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Assay Detail

CHEMBL956587

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

Functional
Inhibition of LPS-stimulated TNFalpha release from human PBMC after 3 hrs
17
Total Activities
17
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

Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.
Schlapbach A, Feifel R, Hawtin S, Heng R, Koch G, Moebitz H, Revesz L, Scheufler C, Velcicky J, Waelchli R, Huppertz C.
Bioorg Med Chem Lett (2008) 18 : 6142 -6146
PubMed 18945615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.28 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL461140 1 7.40
CHEMBL461139 1 6.96
CHEMBL516802 1 6.82
CHEMBL516504 1 6.46
CHEMBL461316 1 6.42
CHEMBL504267 1 5.96
CHEMBL518824 1 5.82
CHEMBL507348 1 5.64
CHEMBL455156 1 5.00
CHEMBL462578 1 -
CHEMBL462371 1 -
CHEMBL462372 1 -
CHEMBL460091 1 -
CHEMBL452086 1 -
CHEMBL452085 1 -
CHEMBL455396 1 -
CHEMBL462579 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL461140 IC50 = 40.0 nM 7.40
CHEMBL461139 IC50 = 110.0 nM 6.96
CHEMBL516802 IC50 = 150.0 nM 6.82
CHEMBL516504 IC50 = 350.0 nM 6.46
CHEMBL461316 IC50 = 380.0 nM 6.42
CHEMBL504267 IC50 = 1100.0 nM 5.96
CHEMBL518824 IC50 = 1500.0 nM 5.82
CHEMBL507348 IC50 = 2300.0 nM 5.64
CHEMBL455156 IC50 = 10000.0 nM 5.00
CHEMBL462578 IC50 - -
CHEMBL462371 IC50 - -
CHEMBL462372 IC50 - -
CHEMBL460091 IC50 > 10000.0 nM -
CHEMBL452086 IC50 - -
CHEMBL452085 IC50 - -
CHEMBL455396 IC50 > 10000.0 nM -
CHEMBL462579 IC50 - -