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Assay Detail

CHEMBL5734810

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

Binding
Assay of p38 Kinase Activity: Experimental Method: 40 nM p38a was added into a reaction buffer, which include 20 mM HEPES (4-hydroxyethylpiperazine ethanesulfonic acid), 5 mM MgCl2 and 1 mM DTT (dithiothreitol) at pH 7.4. 40 μM phosphorylated peptide substrate was added, followed by different concentrations of drugs and 100 μM ATP (adenosine triphosphate), and reacted for 90 minutes in dark. The fluorescence values were determined at excitation and emission wavelengths of 544 nM and 590 nM respectively. The IC50 values of the compounds were obtained according to the fluorescence values.
72
Total Activities
24
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzamide derivative
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.14 6.26
kon 24 - -
k_off 24 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5845520 3 6.26
CHEMBL5849787 3 6.26
CHEMBL5851332 3 6.26
CHEMBL6018153 3 6.26
CHEMBL5954596 3 6.26
CHEMBL6053768 3 6.26
CHEMBL5888672 3 6.26
CHEMBL1088752 LOSMAPIMOD 3.0 3 5.26
CHEMBL5959448 3 -
CHEMBL5977503 3 -
CHEMBL6021110 3 -
CHEMBL5838074 3 -
CHEMBL6000030 3 -
CHEMBL5742619 3 -
CHEMBL5864316 3 -
CHEMBL5905513 3 -
CHEMBL5875721 3 -
CHEMBL5753624 3 -
CHEMBL5972656 3 -
CHEMBL5825952 3 -
CHEMBL6032738 3 -
CHEMBL6001751 3 -
CHEMBL5959348 3 -
CHEMBL5948708 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5851332 IC50 = 550.0 nM 6.26
CHEMBL5888672 IC50 = 550.0 nM 6.26
CHEMBL6018153 IC50 = 550.0 nM 6.26
CHEMBL5954596 IC50 = 550.0 nM 6.26
CHEMBL5849787 IC50 = 550.0 nM 6.26
CHEMBL6053768 IC50 = 550.0 nM 6.26
CHEMBL5845520 IC50 = 550.0 nM 6.26
CHEMBL1088752 LOSMAPIMOD IC50 = 5500.0 nM 5.26
CHEMBL5742619 IC50 < 100.0 nM -
CHEMBL6021110 IC50 < 100.0 nM -
CHEMBL1088752 LOSMAPIMOD k_off = - s-1 -
CHEMBL5742619 k_off = - s-1 -
CHEMBL6000030 IC50 < 100.0 nM -
CHEMBL6000030 kon = - -
CHEMBL6000030 k_off = - s-1 -
CHEMBL5838074 IC50 < 100.0 nM -
CHEMBL5838074 kon = - -
CHEMBL5864316 k_off = - s-1 -
CHEMBL5972656 kon = - -
CHEMBL5972656 k_off = - s-1 -
CHEMBL6032738 k_off = - s-1 -
CHEMBL6032738 kon = - -
CHEMBL6032738 IC50 < 100.0 nM -
CHEMBL5825952 k_off = - s-1 -
CHEMBL5825952 kon = - -
CHEMBL5825952 IC50 < 100.0 nM -
CHEMBL5849787 k_off = - s-1 -
CHEMBL5849787 kon = - -
CHEMBL5954596 kon = - -
CHEMBL5888672 kon = - -
CHEMBL5864316 kon = - -
CHEMBL5742619 kon = - -
CHEMBL5864316 IC50 < 100.0 nM -
CHEMBL5905513 k_off = - s-1 -
CHEMBL5905513 kon = - -
CHEMBL5905513 IC50 < 100.0 nM -
CHEMBL5875721 k_off = - s-1 -
CHEMBL5875721 kon = - -
CHEMBL5875721 IC50 < 100.0 nM -
CHEMBL5888672 k_off = - s-1 -
CHEMBL6021110 kon = - -
CHEMBL5845520 k_off = - s-1 -
CHEMBL5845520 kon = - -
CHEMBL5838074 k_off = - s-1 -
CHEMBL5959448 IC50 < 100.0 nM -
CHEMBL1088752 LOSMAPIMOD kon = - -
CHEMBL5977503 k_off = - s-1 -
CHEMBL5977503 kon = - -
CHEMBL5977503 IC50 < 100.0 nM -
CHEMBL6021110 k_off = - s-1 -