Assay Detail
Binding
CHEMBL3705880
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Human recombinant HDAC4 was expressed in full length form (aa 2-1084) in Sf9 insect cells (obtained from ATCC) using baculovirus generated with Bac-to-Bac system (Invitrogen). Test compounds were serially diluted to reach final test concentrations from 0.000128 uM to 10 uM. HDAC4 and test compounds were incubated in 25 mM Tris buffer pH 8.0 containing 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 0.05% (w/v) bovine serum albumine and 0.005% (v/v) Triton-X-100 for 2 hours at room temperature in presence of 5 uM of acetyl-Gly-Ala-Lys(E-trifluoroacetyl)-AMC (AMC=7-amino-4-methyl coumarin) in a final volume of 9 ul. Control wells with HDAC4 only (positive control) and without HDAC4 (negative control) were included on the microplate. Bovine trypsin (4.5 ul of a 300 nM solution) was added and the plate incubated for additional 15 minutes at room temperature. The plate was placed in a fluorescence microplate reader, and read at an excitation wavelength of 360 nm.
151
Total Activities
148
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Trifluoromethyl-oxadiazole derivatives and their use in the treatment of disease
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 151 | 6.74 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3692678 | — | — | 1 | 9.12 |
| CHEMBL3692689 | — | — | 1 | 9.07 |
| CHEMBL3692671 | — | — | 1 | 9.01 |
| CHEMBL3692673 | — | — | 1 | 9.00 |
| CHEMBL3692683 | — | — | 1 | 8.96 |
| CHEMBL3692676 | — | — | 1 | 8.92 |
| CHEMBL3639915 | — | — | 1 | 8.85 |
| CHEMBL3692679 | — | — | 1 | 8.80 |
| CHEMBL3692684 | — | — | 1 | 8.74 |
| CHEMBL3692686 | — | — | 1 | 8.44 |
| CHEMBL3692672 | — | — | 1 | 8.35 |
| CHEMBL3692666 | — | — | 1 | 8.30 |
| CHEMBL3692675 | — | — | 1 | 8.14 |
| CHEMBL3692657 | — | — | 1 | 8.12 |
| CHEMBL3692685 | — | — | 1 | 8.08 |
| CHEMBL3692660 | — | — | 1 | 8.05 |
| CHEMBL3692670 | — | — | 1 | 8.05 |
| CHEMBL3692668 | — | — | 1 | 8.01 |
| CHEMBL3692665 | — | — | 1 | 8.00 |
| CHEMBL3692669 | — | — | 1 | 8.00 |
| CHEMBL3692664 | — | — | 1 | 7.96 |
| CHEMBL3692622 | — | — | 1 | 7.92 |
| CHEMBL3692688 | — | — | 1 | 7.92 |
| CHEMBL3692663 | — | — | 1 | 7.89 |
| CHEMBL3692619 | — | — | 1 | 7.82 |
| CHEMBL3692655 | — | — | 1 | 7.82 |
| CHEMBL3692589 | — | — | 1 | 7.58 |
| CHEMBL3692616 | — | — | 3 | 7.58 |
| CHEMBL3692662 | — | — | 1 | 7.58 |
| CHEMBL3692614 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3692678 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL3692689 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL3692671 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL3692673 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3692683 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3692676 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3639915 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3692679 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3692684 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3692686 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3692672 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3692666 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3692675 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3692657 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3692685 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3692670 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3692660 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3692668 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL3692669 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3692665 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3692664 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3692688 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3692622 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3692663 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3692655 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3692619 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3692616 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3692589 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3692662 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3692614 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3692617 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3692653 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3692690 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3692661 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3692623 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3692621 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3692659 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3692609 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3692583 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3692637 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3692568 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3692626 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3692656 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3692587 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3692642 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3692630 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3692643 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3692651 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3692687 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3692618 | — | IC50 | = | 120.0 | nM | 6.92 |