Assay Detail
Binding
CHEMBL3865749
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Inhibition of Mycobacterium tuberculosis H37Rv Eis expressed in Escherichia coli BL21(DE3) using Acetyl-CoA as substrate preincubated for 10 mins followed by substrate addition measured every 30 sec for 10 mins
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mycobacterium tuberculosis H37Rv |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
N-acetyltransferase Eis (CHEMBL3879870) ↗| Type | SINGLE PROTEIN |
| Organism | Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv) |
Publication
Discovery and Optimization of Two Eis Inhibitor Families as Kanamycin Adjuvants against Drug-Resistant M. tuberculosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.13 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3931070 | — | — | 1 | 7.82 |
| CHEMBL1410785 | — | — | 1 | 7.05 |
| CHEMBL3950034 | — | — | 1 | 6.80 |
| CHEMBL3976122 | — | — | 1 | 6.60 |
| CHEMBL3960292 | — | — | 1 | 6.52 |
| CHEMBL3903088 | — | — | 1 | 6.52 |
| CHEMBL3927142 | — | — | 1 | 6.48 |
| CHEMBL3905343 | — | — | 1 | 6.30 |
| CHEMBL3927499 | — | — | 1 | 6.27 |
| CHEMBL3980494 | — | — | 1 | 6.22 |
| CHEMBL3915019 | — | — | 1 | 5.92 |
| CHEMBL1612166 | — | — | 1 | 5.66 |
| CHEMBL3926253 | — | — | 1 | 5.54 |
| CHEMBL3958709 | — | — | 1 | 5.52 |
| CHEMBL3909271 | — | — | 1 | 5.24 |
| CHEMBL3890216 | — | — | 1 | 5.06 |
| CHEMBL3899105 | — | — | 1 | 4.64 |
| CHEMBL3900249 | — | — | 1 | - |
| CHEMBL3971387 | — | — | 1 | - |
| CHEMBL3979506 | — | — | 1 | - |
| CHEMBL3964177 | — | — | 1 | - |
| CHEMBL3891229 | — | — | 1 | - |
| CHEMBL3940094 | — | — | 1 | - |
| CHEMBL1538832 | — | — | 1 | - |
| CHEMBL3952477 | — | — | 1 | - |
| CHEMBL3976851 | — | — | 1 | - |
| CHEMBL1702313 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3931070 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1410785 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3950034 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3976122 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3960292 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3903088 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3927142 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3905343 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3927499 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3980494 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3915019 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1612166 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3926253 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3958709 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3909271 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3890216 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL3899105 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3900249 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3971387 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3979506 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3964177 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3891229 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3940094 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1538832 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3952477 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3976851 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1702313 | — | IC50 | > | 200000.0 | nM | - |