEMBL5561036 EC50 = 7.6 nM 8.12
CHEMBL5562395 EC50 = 8.3 nM 8.08
CHEMBL5566734 EC50 = 8.3 nM 8.08
CHEMBL5568607 EC50 = 8.8 nM 8.06
CHEMBL5556292 EC50 = 9.8 nM 8.01
CHEMBL5558452 EC50 = 10.0 nM 8.00
CHEMBL5563484 EC50 = 10.9 nM 7.96
CHEMBL5568551 EC50 = 11.7 nM 7.93
CHEMBL5561523 EC50 = 12.5 nM 7.90
CHEMBL5568348 EC50 = 14.1 nM 7.85
CHEMBL5563478 EC50 = 20.3 nM 7.69
CHEMBL5564150 EC50 = 27.3 nM 7.56
CHEMBL5567654 EC50 = 29.9 nM 7.52
CHEMBL5559956 EC50 = 32.9 nM 7.48
CHEMBL5562465 EC50 = 56.8 nM 7.25
CHEMBL5565633 EC50 = 60.0 nM 7.22
CHEMBL5562035 EC50 = 82.7 nM 7.08
CHEMBL5561071 EC50 > 100.0 nM -
CHEMBL5568096 EC50 > 100.0 nM -