| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA679355 | B | Inhibition of ERK2 kinase | Mus musculus | 1 | single protein format | Scientific Literature | ||
| 2. | ALA732076 | B | Inhibition of mitogen-activated protein kinase 2 | Mus musculus | 3 | single protein format | Scientific Literature | ||
| 3. | ALA732077 | B | Inhibition of mouse Mitogen-activated protein kinase 2 at 10 uM | Mus musculus | 2 | single protein format | Scientific Literature | ||
| 4. | ALA827548 | B | Inhibition of Mitogen-activated protein kinase/extracellular signal-regulated kinase 2 in P19 cells | Mus musculus | 7 | cell-based format | Scientific Literature | ||
| 5. | ALA1952646 | B | Activity at mouse ERK2 receptor at 10 uM | Mus musculus | 1 | single protein format | Scientific Literature | ||
| 6. | ALA898197 | B | Increase in ERK2 phosphorylation in mouse B16 cells at 4-8 hrs | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 7. | ALA939178 | B | Inhibition of IGF1-stimulated purified ERK2 phosphorylation in mouse 3T3 cells | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 8. | ALA939650 | B | Reversal of ERK2 phosphorylation in mouse C2C12 at 20 uM in presence of 50 uM LY-294002 after 48 hrs | Mus musculus | 1 | single protein format | Scientific Literature | ||
| 9. | ALA950815 | B | Inhibition of mouse MAPK2 at 10 uM | Mus musculus | 1 | single protein format | Scientific Literature | ||
| 10. | ALA1026918 | B | Inhibition of GST-fused mouse MAPK2 expressed in Escherichia coli at 10 uM | Mus musculus | 1 | assay format | Scientific Literature | ||
| 11. | ALA1646188 | B | Inhibition of mouse MAPK2 at 10 uM after 60 mins by TR-FRET assay | Mus musculus | 1 | single protein format | Scientific Literature | ||
| 12. | ALA2345863 | B | Activation of ERK2 in mouse RAW264.7 cells assessed as phosphorylation at Thr185/Tyr187 at 50 uM after 30 mins by Western blotting analysis | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 13. | ALA2410778 | B | Inhibition of mouse ERK2 pre-incubation for 15 mins before substrate addition measured after 60 mins by IMAP-FP assay | Mus musculus | 3 | single protein format | Scientific Literature | ||
| 14. | ALA3591270 | B | Binding affinity to ERK2 in mouse fibroblasts assessed as half-life | Mus musculus | 1 | single protein format | Scientific Literature | ||
| 15. | ALA3705054 | B | IMAP Assay: Activated ERK2 activity was determined in the IMAP assay format. | Mus musculus | 14 | single protein format | BindingDB Database | ||
| 16. | ALA3706036 | B | IMAP-FP Assay: Activated ERK2 activity was determined in an IMAP-FP assay (Molecular Devices). Using this assay format, the potency (IC50) of each compound was determined from a 10 point (1:3 serial dilution, 3 uM starting compound concentration) titration curve using the following outlined procedure. To each well of a black Corning 384-well plate (Corning Catalog #3575), 7.5 mL of compound (3333 fold dilution in final assay volume of 25 uL) was dispensed, followed by the addition of 15 uL of kinase buffer (tween containing kinase buffer, Molecular Devices) containing 0.0133 ng/mL (0.316 nM) of phosphorylated active mERK2 enzyme. Following a 15 minute compound & enzyme incubation, each reaction was initiated by the addition of 10 uL kinase buffer containing 2.45 uM ERK2 IMAP substrate peptides (2.25 uM-unlabeled IPTTPITTTYFFFK-COOH and 200 nM-labeled IPTTPITTTYFFFK-5FAM (5-carboxyfluorescein)-COOH), and 75 uM ATP. | Mus musculus | 24 | single protein format | BindingDB Database | ||
