Assay Detail
Binding
CHEMBL3706036
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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.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Compounds that are ERK inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.71 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3703711 | — | — | 1 | 9.82 |
| CHEMBL2408789 | — | — | 1 | 9.82 |
| CHEMBL2408790 | — | — | 1 | 9.82 |
| CHEMBL3703710 | — | — | 1 | 9.67 |
| CHEMBL2408788 | — | — | 1 | 9.65 |
| CHEMBL3654670 | — | — | 1 | 9.53 |
| CHEMBL3654677 | — | — | 1 | 9.34 |
| CHEMBL3703707 | — | — | 1 | 9.30 |
| CHEMBL3703709 | — | — | 1 | 9.29 |
| CHEMBL3654671 | — | — | 1 | 9.27 |
| CHEMBL3654673 | — | — | 1 | 9.04 |
| CHEMBL3703706 | — | — | 1 | 8.95 |
| CHEMBL3703714 | — | — | 1 | 8.94 |
| CHEMBL3654672 | — | — | 1 | 8.65 |
| CHEMBL3654674 | — | — | 1 | 8.65 |
| CHEMBL3703704 | — | — | 1 | 8.50 |
| CHEMBL3703712 | — | — | 1 | 8.43 |
| CHEMBL3654667 | — | — | 1 | 8.42 |
| CHEMBL3654669 | — | — | 1 | 8.02 |
| CHEMBL3703713 | — | — | 1 | 7.99 |
| CHEMBL3703705 | — | — | 1 | 7.44 |
| CHEMBL3703708 | — | — | 1 | 7.42 |
| CHEMBL3654668 | — | — | 1 | 6.97 |
| CHEMBL3654675 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3703711 | — | IC50 | = | 0.1524 | nM | 9.82 |
| CHEMBL2408789 | — | IC50 | = | 0.1524 | nM | 9.82 |
| CHEMBL2408790 | — | IC50 | = | 0.1524 | nM | 9.82 |
| CHEMBL3703710 | — | IC50 | = | 0.2153 | nM | 9.67 |
| CHEMBL2408788 | — | IC50 | = | 0.2223 | nM | 9.65 |
| CHEMBL3654670 | — | IC50 | = | 0.296 | nM | 9.53 |
| CHEMBL3654677 | — | IC50 | = | 0.4572 | nM | 9.34 |
| CHEMBL3703707 | — | IC50 | = | 0.5018 | nM | 9.30 |
| CHEMBL3703709 | — | IC50 | = | 0.5162 | nM | 9.29 |
| CHEMBL3654671 | — | IC50 | = | 0.5369 | nM | 9.27 |
| CHEMBL3654673 | — | IC50 | = | 0.9192 | nM | 9.04 |
| CHEMBL3703706 | — | IC50 | = | 1.119 | nM | 8.95 |
| CHEMBL3703714 | — | IC50 | = | 1.161 | nM | 8.94 |
| CHEMBL3654672 | — | IC50 | = | 2.232 | nM | 8.65 |
| CHEMBL3654674 | — | IC50 | = | 2.223 | nM | 8.65 |
| CHEMBL3703704 | — | IC50 | = | 3.13 | nM | 8.50 |
| CHEMBL3703712 | — | IC50 | = | 3.724 | nM | 8.43 |
| CHEMBL3654667 | — | IC50 | = | 3.779 | nM | 8.42 |
| CHEMBL3654669 | — | IC50 | = | 9.462 | nM | 8.02 |
| CHEMBL3703713 | — | IC50 | = | 10.23 | nM | 7.99 |
| CHEMBL3703705 | — | IC50 | = | 36.63 | nM | 7.44 |
| CHEMBL3703708 | — | IC50 | = | 38.29 | nM | 7.42 |
| CHEMBL3654668 | — | IC50 | = | 107.7 | nM | 6.97 |
| CHEMBL3654675 | — | IC50 | = | 682.2 | nM | 6.17 |