Assay Detail
Binding
CHEMBL3419558
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Inhibition of recombinant histone acetyltransferase p300 (unknown origin) using dH3-H4 tetramer and [3H]-acetyl-CoA assessed as acetate incorporation after 30 mins by liquid scintillation counting
22
Total Activities
22
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
PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.70 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3416552 | — | — | 1 | 6.58 |
| CHEMBL1331211 | — | — | 1 | 6.48 |
| CHEMBL2030281 | — | — | 1 | 6.29 |
| CHEMBL2031566 | — | — | 1 | 6.18 |
| CHEMBL3416536 | — | — | 1 | 6.00 |
| CHEMBL3416321 | — | — | 1 | 5.96 |
| CHEMBL3235887 | — | — | 1 | 5.96 |
| CHEMBL502489 | GARCINOL | — | 1 | 5.77 |
| CHEMBL1385343 | — | — | 1 | 5.75 |
| CHEMBL3416537 | — | — | 1 | 5.75 |
| CHEMBL3416335 | — | — | 1 | 5.72 |
| CHEMBL1600114 | — | — | 1 | 5.70 |
| CHEMBL3416317 | — | — | 1 | 5.66 |
| CHEMBL3416526 | — | — | 1 | 5.55 |
| CHEMBL3235890 | — | — | 1 | 5.51 |
| CHEMBL3416525 | — | — | 1 | 5.43 |
| CHEMBL3416316 | — | — | 1 | 5.21 |
| CHEMBL3416315 | — | — | 1 | 5.21 |
| CHEMBL3416307 | — | — | 1 | 5.12 |
| CHEMBL3416528 | — | — | 1 | 5.01 |
| CHEMBL1602759 | — | — | 1 | 4.96 |
| CHEMBL106 | FLUCONAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3416552 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1331211 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2030281 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2031566 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3416536 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3416321 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3235887 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL502489 | GARCINOL | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1385343 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3416537 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3416335 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1600114 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3416317 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3416526 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3235890 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3416525 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3416316 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL3416315 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL3416307 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3416528 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL1602759 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL106 | FLUCONAZOLE | IC50 | - | — | - |