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Assay Detail

CHEMBL4186129

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

Binding
Inhibition of TACE in NHEK assessed as reduction in LPS/TPA-stimulated TNFalpha production preincubated for 1 hr followed by LPS/TPA stimulation for 24 hrs by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.
Boiteau JG, Ouvry G, Arlabosse JM, Astri S, Beillard A, Bhurruth-Alcor Y, Bonnary L, Bouix-Peter C, Bouquet K, Bourotte M, Cardinaud I, Comino C, Deprez B, Duvert D, Féret A, Hacini-Rachinel F, Harris CS, Luzy AP, Mathieu A, Millois C, Orsini N, Pascau J, Pinto A, Piwnica D, Polge G, Reitz A, Reversé K, Rodeville N, Rossio P, Spiesse D, Tabet S, Taquet N, Tomas L, Vial E, Hennequin LF.
Bioorg Med Chem (2018) 26 : 945 -956
PubMed 28818461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.11 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215407 1 8.52
CHEMBL4208519 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215407 IC50 = 3.0 nM 8.52
CHEMBL4208519 IC50 = 20.0 nM 7.70