| 17. | ALA3706286 | B | Fluorescence Quenching Assay: CADD and biological testing to identify compounds that interact with novel ERK substrate docking sites. The known ERK2 docking sites include the DRS (site 1) and FRS (site 5) regions, whereas predicted docking sites are labeled sites 2-4 (Table 6). One compound, 76, that targets the DRS is being marketed by Calbiochem/EMD Biosciences (Cat#328006) as an ERK inhibitor. Successful inhibitor identification to date has been based on a combination of fluorescence quenching (FQ) of ERK2 wild type and docking site mutants in the presence of test compound. | Mus musculus | 8 | single protein format | BindingDB Database | ||
| 18. | ALA3705760 | B | Coupled ERK2 (cERK) Assay: Activity of compounds against inactive ERK2 was tested in a coupled MEK1/ERK2 IMAP assay as follows: Compounds were diluted to 25x final test concentration in 100% DMSO. 14 ul of kinase buffer (10 mM Tris.HCl pH 7.2, 10 mM MgCl2, 0.01% Tween-20, 1 mM DTT) containing 0.4 ng unphosphorylated Mouse ERK2 protein was added to each well of a black 384-well assay plate. 1 ul of 25x compound was added to each well and incubated at room temperature for 30 minutes to allow an opportunity for the compound to bind to the inactive enzyme. DMSO concentration during initial incubation is 6.7%. ERK2 activity was determined to be insensitive to DMSO concentrations up to 20%. ERK2 was then activated and it's kinase activity measured by the addition of 10 ul kinase buffer with the following components (final concentration per reaction): 2 ng active (phosphorylated) human MEK1 protein and 4 uM (total) ERK2 IMAP substrate peptides. | Mus musculus | 16 | single protein format | BindingDB Database | ||
| 19. | ALA3705761 | B | IMAP-FP Assay: Condition 2: Activated ERK2 activity was determined in an IMAP-FP assay (Molecular Devices). Using this assay format, the potency (IC50) of each compound was determined from a 10 point (1:3 serial dilution, 3 uM starting compound concentration) titration curve using the following outlined procedure. 7.5 mL of compound (3333 fold dilution in final assay volume of 25 uL) was added to 15 uL of kinase buffer containing 0.0133 ng/mL (0.316 nM) of fully phosphorylated, mouse aERK2 enzyme. Following a 15 minute incubation, each reaction was initiated by the addition of 10 uL kinase buffer containing 2.45 uM ERK2 IMAP substrate peptides (2.25 uM-unlabeled IPTTPITTTYFFFK-COOH and 200 nM-labeled IPTTPITTTYFFFK-5FAM (5-carboxyfluorescein)-COOH), and 75 uM ATP. The final reaction in each well of 25 uL consists of 0.19 nM mouse ERK2, 900 nM unlabeled peptide, 80 nM labeled-peptide, and 30 uM ATP. Phosphorylation reactions were allowed to proceed for 40-45 minutes. | Mus musculus | 31 | single protein format | BindingDB Database | ||
| 20. | ALA3705762 | B | IMAP Assay : Condition 1: Activated ERK2 activity was also determined in the IMAP assay format using the procedure outlined above. 1 μl of 25× compound was added to 140 of kinase buffer containing 0.25 ng fully phosphorylated, active Mouse ERK2 protein. Following a 30 minute incubation, the reactions were initiated by addition of 10 μl of kinase buffer containing 1 μM ERK2 IMAP substrate peptide (0.9 μM unlabeled IPTTPITTTYFFFK-CONH2 and 100 nM IPTTPITTTYFFFK(5-carboxyfluorescein)-CONH2) and 30 μM ATP. Reactions proceeded for 30 minutes before termination by addition of 60 μl IMAP detection beads in binding buffer. Plates were read as above after 30 minute binding equilibration. Active compounds were reconfirmed in an independent assay. | Mus musculus | 280 | single protein format | BindingDB Database |
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