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Assay Detail

CHEMBL769659

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

Functional
In vitro inhibition of IL1-beta release from LPS stimulated human peripheral blood mononuclear cells.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

MAP kinase p38 (CHEMBL2094115)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.
Ottosen ER, Sørensen MD, Björkling F, Skak-Nielsen T, Fjording MS, Aaes H, Binderup L.
J Med Chem (2003) 46 : 5651 -5662
PubMed 14667219 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.13 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155508 1 8.05
CHEMBL152767 1 7.85
CHEMBL153012 1 7.80
CHEMBL152208 1 7.77
CHEMBL422510 1 7.68
CHEMBL152820 1 7.66
CHEMBL153265 1 7.58
CHEMBL356455 1 7.55
CHEMBL347496 1 7.52
CHEMBL152440 1 7.35
CHEMBL357732 1 7.17
CHEMBL347770 1 7.16
CHEMBL155567 1 6.92
CHEMBL152349 1 6.76
CHEMBL152596 1 6.65
CHEMBL279416 VK-19911 1 6.57
CHEMBL356157 1 6.46
CHEMBL347576 1 6.37
CHEMBL155448 1 6.36
CHEMBL356809 1 6.32
CHEMBL152209 1 6.24
CHEMBL153795 1 -
CHEMBL152403 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155508 IC50 = 9.0 nM 8.05
CHEMBL152767 IC50 = 14.0 nM 7.85
CHEMBL153012 IC50 = 16.0 nM 7.80
CHEMBL152208 IC50 = 17.0 nM 7.77
CHEMBL422510 IC50 = 21.0 nM 7.68
CHEMBL152820 IC50 = 22.0 nM 7.66
CHEMBL153265 IC50 = 26.0 nM 7.58
CHEMBL356455 IC50 = 28.0 nM 7.55
CHEMBL347496 IC50 = 30.0 nM 7.52
CHEMBL152440 IC50 = 45.0 nM 7.35
CHEMBL357732 IC50 = 67.0 nM 7.17
CHEMBL347770 IC50 = 70.0 nM 7.16
CHEMBL155567 IC50 = 119.0 nM 6.92
CHEMBL152349 IC50 = 175.0 nM 6.76
CHEMBL152596 IC50 = 226.0 nM 6.65
CHEMBL279416 VK-19911 IC50 = 272.0 nM 6.57
CHEMBL356157 IC50 = 343.0 nM 6.46
CHEMBL347576 IC50 = 427.0 nM 6.37
CHEMBL155448 IC50 = 437.0 nM 6.36
CHEMBL356809 IC50 = 483.0 nM 6.32
CHEMBL152209 IC50 = 580.0 nM 6.24
CHEMBL153795 IC50 > 10000.0 nM -
CHEMBL152403 IC50 > 5000.0 nM -