Assay Detail
Binding
CHEMBL4404752
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal NusA-fused His6-tagged human KAT6A (507 to 778 residues) expressed in Escherichia coli BL21 (DE3) cells using 0.4 uM acetyl coenzyme A and N-terminal histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRKV-GGK-biotin) as substrate incubated for 60 mins by Alpha screen technology
177
Total Activities
177
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
Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 177 | 6.86 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4468833 | — | — | 1 | 8.30 |
| CHEMBL4437798 | — | — | 1 | 8.26 |
| CHEMBL4466823 | — | — | 1 | 8.22 |
| CHEMBL4456585 | WM-1119 | — | 1 | 8.20 |
| CHEMBL4475883 | — | — | 1 | 8.15 |
| CHEMBL4539384 | — | — | 1 | 8.10 |
| CHEMBL4441439 | — | — | 1 | 8.05 |
| CHEMBL4521125 | — | — | 1 | 8.05 |
| CHEMBL4565790 | — | — | 1 | 8.03 |
| CHEMBL4458272 | — | — | 1 | 7.96 |
| CHEMBL4445473 | — | — | 1 | 7.89 |
| CHEMBL4465716 | — | — | 1 | 7.89 |
| CHEMBL4516984 | — | — | 1 | 7.85 |
| CHEMBL4541948 | — | — | 1 | 7.85 |
| CHEMBL4436877 | — | — | 1 | 7.85 |
| CHEMBL4449163 | — | — | 1 | 7.82 |
| CHEMBL4518462 | — | — | 1 | 7.80 |
| CHEMBL4446917 | — | — | 1 | 7.80 |
| CHEMBL4593500 | — | — | 1 | 7.77 |
| CHEMBL4573736 | — | — | 1 | 7.77 |
| CHEMBL4566403 | — | — | 1 | 7.75 |
| CHEMBL4588945 | — | — | 1 | 7.75 |
| CHEMBL4572653 | — | — | 1 | 7.70 |
| CHEMBL4455027 | — | — | 1 | 7.70 |
| CHEMBL4456874 | — | — | 1 | 7.64 |
| CHEMBL4464911 | — | — | 1 | 7.64 |
| CHEMBL4453559 | — | — | 1 | 7.62 |
| CHEMBL4593937 | — | — | 1 | 7.62 |
| CHEMBL4530056 | — | — | 1 | 7.62 |
| CHEMBL4454163 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4468833 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4437798 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4466823 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4456585 | WM-1119 | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4475883 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4539384 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4441439 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4521125 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4565790 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4458272 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4465716 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4445473 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4541948 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4436877 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4516984 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4449163 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4446917 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4518462 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4593500 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4573736 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4588945 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4566403 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4455027 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4572653 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4456874 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4464911 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4453559 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4530056 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4593937 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4454163 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4445456 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4559662 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4454507 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4526110 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4554392 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4450971 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4446616 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4441001 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4461380 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4451170 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4464974 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4444077 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4560554 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4475866 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4464572 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4465155 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4468268 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4464519 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4576670 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4524297 | — | IC50 | = | 61.0 | nM | 7.21 |