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Assay Detail

CHEMBL732094

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

Binding
In vitro inhibitory activity determined against human mitogen-activated protein kinase p38 alpha
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
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 24 7.25 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL152208 1 8.40
CHEMBL356455 1 8.30
CHEMBL155567 1 8.15
CHEMBL152767 1 8.00
CHEMBL153265 1 7.92
CHEMBL152820 1 7.89
CHEMBL155508 1 7.68
CHEMBL119385 NEFLAMAPIMOD 2.0 1 7.54
CHEMBL357732 1 7.54
CHEMBL279416 VK-19911 1 7.42
CHEMBL347496 1 7.41
CHEMBL153012 1 7.38
CHEMBL152440 1 7.27
CHEMBL422510 1 7.20
CHEMBL347770 1 7.00
CHEMBL155448 1 6.86
CHEMBL356157 1 6.84
CHEMBL152596 1 6.84
CHEMBL152349 1 6.71
CHEMBL347576 1 6.36
CHEMBL152209 1 6.24
CHEMBL356809 1 6.09
CHEMBL152403 1 5.81
CHEMBL153795 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL152208 IC50 = 4.0 nM 8.40
CHEMBL356455 IC50 = 5.0 nM 8.30
CHEMBL155567 IC50 = 7.0 nM 8.15
CHEMBL152767 IC50 = 10.0 nM 8.00
CHEMBL153265 IC50 = 12.0 nM 7.92
CHEMBL152820 IC50 = 13.0 nM 7.89
CHEMBL155508 IC50 = 21.0 nM 7.68
CHEMBL119385 NEFLAMAPIMOD IC50 = 29.0 nM 7.54
CHEMBL357732 IC50 = 29.0 nM 7.54
CHEMBL279416 VK-19911 IC50 = 38.0 nM 7.42
CHEMBL347496 IC50 = 39.0 nM 7.41
CHEMBL153012 IC50 = 42.0 nM 7.38
CHEMBL152440 IC50 = 54.0 nM 7.27
CHEMBL422510 IC50 = 63.0 nM 7.20
CHEMBL347770 IC50 = 101.0 nM 7.00
CHEMBL155448 IC50 = 139.0 nM 6.86
CHEMBL356157 IC50 = 143.0 nM 6.84
CHEMBL152596 IC50 = 145.0 nM 6.84
CHEMBL152349 IC50 = 193.0 nM 6.71
CHEMBL347576 IC50 = 437.0 nM 6.36
CHEMBL152209 IC50 = 574.0 nM 6.24
CHEMBL356809 IC50 = 811.0 nM 6.09
CHEMBL152403 IC50 = 1550.0 nM 5.81
CHEMBL153795 IC50 > 100000.0 nM -