Assay Detail
Binding
CHEMBL3583540
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Binding affinity to biotinylated human recombinant glucokinase expressed in Escherichia coli assessed as dissociation rate constant by SPR method
17
Total Activities
16
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
Optimizing glucokinase activator binding kinetics to lower in vivo hypoglycemia risk
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 17 | 7.35 | 8.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3217925 | — | — | 1 | 8.67 |
| CHEMBL3580738 | — | — | 2 | 8.62 |
| CHEMBL3580737 | MK-0941 FREE BASE | 2.0 | 1 | 8.53 |
| CHEMBL3219124 | AZD-1656 | 2.0 | 1 | 7.97 |
| CHEMBL3580740 | — | — | 1 | 7.76 |
| CHEMBL3580742 | — | — | 1 | 7.67 |
| CHEMBL499520 | — | — | 1 | 7.59 |
| CHEMBL3580739 | — | — | 1 | 7.06 |
| CHEMBL3218477 | — | — | 1 | 7.05 |
| CHEMBL2204663 | — | — | 1 | 6.94 |
| CHEMBL3580741 | — | — | 1 | 6.85 |
| CHEMBL608393 | — | — | 1 | 6.78 |
| CHEMBL2165616 | — | — | 1 | 6.76 |
| CHEMBL2165615 | NERIGLIATIN | 2.0 | 1 | 6.72 |
| CHEMBL1783734 | PIRAGLIATIN | 2.0 | 1 | 6.66 |
| CHEMBL2204655 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3217925 | — | Kd | = | 2.16 | nM | 8.67 |
| CHEMBL3580738 | — | Kd | = | 2.42 | nM | 8.62 |
| CHEMBL3580737 | MK-0941 FREE BASE | Kd | = | 2.93 | nM | 8.53 |
| CHEMBL3219124 | AZD-1656 | Kd | = | 10.8 | nM | 7.97 |
| CHEMBL3580740 | — | Kd | = | 17.5 | nM | 7.76 |
| CHEMBL3580742 | — | Kd | = | 21.4 | nM | 7.67 |
| CHEMBL499520 | — | Kd | = | 25.6 | nM | 7.59 |
| CHEMBL3580739 | — | Kd | = | 86.4 | nM | 7.06 |
| CHEMBL3218477 | — | Kd | = | 89.9 | nM | 7.05 |
| CHEMBL3580738 | — | Kd | = | 96.8 | nM | 7.01 |
| CHEMBL2204663 | — | Kd | = | 114.1 | nM | 6.94 |
| CHEMBL3580741 | — | Kd | = | 141.5 | nM | 6.85 |
| CHEMBL608393 | — | Kd | = | 164.9 | nM | 6.78 |
| CHEMBL2165616 | — | Kd | = | 174.8 | nM | 6.76 |
| CHEMBL2165615 | NERIGLIATIN | Kd | = | 189.2 | nM | 6.72 |
| CHEMBL1783734 | PIRAGLIATIN | Kd | = | 218.4 | nM | 6.66 |
| CHEMBL2204655 | — | Kd | = | 427.3 | nM | 6.37 |