Assay Detail
Binding
CHEMBL4332025
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged MAP2K5 activated N-terminal GST-tagged recombinant human ERK5 (1 to 398 residues) expressed in Escherichia coli using biotin-Ahx-PPGDYSTTPGGTLFSTTPGGTRI peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by TR-FRET assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.26 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438379 | — | — | 1 | 7.77 |
| CHEMBL4541479 | — | — | 1 | 7.70 |
| CHEMBL4445670 | BAY-885 | — | 1 | 7.46 |
| CHEMBL4469661 | — | — | 1 | 7.29 |
| CHEMBL4550589 | — | — | 1 | 7.27 |
| CHEMBL4542723 | — | — | 1 | 7.19 |
| CHEMBL4526317 | — | — | 1 | 7.17 |
| CHEMBL4441182 | — | — | 1 | 7.01 |
| CHEMBL4450479 | — | — | 1 | 6.96 |
| CHEMBL4450712 | — | — | 1 | 6.82 |
| CHEMBL4544067 | — | — | 1 | 6.77 |
| CHEMBL1673046 | — | — | 1 | 6.70 |
| CHEMBL4582824 | — | — | 1 | 6.68 |
| CHEMBL4535758 | — | — | 1 | 6.57 |
| CHEMBL4446192 | — | — | 1 | 6.46 |
| CHEMBL4466294 | — | — | 1 | 6.42 |
| CHEMBL4565352 | — | — | 1 | 6.28 |
| CHEMBL4520598 | — | — | 1 | 6.12 |
| CHEMBL4545407 | — | — | 1 | 6.04 |
| CHEMBL4468045 | — | — | 1 | 6.00 |
| CHEMBL4468249 | — | — | 1 | 5.95 |
| CHEMBL4515161 | — | — | 1 | 5.79 |
| CHEMBL4455302 | — | — | 1 | 5.78 |
| CHEMBL4550759 | — | — | 1 | 5.66 |
| CHEMBL4563747 | — | — | 1 | 5.56 |
| CHEMBL4450762 | — | — | 1 | 5.41 |
| CHEMBL4573138 | — | — | 1 | 5.39 |
| CHEMBL4455582 | BAY-693 | — | 1 | 5.19 |
| CHEMBL4465121 | — | — | 1 | 5.17 |
| CHEMBL4584254 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438379 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4541479 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4445670 | BAY-885 | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4469661 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4550589 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4542723 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4526317 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4441182 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4450479 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4450712 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4544067 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1673046 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4582824 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4535758 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4446192 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4466294 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4565352 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4520598 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4545407 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4468045 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4468249 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL4515161 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL4455302 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4550759 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL4563747 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL4450762 | — | IC50 | = | 3890.0 | nM | 5.41 |
| CHEMBL4573138 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4455582 | BAY-693 | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4465121 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4584254 | — | IC50 | = | 7090.0 | nM | 5.15 |
| CHEMBL4437100 | — | IC50 | = | 9740.0 | nM | 5.01 |
| CHEMBL4470337 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4459339 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4445067 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4468512 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4445175 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4471256 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4582719 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4569173 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4587463 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4447683 | — | IC50 | > | 20000.0 | nM | - |