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Assay Detail

CHEMBL5535136

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

Functional
Protection against TSZ-induced necroptosis in human HT-29 cells preincubated with compound followed by TNA-alpha,Smac mimetic and Z-VAD-FMK addition and measured after 24 hrs by CCK-8 assay
16
Total Activities
16
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

From Hit to Lead: Structure-Based Optimization of Novel Selective Inhibitors of Receptor-Interacting Protein Kinase 1 (RIPK1) for the Treatment of Inflammatory Diseases.
Zhang L, Li Y, Tian C, Yang R, Wang Y, Xu H, Zhu Q, Chen S, Li L, Yang S.
J Med Chem (2024) 67 : 754 -773
PubMed 38159286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 10.02 10.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5594666 1 10.62
CHEMBL5574073 1 10.59
CHEMBL5570441 1 10.57
CHEMBL5595640 1 10.49
CHEMBL5572223 1 10.23
CHEMBL5572422 1 10.05
CHEMBL5570334 1 10.03
CHEMBL5593492 1 10.00
CHEMBL5592340 1 10.00
CHEMBL5570304 1 9.98
CHEMBL5591986 1 9.97
CHEMBL5575605 1 9.95
CHEMBL5570431 1 9.91
CHEMBL5571760 1 9.89
CHEMBL5403081 1 8.00
CHEMBL5564492 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5594666 EC50 = 0.024 nM 10.62
CHEMBL5574073 EC50 = 0.026 nM 10.59
CHEMBL5570441 EC50 = 0.027 nM 10.57
CHEMBL5595640 EC50 = 0.032 nM 10.49
CHEMBL5572223 EC50 = 0.059 nM 10.23
CHEMBL5572422 EC50 = 0.09 nM 10.05
CHEMBL5570334 EC50 = 0.094 nM 10.03
CHEMBL5593492 EC50 = 0.1 nM 10.00
CHEMBL5592340 EC50 = 0.101 nM 10.00
CHEMBL5570304 EC50 = 0.105 nM 9.98
CHEMBL5591986 EC50 = 0.107 nM 9.97
CHEMBL5575605 EC50 = 0.113 nM 9.95
CHEMBL5570431 EC50 = 0.123 nM 9.91
CHEMBL5571760 EC50 = 0.128 nM 9.89
CHEMBL5403081 EC50 = 10.0 nM 8.00
CHEMBL5564492 EC50 = 0.003 nM -