Assay Detail
Binding
CHEMBL5734102
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity Assay: The MetAP-2 activity is determined by coupling enzymatic reactions. The tripeptide Met-Arg-Ser (MAS) is employed as substrate. The methionine liberated is firstly converted into Metox and H2O2 by L-aminooxidase (AAO). In the second step, the peroxidase (POD) with the aid of the H2O2 catalyses the oxidation of the leukodye dianisidine to dianisidineox, the increase of which is detected photometrically at 450 nm. MetAP-2 activity can be recorded continuously as kinetics. The reaction scheme illustrates that one mol of dianisidineox is formed per mol of methionene. The MetAP-2 enzyme activity can therefore be calculated directly as �� absorption per time unit. Qualification of the MetAP-2 activity (mol of Met/time unit) is possible with the aid of the dianisidineox extinction coefficient. The change in extinction per time unit is depicted graphically and a slope calculation is carried out in the visually linear region of the reaction.
231
Total Activities
76
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrrolidinone derivatives as MetAP-2 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 77 | 6.63 | 7.47 |
| kon | 77 | - | - |
| k_off | 77 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454587 | — | — | 3 | 7.47 |
| CHEMBL5749151 | — | — | 3 | 7.41 |
| CHEMBL5845917 | — | — | 3 | 7.41 |
| CHEMBL6013768 | — | — | 3 | 7.37 |
| CHEMBL5872836 | — | — | 3 | 7.31 |
| CHEMBL5815694 | — | — | 3 | 7.29 |
| CHEMBL5886068 | — | — | 3 | 7.26 |
| CHEMBL5830907 | — | — | 3 | 7.24 |
| CHEMBL5953520 | — | — | 3 | 7.20 |
| CHEMBL5759390 | — | — | 3 | 7.17 |
| CHEMBL5888387 | — | — | 3 | 7.17 |
| CHEMBL5954083 | — | — | 3 | 7.16 |
| CHEMBL5840048 | — | — | 3 | 7.16 |
| CHEMBL5742773 | — | — | 3 | 7.14 |
| CHEMBL5958560 | — | — | 3 | 7.12 |
| CHEMBL5773159 | — | — | 3 | 7.11 |
| CHEMBL5864968 | — | — | 3 | 7.10 |
| CHEMBL6024899 | — | — | 3 | 7.08 |
| CHEMBL5912883 | — | — | 3 | 7.07 |
| CHEMBL5782131 | — | — | 3 | 7.05 |
| CHEMBL4450159 | — | — | 3 | 7.04 |
| CHEMBL4451402 | — | — | 3 | 7.04 |
| CHEMBL5888265 | — | — | 3 | 7.02 |
| CHEMBL5777206 | — | — | 3 | 7.02 |
| CHEMBL5985680 | — | — | 3 | 7.00 |
| CHEMBL5742381 | — | — | 3 | 7.00 |
| CHEMBL5916901 | — | — | 3 | 6.96 |
| CHEMBL6031329 | — | — | 3 | 6.96 |
| CHEMBL5841215 | — | — | 3 | 6.92 |
| CHEMBL5924033 | — | — | 3 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454587 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5749151 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5845917 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL6013768 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5872836 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5815694 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5886068 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5830907 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5953520 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5759390 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5888387 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5840048 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5954083 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5742773 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5958560 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5773159 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5864968 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL6024899 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL5912883 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5782131 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4450159 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4451402 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5888265 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL5777206 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL5742381 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5985680 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5916901 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL6031329 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5841215 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5864600 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL6006995 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5924033 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5996682 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5760876 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4591797 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL6049299 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5898129 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5910476 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5868187 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5858472 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5870963 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5789981 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5987274 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5837176 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5780452 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5913209 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5776582 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5924493 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5861127 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5877505 | — | IC50 | = | 270.0 | nM | 6.57 |