Assay Detail
Binding
CHEMBL4136604
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Inhibition of Mycobacterium tuberculosis PknA (M1 to A296 residues) expressed in Escherichia coli BL21 (DE3) pLysS cells using [T-33P]ATP as substrate after 120 mins in presence of GarA by liquid scintillation method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mycobacterium tuberculosis |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase PknA (CHEMBL4295585) ↗| Type | SINGLE PROTEIN |
| Organism | Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv) |
Publication
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.11 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162308 | — | — | 1 | 8.05 |
| CHEMBL4165984 | — | — | 1 | 7.96 |
| CHEMBL4162544 | — | — | 1 | 7.92 |
| CHEMBL4173915 | — | — | 1 | 7.75 |
| CHEMBL4170479 | — | — | 1 | 7.75 |
| CHEMBL4162719 | — | — | 1 | 7.66 |
| CHEMBL4162511 | — | — | 1 | 5.75 |
| CHEMBL4170446 | — | — | 1 | 5.64 |
| CHEMBL4177445 | — | — | 1 | 5.54 |
| CHEMBL4173877 | — | — | 1 | - |
| CHEMBL4165949 | — | — | 1 | - |
| CHEMBL4159344 | — | — | 1 | - |
| CHEMBL4167265 | — | — | 1 | - |
| CHEMBL4170653 | — | — | 1 | - |
| CHEMBL4166160 | — | — | 1 | - |
| CHEMBL4172982 | — | — | 1 | - |
| CHEMBL4169382 | — | — | 1 | - |
| CHEMBL4170024 | — | — | 1 | - |
| CHEMBL4159392 | — | — | 1 | - |
| CHEMBL4164081 | — | — | 1 | - |
| CHEMBL4174513 | — | — | 1 | - |
| CHEMBL4177229 | — | — | 1 | - |
| CHEMBL4176789 | — | — | 1 | - |
| CHEMBL4172772 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162308 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4165984 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4162544 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4173915 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4170479 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4162719 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4162511 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL4170446 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL4177445 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL4173877 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL4165949 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL4159344 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL4167265 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL4170653 | — | Ki | < | 8.0 | nM | - |
| CHEMBL4166160 | — | Ki | < | 8.0 | nM | - |
| CHEMBL4172982 | — | Ki | < | 8.0 | nM | - |
| CHEMBL4169382 | — | Ki | - | — | - | |
| CHEMBL4170024 | — | Ki | > | 33000.0 | nM | - |
| CHEMBL4159392 | — | Ki | > | 33000.0 | nM | - |
| CHEMBL4164081 | — | Ki | > | 33000.0 | nM | - |
| CHEMBL4174513 | — | Ki | > | 33000.0 | nM | - |
| CHEMBL4177229 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL4176789 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL4172772 | — | Ki | > | 4000.0 | nM | - |