Assay Detail
ADMET
CHEMBL4386410
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) (CHEMBL2111363) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.00 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.40 |
| CHEMBL4532181 | — | — | 1 | 6.80 |
| CHEMBL4578278 | — | — | 1 | 6.40 |
| CHEMBL4541796 | — | — | 1 | 6.30 |
| CHEMBL4066920 | — | — | 1 | 6.20 |
| CHEMBL4470067 | — | — | 1 | 6.10 |
| CHEMBL4531802 | — | — | 1 | 5.90 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 5.80 |
| CHEMBL3971436 | — | — | 1 | 5.50 |
| CHEMBL2018451 | — | — | 1 | 5.40 |
| CHEMBL2170177 | — | — | 1 | 4.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4532181 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4578278 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4541796 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4066920 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4470067 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4531802 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3971436 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL2018451 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL2170177 | — | IC50 | = | 63095.73 | nM | 4.20 |