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Assay Detail

CHEMBL5147326

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

Functional
Anti-necroptic activity in human HT-29 cells assessed as inhibition of TSZ induced necroptosis measured after 16 to 24 hrs by celltiter-glo luminescent cell viability assay
36
Total Activities
36
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

Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors.
Hao Y, Shao H, Qu Z, Li J, Shi Y, Zhang W, Yu J, Fu P, Zhuang C.
Eur J Med Chem (2022) 236 : 114345 -114345
PubMed 35398729 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 6.14 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5188220 1 8.60
CHEMBL5209042 1 8.05
CHEMBL5180233 1 8.05
CHEMBL5177347 1 7.77
CHEMBL5181292 1 7.44
CHEMBL5183211 1 6.74
CHEMBL5205368 1 6.68
CHEMBL5185226 1 6.54
CHEMBL5188420 1 6.44
CHEMBL5190555 1 6.38
CHEMBL5192442 1 6.29
CHEMBL5209141 1 6.25
CHEMBL5204963 1 6.09
CHEMBL5206018 1 6.04
CHEMBL5181537 1 6.00
CHEMBL5187477 1 5.97
CHEMBL5195401 1 5.91
CHEMBL5193950 1 5.81
CHEMBL5181126 1 5.80
CHEMBL5193335 1 5.71
CHEMBL5183398 1 5.65
CHEMBL5195465 1 5.62
CHEMBL5183031 1 5.62
CHEMBL5184282 1 5.57
CHEMBL5197698 1 5.55
CHEMBL5209346 1 5.45
CHEMBL5190483 1 5.44
CHEMBL5183455 1 5.42
CHEMBL5180814 1 5.40
CHEMBL5190780 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5188220 EC50 = 2.5 nM 8.60
CHEMBL5209042 EC50 = 8.9 nM 8.05
CHEMBL5180233 EC50 = 8.9 nM 8.05
CHEMBL5177347 EC50 = 17.0 nM 7.77
CHEMBL5181292 EC50 = 36.0 nM 7.44
CHEMBL5183211 EC50 = 180.6 nM 6.74
CHEMBL5205368 EC50 = 208.5 nM 6.68
CHEMBL5185226 EC50 = 288.0 nM 6.54
CHEMBL5188420 EC50 = 359.6 nM 6.44
CHEMBL5190555 EC50 = 414.0 nM 6.38
CHEMBL5192442 EC50 = 510.0 nM 6.29
CHEMBL5209141 EC50 = 566.0 nM 6.25
CHEMBL5204963 EC50 = 805.0 nM 6.09
CHEMBL5206018 EC50 = 916.1 nM 6.04
CHEMBL5181537 EC50 = 1004.0 nM 6.00
CHEMBL5187477 EC50 = 1066.0 nM 5.97
CHEMBL5195401 EC50 = 1231.0 nM 5.91
CHEMBL5193950 EC50 = 1550.0 nM 5.81
CHEMBL5181126 EC50 = 1583.0 nM 5.80
CHEMBL5193335 EC50 = 1949.0 nM 5.71
CHEMBL5183398 EC50 = 2257.0 nM 5.65
CHEMBL5195465 EC50 = 2403.0 nM 5.62
CHEMBL5183031 EC50 = 2383.0 nM 5.62
CHEMBL5184282 EC50 = 2682.0 nM 5.57
CHEMBL5197698 EC50 = 2825.0 nM 5.55
CHEMBL5209346 EC50 = 3531.0 nM 5.45
CHEMBL5190483 EC50 = 3638.0 nM 5.44
CHEMBL5183455 EC50 = 3834.0 nM 5.42
CHEMBL5180814 EC50 = 3998.0 nM 5.40
CHEMBL5190780 EC50 = 3968.0 nM 5.40
CHEMBL5204361 EC50 = 4423.0 nM 5.35
CHEMBL5189569 EC50 = 4763.0 nM 5.32
CHEMBL5197465 EC50 = 5525.0 nM 5.26
CHEMBL5186322 EC50 = 6311.0 nM 5.20
CHEMBL5187665 EC50 > 10000.0 nM -
CHEMBL5185311 EC50 > 10000.0 nM -