Assay Detail
Binding
CHEMBL5341972
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Inhibition of N-terminal 6His tagged KAT8 (173 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using biotinylated histone H4 peptide and [3H]Acetyl-CoA as substrates preincubated for 20 mins followed by substrate addition and measured after 4 hrs by MicroBeta microplate counter analysis
34
Total Activities
34
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
First-in-Class Selective Inhibitors of the Lysine Acetyltransferase KAT8.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 4.53 | 5.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5437016 | — | — | 1 | 5.09 |
| CHEMBL5426408 | — | — | 1 | 4.92 |
| CHEMBL5436305 | — | — | 1 | 4.86 |
| CHEMBL5421687 | — | — | 1 | 4.82 |
| CHEMBL5427978 | — | — | 1 | 4.78 |
| CHEMBL5410807 | — | — | 1 | 4.76 |
| CHEMBL5418109 | — | — | 1 | 4.73 |
| CHEMBL5403540 | — | — | 1 | 4.71 |
| CHEMBL5411173 | — | — | 1 | 4.71 |
| CHEMBL5401030 | — | — | 1 | 4.70 |
| CHEMBL1215739 | — | — | 1 | 4.69 |
| CHEMBL5423412 | — | — | 1 | 4.68 |
| CHEMBL5410111 | — | — | 1 | 4.57 |
| CHEMBL5402825 | — | — | 1 | 4.55 |
| CHEMBL5428346 | — | — | 1 | 4.54 |
| CHEMBL5437852 | — | — | 1 | 4.53 |
| CHEMBL33778 | ANACARDIC ACID | — | 1 | 4.52 |
| CHEMBL5430065 | — | — | 1 | 4.50 |
| CHEMBL5418231 | — | — | 1 | 4.48 |
| CHEMBL5405835 | — | — | 1 | 4.48 |
| CHEMBL5418574 | — | — | 1 | 4.42 |
| CHEMBL5414046 | — | — | 1 | 4.36 |
| CHEMBL5395500 | — | — | 1 | 4.28 |
| CHEMBL5424909 | — | — | 1 | 4.26 |
| CHEMBL5401537 | — | — | 1 | 4.23 |
| CHEMBL5440607 | — | — | 1 | 4.06 |
| CHEMBL5439437 | — | — | 1 | 4.05 |
| CHEMBL5402969 | — | — | 1 | 4.04 |
| CHEMBL5419803 | — | — | 1 | 4.02 |
| CHEMBL5405887 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5437016 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL5426408 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL5436305 | — | IC50 | = | 13900.0 | nM | 4.86 |
| CHEMBL5421687 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL5427978 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL5410807 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL5418109 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL5403540 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL5411173 | — | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL5401030 | — | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL1215739 | — | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL5423412 | — | IC50 | = | 20800.0 | nM | 4.68 |
| CHEMBL5410111 | — | IC50 | = | 26900.0 | nM | 4.57 |
| CHEMBL5402825 | — | IC50 | = | 28100.0 | nM | 4.55 |
| CHEMBL5428346 | — | IC50 | = | 29200.0 | nM | 4.54 |
| CHEMBL5437852 | — | IC50 | = | 29500.0 | nM | 4.53 |
| CHEMBL33778 | ANACARDIC ACID | IC50 | = | 30200.0 | nM | 4.52 |
| CHEMBL5430065 | — | IC50 | = | 31800.0 | nM | 4.50 |
| CHEMBL5418231 | — | IC50 | = | 33200.0 | nM | 4.48 |
| CHEMBL5405835 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL5418574 | — | IC50 | = | 38100.0 | nM | 4.42 |
| CHEMBL5414046 | — | IC50 | = | 44100.0 | nM | 4.36 |
| CHEMBL5395500 | — | IC50 | = | 52200.0 | nM | 4.28 |
| CHEMBL5424909 | — | IC50 | = | 54700.0 | nM | 4.26 |
| CHEMBL5401537 | — | IC50 | = | 59400.0 | nM | 4.23 |
| CHEMBL5440607 | — | IC50 | = | 86200.0 | nM | 4.06 |
| CHEMBL5439437 | — | IC50 | = | 88900.0 | nM | 4.05 |
| CHEMBL5402969 | — | IC50 | = | 90500.0 | nM | 4.04 |
| CHEMBL5419803 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL5405887 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL5434542 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL5400304 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL5437210 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL5402638 | — | IC50 | > | 150000.0 | nM | - |