Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1780648

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

Functional
Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS-induced TNFalpha production pretreated 30 mins before LPS challenge measured after 4 hrs by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Kaptein A, Oubrie A, de Zwart E, Hoogenboom N, de Wit J, van de Kar B, van Hoek M, Vogel G, de Kimpe V, Schultz-Fademrecht C, Borsboom J, van Zeeland M, Versteegh J, Kazemier B, de Roos J, Wijnands F, Dulos J, Jaeger M, Leandro-Garcia P, Barf T.
Bioorg Med Chem Lett (2011) 21 : 3823 -3827
PubMed 21565498 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.83 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1779485 1 6.37
CHEMBL1779372 1 6.35
CHEMBL1779371 1 6.04
CHEMBL1779488 1 6.03
CHEMBL1779370 1 6.00
CHEMBL1779369 1 5.96
CHEMBL1779374 1 5.89
CHEMBL1779373 1 5.52
CHEMBL1779487 1 5.48
CHEMBL1779489 1 5.37
CHEMBL1779486 1 5.16
CHEMBL1779375 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1779485 EC50 = 430.0 nM 6.37
CHEMBL1779372 EC50 = 450.0 nM 6.35
CHEMBL1779371 EC50 = 920.0 nM 6.04
CHEMBL1779488 EC50 = 930.0 nM 6.03
CHEMBL1779370 EC50 = 1000.0 nM 6.00
CHEMBL1779369 EC50 = 1100.0 nM 5.96
CHEMBL1779374 EC50 = 1300.0 nM 5.89
CHEMBL1779373 EC50 = 3000.0 nM 5.52
CHEMBL1779487 EC50 = 3300.0 nM 5.48
CHEMBL1779489 EC50 = 4300.0 nM 5.37
CHEMBL1779486 EC50 = 6900.0 nM 5.16
CHEMBL1779375 EC50 > 10000.0 nM -