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Assay Detail

CHEMBL3390768

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Functional
Antipyroptotic activity in PMA-differentiated and LPS-primed human THP1 cells assessed as decrease in ATP-induced pyroptosis measured as LDH activity after 1 hrs pretreated with 5 mM ATP for 1 hr by colorimetric assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Electrophilic warhead-based design of compounds preventing NLRP3 inflammasome-dependent pyroptosis.
Cocco M, Garella D, Di Stilo A, Borretto E, Stevanato L, Giorgis M, Marini E, Fantozzi R, Miglio G, Bertinaria M.
J Med Chem (2014) 57 : 10366 -10382
PubMed 25418070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.88 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3358576 1 7.10
CHEMBL3358585 1 7.00
CHEMBL4298697 1 6.90
CHEMBL2047937 1 6.90
CHEMBL3358575 1 6.90
CHEMBL3358584 1 6.90
CHEMBL3358179 1 6.80
CHEMBL3358178 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3358576 EC50 = 79.43 nM 7.10
CHEMBL3358585 EC50 = 100.0 nM 7.00
CHEMBL4298697 EC50 = 125.89 nM 6.90
CHEMBL2047937 EC50 = 125.89 nM 6.90
CHEMBL3358575 EC50 = 125.89 nM 6.90
CHEMBL3358584 EC50 = 125.89 nM 6.90
CHEMBL3358179 EC50 = 158.49 nM 6.80
CHEMBL3358178 EC50 = 316.23 nM 6.50