Assay Detail

CHEMBL3390769

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

Functional

Antipyroptotic activity in PMA-differentiated and LPS-primed human THP1 cells assessed as decrease in nigericin-induced pyroptosis measured as LDH activity after 1 hrs pretreated with 10 uM nigericin for 1.5 hrs by colorimetric assay

ChEMBL ↗

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Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗

Open DB target context

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NON-PROTEIN TARGET (CHEMBL3879801) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target NON-PROTEIN TARGET

CHEMBL3879801

Anchored from Assay target.

Protein identity NON-PROTEIN TARGET

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗

Type	NON-MOLECULAR

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	6.64	6.90
Inhibition	8	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3358575	—	—	2	6.90
CHEMBL2047937	—	—	2	6.80
CHEMBL3358584	—	—	2	6.80
CHEMBL3358178	—	—	2	6.70
CHEMBL3358576	—	—	2	6.70
CHEMBL3358179	—	—	2	6.60
CHEMBL4298697	—	—	2	6.30
CHEMBL3358585	—	—	2	6.30

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3358575	—	EC50	=	125.89	nM	6.90
CHEMBL2047937	—	EC50	=	158.49	nM	6.80
CHEMBL3358584	—	EC50	=	158.49	nM	6.80
CHEMBL3358178	—	EC50	=	199.53	nM	6.70
CHEMBL3358576	—	EC50	=	199.53	nM	6.70
CHEMBL3358179	—	EC50	=	251.19	nM	6.60
CHEMBL4298697	—	EC50	=	501.19	nM	6.30
CHEMBL3358585	—	EC50	=	501.19	nM	6.30
CHEMBL4298697	—	Inhibition		-	%	-
CHEMBL3358178	—	Inhibition		-	%	-
CHEMBL2047937	—	Inhibition		-	%	-
CHEMBL3358179	—	Inhibition		-	%	-
CHEMBL3358575	—	Inhibition		-	%	-
CHEMBL3358576	—	Inhibition		-	%	-
CHEMBL3358584	—	Inhibition		-	%	-
CHEMBL3358585	—	Inhibition		-	%	-