Assay Detail
Binding
CHEMBL1057686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human glutaminyl cyclase expressed in Pichia pastoris by pGAP coupled enzyme assay
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Inhibitors for human glutaminyl cyclase by structure based design and bioisosteric replacement.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 47 | 6.65 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL583368 | — | — | 1 | 8.59 |
| CHEMBL566563 | — | — | 1 | 8.20 |
| CHEMBL574500 | — | — | 1 | 7.77 |
| CHEMBL567646 | — | — | 1 | 7.75 |
| CHEMBL565265 | — | — | 1 | 7.70 |
| CHEMBL578153 | — | — | 1 | 7.47 |
| CHEMBL567842 | — | — | 1 | 7.41 |
| CHEMBL578798 | — | — | 1 | 7.39 |
| CHEMBL565907 | — | — | 1 | 7.38 |
| CHEMBL574357 | — | — | 1 | 7.36 |
| CHEMBL567406 | — | — | 1 | 7.29 |
| CHEMBL201747 | — | — | 1 | 7.22 |
| CHEMBL565917 | — | — | 1 | 7.22 |
| CHEMBL567221 | — | — | 1 | 7.21 |
| CHEMBL566321 | — | — | 1 | 7.19 |
| CHEMBL565908 | — | — | 1 | 7.17 |
| CHEMBL567407 | — | — | 1 | 7.09 |
| CHEMBL578632 | — | — | 1 | 7.08 |
| CHEMBL203195 | — | — | 1 | 7.05 |
| CHEMBL574356 | — | — | 1 | 6.89 |
| CHEMBL577061 | — | — | 1 | 6.64 |
| CHEMBL566320 | — | — | 1 | 6.60 |
| CHEMBL565704 | — | — | 1 | 6.52 |
| CHEMBL578765 | — | — | 1 | 6.47 |
| CHEMBL565694 | — | — | 1 | 6.44 |
| CHEMBL577493 | — | — | 1 | 6.30 |
| CHEMBL565480 | — | — | 1 | 6.28 |
| CHEMBL565479 | — | — | 1 | 6.27 |
| CHEMBL565492 | — | — | 1 | 6.27 |
| CHEMBL567415 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL583368 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL566563 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL574500 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL567646 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL565265 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL578153 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL567842 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL578798 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL565907 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL574357 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL567406 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL201747 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL565917 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL567221 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL566321 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL565908 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL567407 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL578632 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL203195 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL574356 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL577061 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL566320 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL565704 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL578765 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL565694 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL577493 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL565480 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL565479 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL565492 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL567415 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL565695 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL582920 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL567615 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL579184 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL565716 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL574137 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL577246 | — | Ki | = | 1030.0 | nM | 5.99 |
| CHEMBL577059 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL578366 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL573684 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL568073 | — | Ki | = | 1290.0 | nM | 5.89 |
| CHEMBL577287 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL578155 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL584587 | — | Ki | = | 1530.0 | nM | 5.82 |
| CHEMBL568072 | — | Ki | = | 1650.0 | nM | 5.78 |
| CHEMBL566549 | — | Ki | = | 6720.0 | nM | 5.17 |
| CHEMBL573682 | — | Ki | = | 20550.0 | nM | 4.69 |