Assay Detail
Binding
CHEMBL3240701
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Inhibition of biotin-tagged human GKRP/fluorescein-tagged GK interaction preincubated for 20 mins prior to GK addition measured after 2 to 4 hrs by AlphaScreen assay
40
Total Activities
40
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: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.12 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3114185 | — | — | 1 | 8.40 |
| CHEMBL3237987 | — | — | 1 | 8.30 |
| CHEMBL3237986 | — | — | 1 | 8.22 |
| CHEMBL3237981 | — | — | 1 | 8.22 |
| CHEMBL3114187 | — | — | 1 | 8.05 |
| CHEMBL3238310 | — | — | 1 | 8.00 |
| CHEMBL3238309 | — | — | 1 | 8.00 |
| CHEMBL3238313 | — | — | 1 | 7.89 |
| CHEMBL3238308 | — | — | 1 | 7.89 |
| CHEMBL3238307 | — | — | 1 | 7.89 |
| CHEMBL3237985 | — | — | 1 | 7.80 |
| CHEMBL3238303 | — | — | 1 | 7.77 |
| CHEMBL3238306 | — | — | 1 | 7.75 |
| CHEMBL3238312 | — | — | 1 | 7.62 |
| CHEMBL3237980 | — | — | 1 | 7.55 |
| CHEMBL3237984 | — | — | 1 | 7.55 |
| CHEMBL3237993 | — | — | 1 | 7.46 |
| CHEMBL3238301 | — | — | 1 | 7.35 |
| CHEMBL3237983 | — | — | 1 | 7.33 |
| CHEMBL3238316 | — | — | 1 | 7.31 |
| CHEMBL3237992 | — | — | 1 | 7.21 |
| CHEMBL3238311 | — | — | 1 | 7.17 |
| CHEMBL3238314 | — | — | 1 | 7.16 |
| CHEMBL3238305 | — | — | 1 | 7.16 |
| CHEMBL3238315 | — | — | 1 | 7.09 |
| CHEMBL3237994 | — | — | 1 | 7.00 |
| CHEMBL3238302 | — | — | 1 | 6.74 |
| CHEMBL3238296 | — | — | 1 | 6.63 |
| CHEMBL3238300 | — | — | 1 | 6.59 |
| CHEMBL3238304 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3114185 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3237987 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3237981 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3237986 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3114187 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3238310 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3238309 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3238313 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3238308 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3238307 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3237985 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3238303 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3238306 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3238312 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3237984 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3237980 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3237993 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3238301 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3237983 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3238316 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3237992 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3238311 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3238314 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3238305 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3238315 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3237994 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL3238302 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL3238296 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL3238300 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL3238304 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL3238299 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3238297 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3237982 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL3237991 | — | IC50 | = | 401.0 | nM | 6.40 |
| CHEMBL3237979 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3237988 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL3238298 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3237989 | — | IC50 | = | 3070.0 | nM | 5.51 |
| CHEMBL3237990 | — | IC50 | = | 3360.0 | nM | 5.47 |
| CHEMBL3237978 | — | IC50 | = | 25000.0 | nM | 4.60 |