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Items: 1 to 20 of 956

5.

BindingDB_Patents: Fluorescence Resonance Energy Transfer (FRET) Assay. The enzyme inhibitory activity of test compounds was determined by fluorescence resonance energy transfer (FRET) using synthetic peptides labelled with both donor and acceptor fluorophores (Z-LYTE, Invitrogen). Recombinant, phosphorylated p38 MAPK (MAPK12:Millipore) was diluted in HEPES buffer, mixed with compound at the desired final concentrations and incubated for 2 hr at RT. The FRET peptide (2 uM) and ATP (100 uM) were next added to the enzyme/compound mixture and incubated for 1 hr. Development reagent (protease) was added for 1 hr prior to detection in a fluorescence microplate reader. The site-specific protease only cleaves non-phosphorylated peptide and eliminates the FRET signal. Phosphorylation levels of each reaction were calculated using the ratio of coumarin emission (donor) over fluorescein emission (acceptor) with high ratios indicating high phosphorylation levels and low ratios indicating low phosp

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 14; MAP kinase 14; MAPK 14; Cytokine suppressive anti-inflammatory drug-binding protein; CSAID-binding protein; CSBP; MAP kinase MXI2; MAX-interacting protein 2; Mitogen-activated protein kinase p38 alpha; MAP kinase p38 alpha; Stress-activated protein kinase 2a; SAPK2a
AID:
1258481
8.

BindingDB_Patents: Inhibition Assay. Enzymatic activity assay was performed in 96-well microtiter plates (Corning, catalog number #3686) using a total volume of 50 ul of an assay buffer composed of 50 mM HEPES pH 7.5, 10 mM MgCl2, 1.75 mM Na3VO4. Various concentrations of the test compound or vehicle controls were pre-incubated for one hour with 0.055 ug/ml of the human p38alfa (SAPKa) enzyme (obtained from University of Dundee). The reaction was started by addition of biotinylated ATF2 substrate and ATP in concentrations around their Km values (final concentration 0.62 uM and 60 uM respectively) and took place for one hour at 25 C. Addition of the detection reagents, streptavidin XL665 and anti-phosphoresidue antibody coupled to Europium cryptate, caused the juxtaposition of the cryptate and the XL665 fluorophore, resulting in fluorescence energy transfer (FRET). The FRET intensity depends on the amount of bounded cryptate antibody, which is proportional to the extent of substrate pho

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 14; MAP kinase 14; MAPK 14; Cytokine suppressive anti-inflammatory drug-binding protein; CSAID-binding protein; CSBP; MAP kinase MXI2; MAX-interacting protein 2; Mitogen-activated protein kinase p38 alpha; MAP kinase p38 alpha; Stress-activated protein kinase 2a; SAPK2a
AID:
1258079
10.
11.

Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by proprietary radioisotopic protein kinase assay

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 14; MAP kinase 14; MAPK 14; Cytokine suppressive anti-inflammatory drug-binding protein; CSAID-binding protein; CSBP; MAP kinase MXI2; MAX-interacting protein 2; Mitogen-activated protein kinase p38 alpha; MAP kinase p38 alpha; Stress-activated protein kinase 2a; SAPK2a
12.

Inhibition of P38a (unknown origin) after 120 mins by HotSpot assay

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 14; MAP kinase 14; MAPK 14; Cytokine suppressive anti-inflammatory drug-binding protein; CSAID-binding protein; CSBP; MAP kinase MXI2; MAX-interacting protein 2; Mitogen-activated protein kinase p38 alpha; MAP kinase p38 alpha; Stress-activated protein kinase 2a; SAPK2a
13.

Inhibition of P38gamma (unknown origin) at 10 uM after 120 mins P33 radiolabeled kinase activity assay

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 12; MAP kinase 12; MAPK 12; Extracellular signal-regulated kinase 6; ERK-6; Mitogen-activated protein kinase p38 gamma; MAP kinase p38 gamma; Stress-activated protein kinase 3
14.

Inhibition of P38delta (unknown origin) at 10 uM after 120 mins P33 radiolabeled kinase activity assay

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 13; MAP kinase 13; MAPK 13; Mitogen-activated protein kinase p38 delta; MAP kinase p38 delta; Stress-activated protein kinase 4
15.

Inhibition of P38beta (unknown origin) at 10 uM after 120 mins P33 radiolabeled kinase activity assay

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 11; MAP kinase 11; MAPK 11; Mitogen-activated protein kinase p38 beta; MAP kinase p38 beta; p38b; Stress-activated protein kinase 2b; SAPK2b; p38-2
16.

Inhibition of P38alpha (unknown origin) at 10 uM after 120 mins P33 radiolabeled kinase activity assay

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 14; MAP kinase 14; MAPK 14; Cytokine suppressive anti-inflammatory drug-binding protein; CSAID-binding protein; CSBP; MAP kinase MXI2; MAX-interacting protein 2; Mitogen-activated protein kinase p38 alpha; MAP kinase p38 alpha; Stress-activated protein kinase 2a; SAPK2a
17.

Inhibition of p38-beta (unknown origin) assessed as remaining activity at 10 uM by high-throughput assay relative to control

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 11; MAP kinase 11; MAPK 11; Mitogen-activated protein kinase p38 beta; MAP kinase p38 beta; p38b; Stress-activated protein kinase 2b; SAPK2b; p38-2
18.

Inhibition of p38-alpha (unknown origin) assessed as remaining activity at 10 uM by high-throughput assay relative to control

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 14; MAP kinase 14; MAPK 14; Cytokine suppressive anti-inflammatory drug-binding protein; CSAID-binding protein; CSBP; MAP kinase MXI2; MAX-interacting protein 2; Mitogen-activated protein kinase p38 alpha; MAP kinase p38 alpha; Stress-activated protein kinase 2a; SAPK2a
19.

Inhibition of p38alpha (unknown origin) at 1 uM by FRET method

Source:
ChEMBL
Protein Target:
Mitogen-activated protein kinase 14; MAP kinase 14; MAPK 14; Cytokine suppressive anti-inflammatory drug-binding protein; CSAID-binding protein; CSBP; MAP kinase MXI2; MAX-interacting protein 2; Mitogen-activated protein kinase p38 alpha; MAP kinase p38 alpha; Stress-activated protein kinase 2a; SAPK2a
20.

Activation of p38 in human Caki1 cells assessed as downregulation of Snail at 250 to 1000 pM after 24 hrs by Western blot analysis

Source:
ChEMBL
Protein Targets:
Mitogen-activated protein kinase 11; MAP kinase 11; MAPK 11; Mitogen-activated protein kinase p38 beta; MAP kinase p38 beta; p38b; Stress-activated protein kinase 2b; SAPK2b; p38-2; ...
Total:
4
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