Assay Detail
Binding
CHEMBL4139705
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Inhibition of KAT3B catalytic domain (1284 to 1673 residues) (unknown origin) using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate after 5 mins in presence of Ac-CoA by fluorescence assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The relevance of Ki calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.11 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4159902 | — | — | 1 | 5.96 |
| CHEMBL576321 | — | — | 1 | 5.85 |
| CHEMBL4166834 | — | — | 1 | 5.58 |
| CHEMBL4172065 | — | — | 1 | 5.52 |
| CHEMBL4160049 | — | — | 1 | 5.43 |
| CHEMBL4170165 | — | — | 1 | 4.28 |
| CHEMBL4170179 | — | — | 1 | 4.22 |
| CHEMBL4175261 | — | — | 1 | 4.02 |
| CHEMBL1232567 | — | — | 1 | - |
| CHEMBL4174622 | — | — | 1 | - |
| CHEMBL4166714 | — | — | 1 | - |
| CHEMBL2312200 | — | — | 1 | - |
| CHEMBL4172714 | — | — | 1 | - |
| CHEMBL4168293 | — | — | 1 | - |
| CHEMBL4172575 | — | — | 1 | - |
| CHEMBL4168302 | — | — | 1 | - |
| CHEMBL4161954 | — | — | 1 | - |
| CHEMBL4163878 | — | — | 1 | - |
| CHEMBL1142 | 4-AMINOPHENOL | — | 1 | - |
| CHEMBL4168076 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4159902 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL576321 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4166834 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4172065 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4160049 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4170165 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL4170179 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL4175261 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL1232567 | — | IC50 | - | — | - | |
| CHEMBL4174622 | — | IC50 | - | — | - | |
| CHEMBL4166714 | — | IC50 | - | — | - | |
| CHEMBL2312200 | — | IC50 | = | 106000.0 | nM | - |
| CHEMBL4172714 | — | IC50 | - | — | - | |
| CHEMBL4168293 | — | IC50 | - | — | - | |
| CHEMBL4172575 | — | IC50 | - | — | - | |
| CHEMBL4168302 | — | IC50 | - | — | - | |
| CHEMBL4161954 | — | IC50 | - | — | - | |
| CHEMBL4163878 | — | IC50 | = | 250000.0 | nM | - |
| CHEMBL1142 | 4-AMINOPHENOL | IC50 | > | 500000.0 | nM | - |
| CHEMBL4168076 | — | IC50 | - | — | - |