Assay Detail
Binding
CHEMBL826403
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Inhibitory concentration required against Escherichia coli MetAP1 (150 nM)
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Escherichia coli |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.78 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL359683 | — | — | 1 | 7.62 |
| CHEMBL180070 | — | — | 1 | 7.54 |
| CHEMBL360955 | — | — | 1 | 7.40 |
| CHEMBL178815 | — | — | 1 | 7.38 |
| CHEMBL359851 | — | — | 1 | 7.36 |
| CHEMBL367801 | — | — | 1 | 7.27 |
| CHEMBL176607 | — | — | 1 | 7.22 |
| CHEMBL179543 | — | — | 1 | 7.19 |
| CHEMBL360353 | — | — | 1 | 7.18 |
| CHEMBL178091 | — | — | 1 | 7.13 |
| CHEMBL179431 | — | — | 1 | 7.12 |
| CHEMBL361155 | — | — | 1 | 7.12 |
| CHEMBL361618 | — | — | 1 | 7.09 |
| CHEMBL361978 | — | — | 1 | 7.09 |
| CHEMBL178736 | — | — | 1 | 7.06 |
| CHEMBL179919 | — | — | 1 | 7.05 |
| CHEMBL426237 | — | — | 1 | 7.04 |
| CHEMBL179174 | — | — | 1 | 7.00 |
| CHEMBL178764 | — | — | 1 | 6.96 |
| CHEMBL179656 | — | — | 1 | 6.96 |
| CHEMBL175540 | — | — | 1 | 6.96 |
| CHEMBL369255 | — | — | 1 | 6.85 |
| CHEMBL179175 | — | — | 1 | 6.80 |
| CHEMBL178249 | — | — | 1 | 6.80 |
| CHEMBL360016 | — | — | 1 | 6.77 |
| CHEMBL178225 | — | — | 1 | 6.77 |
| CHEMBL180521 | — | — | 1 | 6.75 |
| CHEMBL179759 | — | — | 1 | 6.75 |
| CHEMBL367534 | — | — | 1 | 6.72 |
| CHEMBL362868 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL359683 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL180070 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL360955 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL178815 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL359851 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL367801 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL176607 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL179543 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL360353 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL178091 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL361155 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL179431 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL361618 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL361978 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL178736 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL179919 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL426237 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL179174 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL175540 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL179656 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL178764 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL369255 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL179175 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL178249 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL360016 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL178225 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL180521 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL179759 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL362868 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL367534 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL180426 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL443562 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL178352 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL178647 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL179357 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL89671 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL179063 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL179582 | — | IC50 | = | 76500.0 | nM | 4.12 |
| CHEMBL90048 | — | IC50 | = | 130000.0 | nM | - |