Assay Detail
Binding
CHEMBL3862754
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate
30
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.47 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3944427 | — | — | 1 | 8.72 |
| CHEMBL3941804 | — | — | 1 | 8.69 |
| CHEMBL2105762 | OMARIGLIPTIN | 4.0 | 1 | 8.65 |
| CHEMBL3979508 | — | — | 1 | 8.29 |
| CHEMBL3932825 | — | — | 2 | 8.24 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 8.21 |
| CHEMBL3942843 | — | — | 1 | 8.21 |
| CHEMBL3920234 | — | — | 1 | 8.07 |
| CHEMBL3959221 | — | — | 2 | 8.05 |
| CHEMBL3910262 | — | — | 1 | 7.84 |
| CHEMBL3928073 | — | — | 2 | 7.83 |
| CHEMBL3950517 | — | — | 1 | 7.75 |
| CHEMBL3901191 | — | — | 1 | 7.71 |
| CHEMBL3934008 | — | — | 1 | 7.49 |
| CHEMBL3892233 | — | — | 1 | 7.41 |
| CHEMBL3929146 | — | — | 2 | 7.30 |
| CHEMBL3890161 | — | — | 1 | 7.15 |
| CHEMBL3952691 | — | — | 1 | 7.11 |
| CHEMBL3926320 | — | — | 1 | 6.96 |
| CHEMBL3892398 | — | — | 1 | 6.92 |
| CHEMBL3959577 | — | — | 1 | 6.78 |
| CHEMBL3942715 | — | — | 1 | 6.69 |
| CHEMBL3919178 | — | — | 1 | 6.67 |
| CHEMBL3972474 | — | — | 1 | 6.47 |
| CHEMBL3981442 | — | — | 1 | 6.25 |
| CHEMBL3955701 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3944427 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3941804 | — | IC50 | = | 2.06 | nM | 8.69 |
| CHEMBL2105762 | OMARIGLIPTIN | IC50 | = | 2.22 | nM | 8.65 |
| CHEMBL3979508 | — | IC50 | = | 5.17 | nM | 8.29 |
| CHEMBL3932825 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 6.24 | nM | 8.21 |
| CHEMBL3942843 | — | IC50 | = | 6.13 | nM | 8.21 |
| CHEMBL3920234 | — | IC50 | = | 8.42 | nM | 8.07 |
| CHEMBL3959221 | — | IC50 | = | 8.91 | nM | 8.05 |
| CHEMBL3932825 | — | IC50 | = | 10.71 | nM | 7.97 |
| CHEMBL3959221 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL3910262 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL3928073 | — | IC50 | = | 14.95 | nM | 7.83 |
| CHEMBL3950517 | — | IC50 | = | 17.65 | nM | 7.75 |
| CHEMBL3901191 | — | IC50 | = | 19.64 | nM | 7.71 |
| CHEMBL3934008 | — | IC50 | = | 32.64 | nM | 7.49 |
| CHEMBL3892233 | — | IC50 | = | 39.2 | nM | 7.41 |
| CHEMBL3929146 | — | IC50 | = | 49.73 | nM | 7.30 |
| CHEMBL3928073 | — | IC50 | = | 60.61 | nM | 7.22 |
| CHEMBL3890161 | — | IC50 | = | 70.42 | nM | 7.15 |
| CHEMBL3952691 | — | IC50 | = | 78.33 | nM | 7.11 |
| CHEMBL3926320 | — | IC50 | = | 110.1 | nM | 6.96 |
| CHEMBL3892398 | — | IC50 | = | 121.56 | nM | 6.92 |
| CHEMBL3959577 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3942715 | — | IC50 | = | 205.2 | nM | 6.69 |
| CHEMBL3919178 | — | IC50 | = | 216.2 | nM | 6.67 |
| CHEMBL3972474 | — | IC50 | = | 337.8 | nM | 6.47 |
| CHEMBL3981442 | — | IC50 | = | 563.9 | nM | 6.25 |
| CHEMBL3929146 | — | IC50 | = | 813.44 | nM | 6.09 |
| CHEMBL3955701 | — | IC50 | = | 2930.0 | nM | 5.53 |