Assay Detail
Binding
CHEMBL3364949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP compound incubated for 20 mins prior to addition of fluorescein-labeled GK measured after 2 to 4 hrs by AlphaScreen assay
45
Total Activities
45
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
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 7.45 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3319533 | — | — | 1 | 9.00 |
| CHEMBL3319534 | — | — | 1 | 8.30 |
| CHEMBL3319529 | — | — | 1 | 8.30 |
| CHEMBL3319540 | — | — | 1 | 8.30 |
| CHEMBL3319549 | — | — | 1 | 8.30 |
| CHEMBL3319544 | — | — | 1 | 8.22 |
| CHEMBL3319541 | — | — | 1 | 8.15 |
| CHEMBL3319542 | — | — | 1 | 8.15 |
| CHEMBL3319543 | — | — | 1 | 8.10 |
| CHEMBL3317472 | — | — | 1 | 7.96 |
| CHEMBL3319551 | — | — | 1 | 7.96 |
| CHEMBL3319528 | — | — | 1 | 7.85 |
| CHEMBL3319559 | — | — | 1 | 7.82 |
| CHEMBL3319554 | — | — | 1 | 7.80 |
| CHEMBL3319555 | — | — | 1 | 7.77 |
| CHEMBL3319531 | — | — | 1 | 7.77 |
| CHEMBL3319539 | — | — | 1 | 7.72 |
| CHEMBL3319560 | — | — | 1 | 7.70 |
| CHEMBL3319558 | — | — | 1 | 7.70 |
| CHEMBL3319548 | — | — | 1 | 7.68 |
| CHEMBL3319535 | — | — | 1 | 7.64 |
| CHEMBL3319550 | — | — | 1 | 7.62 |
| CHEMBL3319564 | — | — | 1 | 7.57 |
| CHEMBL3319552 | — | — | 1 | 7.54 |
| CHEMBL3319561 | — | — | 1 | 7.48 |
| CHEMBL3319527 | — | — | 1 | 7.48 |
| CHEMBL3319557 | — | — | 1 | 7.46 |
| CHEMBL3319553 | — | — | 1 | 7.40 |
| CHEMBL3319537 | — | — | 1 | 7.40 |
| CHEMBL3319547 | — | — | 1 | 7.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3319533 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3319534 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3319549 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3319529 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3319540 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3319544 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3319541 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3319542 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3319543 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3317472 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3319551 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3319528 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3319559 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3319554 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3319531 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3319555 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3319539 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3319560 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3319558 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3319548 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3319535 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3319550 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3319564 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3319552 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3319561 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3319527 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3319557 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3319553 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3319537 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3319547 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3319556 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3319565 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3319530 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3319546 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3319562 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3319536 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3319524 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3319522 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL3319532 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL3319523 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL3319545 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL3319526 | — | IC50 | = | 601.0 | nM | 6.22 |
| CHEMBL3319525 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL3319563 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL3319538 | — | IC50 | = | 30000.0 | nM | 4.52 |