Assay Detail
Binding
CHEMBL4139703
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate after 5 mins in presence of Ac-CoA by fluorescence assay
31
Total Activities
31
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 | 31 | 4.57 | 5.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4159902 | — | — | 1 | 5.12 |
| CHEMBL576321 | — | — | 1 | 5.01 |
| CHEMBL4160049 | — | — | 1 | 4.64 |
| CHEMBL4166834 | — | — | 1 | 4.43 |
| CHEMBL4172065 | — | — | 1 | 4.18 |
| CHEMBL4175261 | — | — | 1 | 4.05 |
| CHEMBL4175125 | — | — | 1 | - |
| CHEMBL456807 | PHENYLHYDRAZINE | — | 1 | - |
| CHEMBL4168293 | — | — | 1 | - |
| CHEMBL4165941 | — | — | 1 | - |
| CHEMBL165373 | — | — | 1 | - |
| CHEMBL57394 | — | — | 1 | - |
| CHEMBL1142 | 4-AMINOPHENOL | — | 1 | - |
| CHEMBL15888 | 4-CHLOROANILINE | — | 1 | - |
| CHEMBL12392 | — | — | 1 | - |
| CHEMBL32014 | — | — | 1 | - |
| CHEMBL4165575 | — | — | 1 | - |
| CHEMBL3182475 | — | — | 1 | - |
| CHEMBL4174622 | — | — | 1 | - |
| CHEMBL4163878 | — | — | 1 | - |
| CHEMBL4170179 | — | — | 1 | - |
| CHEMBL4161954 | — | — | 1 | - |
| CHEMBL4168302 | — | — | 1 | - |
| CHEMBL4172575 | — | — | 1 | - |
| CHEMBL4168076 | — | — | 1 | - |
| CHEMBL4172714 | — | — | 1 | - |
| CHEMBL4170165 | — | — | 1 | - |
| CHEMBL2312200 | — | — | 1 | - |
| CHEMBL1232567 | — | — | 1 | - |
| CHEMBL4166714 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4159902 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL576321 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4160049 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4166834 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL4172065 | — | IC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL4175261 | — | IC50 | = | 89000.0 | nM | 4.05 |
| CHEMBL4168293 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4167262 | — | IC50 | = | 680000.0 | nM | - |
| CHEMBL4165941 | — | IC50 | = | 940000.0 | nM | - |
| CHEMBL165373 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL57394 | — | IC50 | = | 181000.0 | nM | - |
| CHEMBL1142 | 4-AMINOPHENOL | IC50 | > | 500000.0 | nM | - |
| CHEMBL15888 | 4-CHLOROANILINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL12392 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL32014 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4165575 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3182475 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL456807 | PHENYLHYDRAZINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4175125 | — | IC50 | = | 310000.0 | nM | - |
| CHEMBL4174622 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4163878 | — | IC50 | = | 365000.0 | nM | - |
| CHEMBL4170179 | — | IC50 | = | 250000.0 | nM | - |
| CHEMBL4161954 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4168302 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4172575 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4168076 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4172714 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4170165 | — | IC50 | = | 177000.0 | nM | - |
| CHEMBL2312200 | — | IC50 | = | 141000.0 | nM | - |
| CHEMBL1232567 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4166714 | — | IC50 | > | 500000.0 | nM | - |