Assay Detail
Binding
CHEMBL3240702
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GKRP-GK interaction in mouse hepatocytes assessed as induction of GK translocation from nucleus to cytoplasm incubated for 20 mins prior to glucose addition measured after 40 mins
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | Hepatocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 39 | 6.44 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237992 | — | — | 1 | 7.43 |
| CHEMBL3237981 | — | — | 1 | 7.05 |
| CHEMBL3237980 | — | — | 1 | 7.01 |
| CHEMBL3237993 | — | — | 1 | 7.01 |
| CHEMBL3114187 | — | — | 1 | 6.92 |
| CHEMBL3237986 | — | — | 1 | 6.89 |
| CHEMBL3237987 | — | — | 1 | 6.86 |
| CHEMBL3238312 | — | — | 1 | 6.84 |
| CHEMBL3238314 | — | — | 1 | 6.81 |
| CHEMBL3238307 | — | — | 1 | 6.80 |
| CHEMBL3238296 | — | — | 1 | 6.75 |
| CHEMBL3237985 | — | — | 1 | 6.70 |
| CHEMBL3114185 | — | — | 1 | 6.70 |
| CHEMBL3238300 | — | — | 1 | 6.68 |
| CHEMBL3237984 | — | — | 1 | 6.66 |
| CHEMBL3237994 | — | — | 1 | 6.59 |
| CHEMBL3238297 | — | — | 1 | 6.57 |
| CHEMBL3238306 | — | — | 1 | 6.53 |
| CHEMBL3238313 | — | — | 1 | 6.46 |
| CHEMBL3238311 | — | — | 1 | 6.42 |
| CHEMBL3238308 | — | — | 1 | 6.42 |
| CHEMBL3238303 | — | — | 1 | 6.41 |
| CHEMBL3238309 | — | — | 1 | 6.38 |
| CHEMBL3237983 | — | — | 1 | 6.27 |
| CHEMBL3238301 | — | — | 1 | 6.25 |
| CHEMBL3238299 | — | — | 1 | 6.15 |
| CHEMBL3237991 | — | — | 1 | 6.03 |
| CHEMBL3238305 | — | — | 1 | 5.84 |
| CHEMBL3237979 | — | — | 1 | 5.81 |
| CHEMBL3238304 | — | — | 1 | 5.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237992 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3237981 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3237993 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3237980 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3114187 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3237986 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3237987 | — | EC50 | = | 137.0 | nM | 6.86 |
| CHEMBL3238312 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL3238314 | — | EC50 | = | 155.0 | nM | 6.81 |
| CHEMBL3238307 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3238296 | — | EC50 | = | 178.0 | nM | 6.75 |
| CHEMBL3237985 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3114185 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3238300 | — | EC50 | = | 208.0 | nM | 6.68 |
| CHEMBL3237984 | — | EC50 | = | 219.0 | nM | 6.66 |
| CHEMBL3237994 | — | EC50 | = | 254.0 | nM | 6.59 |
| CHEMBL3238297 | — | EC50 | = | 271.0 | nM | 6.57 |
| CHEMBL3238306 | — | EC50 | = | 294.0 | nM | 6.53 |
| CHEMBL3238313 | — | EC50 | = | 349.0 | nM | 6.46 |
| CHEMBL3238311 | — | EC50 | = | 381.0 | nM | 6.42 |
| CHEMBL3238308 | — | EC50 | = | 382.0 | nM | 6.42 |
| CHEMBL3238303 | — | EC50 | = | 388.0 | nM | 6.41 |
| CHEMBL3238309 | — | EC50 | = | 421.0 | nM | 6.38 |
| CHEMBL3237983 | — | EC50 | = | 537.0 | nM | 6.27 |
| CHEMBL3238301 | — | EC50 | = | 567.0 | nM | 6.25 |
| CHEMBL3238299 | — | EC50 | = | 704.0 | nM | 6.15 |
| CHEMBL3237991 | — | EC50 | = | 936.0 | nM | 6.03 |
| CHEMBL3238305 | — | EC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL3237979 | — | EC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL3238304 | — | EC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL3238310 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3238302 | — | EC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL3237989 | — | EC50 | = | 4050.0 | nM | 5.39 |
| CHEMBL3237982 | — | EC50 | = | 5670.0 | nM | 5.25 |
| CHEMBL3238298 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3237990 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3237988 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3238315 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3238316 | — | EC50 | > | 12500.0 | nM | - |