Assay Detail
Binding
CHEMBL4879707
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KinomeScan assay: inhibition of ERK8
109
Total Activities
108
Compounds Tested
2
Activity Types
4
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
SGC KinomeScan assays
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| % Control | 108 | - | - |
| Kd | 1 | 7.52 | 7.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Amino acid Start/Stop | Amino acid Start/Stop | - | — | M1/P437 |
| Expression system | Expression system | - | — | bacterial |
| Kinase construct length | Kinase construct length | - | — | Partial Length |
| Kinase form | Kinase form | - | — | Wild Type |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4538174 | ERKi | — | 2 | 7.52 |
| CHEMBL4539943 | BAY-694 | — | 1 | - |
| CHEMBL4535474 | BAY-293 | — | 1 | - |
| CHEMBL3617968 | BAY-678 | — | 1 | - |
| CHEMBL4526351 | BAY-309 | — | 1 | - |
| CHEMBL3907057 | BAY-826 | — | 1 | - |
| CHEMBL4630643 | BAY-448 | — | 1 | - |
| CHEMBL4630644 | BAY-386 | — | 1 | - |
| CHEMBL4455582 | BAY-693 | — | 1 | - |
| CHEMBL4445670 | BAY-885 | — | 1 | - |
| CHEMBL4552180 | BAY-588 | — | 1 | - |
| CHEMBL4448899 | BAY-876 | — | 1 | - |
| CHEMBL4564312 | BAY-786 | — | 1 | - |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4516843 | BAY-207 | — | 1 | - |
| CHEMBL4521594 | BAY-1797 | — | 1 | - |
| CHEMBL4585243 | BAY-7598 | — | 1 | - |
| CHEMBL4522773 | BAY-827 | — | 1 | - |
| CHEMBL4066040 | A-1596584 | — | 1 | - |
| CHEMBL4093612 | A-1596586 | — | 1 | - |
| CHEMBL4533479 | A-1806262 | — | 1 | - |
| CHEMBL332794 | A-192621 | — | 1 | - |
| CHEMBL4630641 | A-769 | — | 1 | - |
| CHEMBL440687 | ABT-724 | — | 1 | - |
| CHEMBL4513786 | A-545 | — | 1 | - |
| CHEMBL111612 | ABT-546 | — | 1 | - |
| CHEMBL4526341 | A-108 | — | 1 | - |
| CHEMBL4586794 | ABT-100 | — | 1 | - |
| CHEMBL3701197 | A-226 | — | 1 | - |
| CHEMBL3697701 | A-079 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4538174 | ERKi | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL1800285 | MSD-M1PAM | % Control | = | 100.0 | % | - |
| CHEMBL4228713 | A-1211212 | % Control | = | 85.0 | % | - |
| CHEMBL4551344 | A-1210227 | % Control | = | 94.0 | % | - |
| CHEMBL4063249 | TP-021n | % Control | = | 100.0 | % | - |
| CHEMBL4584981 | NVS-MALT1-C | % Control | = | 81.0 | % | - |
| CHEMBL4568735 | NVS-MALT1 | % Control | = | 87.0 | % | - |
| CHEMBL4518706 | PF-00911705 | % Control | = | 4.8 | % | - |
| CHEMBL3137331 | DEFACTINIB | % Control | = | 40.0 | % | - |
| CHEMBL4577237 | BI 9446 | % Control | = | 100.0 | % | - |
| CHEMBL4530740 | BI 1950 | % Control | = | 100.0 | % | - |
| CHEMBL3286797 | PF-04418948 | % Control | = | 74.0 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | % Control | = | 92.0 | % | - |
| CHEMBL4100408 | TP-024n | % Control | = | 100.0 | % | - |
| CHEMBL4536197 | A-486 | % Control | = | 93.0 | % | - |
| CHEMBL4282264 | A-485 | % Control | = | 74.0 | % | - |
| CHEMBL4561806 | BTZO-4 | % Control | = | 100.0 | % | - |
| CHEMBL4516611 | BTZO-1 | % Control | = | 100.0 | % | - |
| CHEMBL4538591 | BAY-440 | % Control | = | 73.0 | % | - |
| CHEMBL3589752 | IPP/CNRS-A017 | % Control | = | 93.0 | % | - |
| CHEMBL4436748 | SR-318 | % Control | = | 100.0 | % | - |
| CHEMBL4531775 | SR-321 | % Control | = | 100.0 | % | - |
| CHEMBL4458424 | BAY-899 | % Control | = | 93.0 | % | - |
| CHEMBL4592872 | BAY-897 | % Control | = | 94.0 | % | - |
| CHEMBL4537673 | BAY-985 | % Control | = | 100.0 | % | - |
| CHEMBL4591082 | SR-302 | % Control | = | 100.0 | % | - |
| CHEMBL4518342 | THPP-1-NC | % Control | = | 100.0 | % | - |
| CHEMBL3342332 | A-1155463 | % Control | = | 100.0 | % | - |
| CHEMBL1091513 | MRK-560 | % Control | = | 94.0 | % | - |
| CHEMBL3609749 | — | % Control | = | 78.0 | % | - |
| CHEMBL4752561 | — | % Control | = | 100.0 | % | - |
| CHEMBL561132 | MK-7246 | % Control | = | 100.0 | % | - |
| CHEMBL1643772 | CRTH2-negative-control | % Control | = | 100.0 | % | - |
| CHEMBL4098877 | MLi-2 | % Control | = | 81.0 | % | - |
| CHEMBL4560589 | MLi-2-NC | % Control | = | 72.0 | % | - |
| CHEMBL1800685 | PPTN | % Control | = | 100.0 | % | - |
| CHEMBL4566600 | PPTN-NC | % Control | = | 100.0 | % | - |
| CHEMBL2204538 | THPP-1 | % Control | = | 100.0 | % | - |
| CHEMBL4082756 | TP-024 | % Control | = | 95.0 | % | - |
| CHEMBL3582478 | MSD-CYP11B2 | % Control | = | 90.0 | % | - |
| CHEMBL3582461 | MSD-CYP11B2-Negative-control | % Control | = | 100.0 | % | - |
| CHEMBL3577885 | PF-05105679 | % Control | = | 93.0 | % | - |
| CHEMBL1651534 | REDAFAMDASTAT | % Control | = | 83.0 | % | - |
| CHEMBL4780458 | — | % Control | = | 100.0 | % | - |
| CHEMBL3337894 | T-26c | % Control | = | 82.4 | % | - |
| CHEMBL3799292 | (R)-9s | % Control | = | 100.0 | % | - |
| CHEMBL3797887 | (S)-9s | % Control | = | 100.0 | % | - |
| CHEMBL4455357 | TP-020 | % Control | = | 78.0 | % | - |
| CHEMBL4585920 | TP-020n | % Control | = | 84.0 | % | - |
| CHEMBL3799512 | TP-004 | % Control | = | 86.0 | % | - |