Assay Detail
Binding
CHEMBL3880356
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of kinase tracer-236 binding to full length recombinant human His-tagged TAK1-TAB1 expressed in baculovirus by FRET assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
4-alkoxy/aralkoxy-5-substituted-pyrrolopyrimidine compounds as TAK1 inhibitors in disease treatment
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.90 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3953067 | — | — | 1 | 8.51 |
| CHEMBL3916326 | — | — | 1 | 8.37 |
| CHEMBL3924740 | — | — | 1 | 8.36 |
| CHEMBL3919781 | — | — | 1 | 8.28 |
| CHEMBL3917140 | — | — | 1 | 8.15 |
| CHEMBL3898170 | — | — | 1 | 7.89 |
| CHEMBL3912681 | — | — | 1 | 7.80 |
| CHEMBL3905384 | — | — | 1 | 7.72 |
| CHEMBL3901893 | — | — | 1 | 7.48 |
| CHEMBL3918925 | — | — | 1 | 7.39 |
| CHEMBL3969384 | — | — | 1 | 7.29 |
| CHEMBL3895287 | — | — | 1 | 7.12 |
| CHEMBL3919897 | — | — | 1 | 7.01 |
| CHEMBL3963009 | — | — | 1 | 7.00 |
| CHEMBL3894718 | — | — | 1 | 6.77 |
| CHEMBL3902720 | — | — | 1 | 6.77 |
| CHEMBL3934288 | — | — | 1 | 6.75 |
| CHEMBL3922526 | — | — | 1 | 6.70 |
| CHEMBL3893882 | — | — | 1 | 6.70 |
| CHEMBL3897406 | — | — | 1 | 6.68 |
| CHEMBL3905341 | — | — | 1 | 6.55 |
| CHEMBL3909192 | — | — | 1 | 6.48 |
| CHEMBL3919844 | — | — | 1 | 6.47 |
| CHEMBL3975493 | — | — | 1 | 6.47 |
| CHEMBL3895447 | — | — | 1 | 6.46 |
| CHEMBL3973552 | — | — | 1 | 6.44 |
| CHEMBL3929132 | — | — | 1 | 6.42 |
| CHEMBL3912629 | — | — | 1 | 6.38 |
| CHEMBL3925269 | — | — | 1 | 6.37 |
| CHEMBL3901362 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3953067 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3916326 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3924740 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3919781 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3917140 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3898170 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3912681 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3905384 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3901893 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3918925 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3969384 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3895287 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3919897 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3963009 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3902720 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3894718 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3934288 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3893882 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3922526 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3897406 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3905341 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3909192 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3919844 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3975493 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3895447 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3973552 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3929132 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3912629 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3925269 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3901362 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3891089 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3907201 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3897133 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3945840 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3904280 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3901598 | — | IC50 | = | 2500.0 | nM | 5.60 |