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Assay Detail

CHEMBL1065268

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Functional
Antiinflammatory activity against LPS-stimulated TNFalpha production in human monocytes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Harris CM, Ericsson AM, Argiriadi MA, Barberis C, Borhani DW, Burchat A, Calderwood DJ, Cunha GA, Dixon RW, Frank KE, Johnson EF, Kamens J, Kwak S, Li B, Mullen KD, Perron DC, Wang L, Wishart N, Wu X, Zhang X, Zmetra TR, Talanian RV.
Bioorg Med Chem Lett (2010) 20 : 334 -337
PubMed 19926477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.72 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL591797 1 7.26
CHEMBL592030 1 7.07
CHEMBL590109 1 6.55
CHEMBL595933 1 6.00
CHEMBL596588 1 -
CHEMBL594090 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL591797 IC50 = 55.0 nM 7.26
CHEMBL592030 IC50 = 86.0 nM 7.07
CHEMBL590109 IC50 = 280.0 nM 6.55
CHEMBL595933 IC50 = 1000.0 nM 6.00
CHEMBL596588 IC50 > 25000.0 nM -
CHEMBL594090 IC50 > 25000.0 nM -