Assay Detail
Binding
CHEMBL5735129
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TR-FRET Assay: Compound dilution series were prepared in DMSO via an approximately 3-fold serial dilution. Compound dilutions were added directly into white, low-volume assay plates (Perkin Elmer Proxiplate 384 Plus#6008280) using a Labcyte Echo in conjunction with Labcyte Access and Thermo Multidrop CombinL robotics. Compounds were then suspended in eight microliters (μL) of assay buffer (20 mM Sodium Phosphate, pH 6.0, 50 mM NaCl, 1 mM Ethylenediaminetetraacetic acid disodium salt dihydrate, 0.01% Triton X-100, 1 mM DL-Dithiothreitol) containing His-tagged bromodomain, Europium-conjugated anti-His antibody (Invitrogen PV5596) and Alexa-647-conjugated probe.The final concentration of 1× assay mixture contained 2% DMSO, 12 nM His tagged BRD4 (BDI_K57-E168) and 100 nM probe or 4 nM His tagged BRD4 (BDII_E352-M457) and 30 nM probe, and 1 nM Europium-conjugated anti-His-tag antibody, and compound concentrations in the range of: 49.02 μM-0.61 nM or 0.98 μM-0.15 nM.After a one-hour equilibration at room temperature, TR-FRET ratios were determined using an Envision multilabel plate reader (Ex 340, Em 495/520).
396
Total Activities
130
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Bromodomain inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 132 | 6.38 | 8.68 |
| kon | 132 | - | - |
| k_off | 132 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 3 | 8.68 |
| CHEMBL5871072 | — | — | 3 | 7.82 |
| CHEMBL5973725 | — | — | 3 | 7.37 |
| CHEMBL5851529 | — | — | 3 | 7.36 |
| CHEMBL3915707 | — | — | 3 | 7.16 |
| CHEMBL3943998 | — | — | 3 | 7.16 |
| CHEMBL6008401 | — | — | 3 | 7.10 |
| CHEMBL5791546 | — | — | 3 | 7.02 |
| CHEMBL5913855 | — | — | 3 | 7.01 |
| CHEMBL5904027 | — | — | 3 | 7.01 |
| CHEMBL6043262 | — | — | 3 | 6.96 |
| CHEMBL5959049 | — | — | 3 | 6.94 |
| CHEMBL5956546 | — | — | 3 | 6.94 |
| CHEMBL6028076 | — | — | 3 | 6.85 |
| CHEMBL5779170 | — | — | 3 | 6.82 |
| CHEMBL5932110 | — | — | 3 | 6.80 |
| CHEMBL4552305 | — | — | 3 | 6.79 |
| CHEMBL4587188 | — | — | 3 | 6.78 |
| CHEMBL5798782 | — | — | 3 | 6.77 |
| CHEMBL5837742 | — | — | 3 | 6.77 |
| CHEMBL5766013 | — | — | 3 | 6.77 |
| CHEMBL5796364 | — | — | 3 | 6.76 |
| CHEMBL6023722 | — | — | 3 | 6.74 |
| CHEMBL5795648 | — | — | 3 | 6.73 |
| CHEMBL5948168 | — | — | 3 | 6.71 |
| CHEMBL6052044 | — | — | 3 | 6.71 |
| CHEMBL5742988 | — | — | 3 | 6.67 |
| CHEMBL5974321 | — | — | 3 | 6.67 |
| CHEMBL5976190 | — | — | 3 | 6.66 |
| CHEMBL6001919 | — | — | 3 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | Ki | = | 2.09 | nM | 8.68 |
| CHEMBL5871072 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5973725 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL5851529 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3943998 | — | Ki | = | 69.9 | nM | 7.16 |
| CHEMBL3915707 | — | Ki | = | 69.9 | nM | 7.16 |
| CHEMBL6008401 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL5791546 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL5904027 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL5913855 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL6043262 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL5959049 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL5956546 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL6028076 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL5779170 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL5932110 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL4552305 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL4587188 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL5837742 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL5766013 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL5798782 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL5796364 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL6023722 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL5795648 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL5948168 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL6052044 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL5742988 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL5974321 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL5976190 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL5874231 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL5877074 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL6001919 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL5988485 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL5818765 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL5877411 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL5801424 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL5946217 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL5744286 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL5993143 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL5887014 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL5972081 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL6027103 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL5973735 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL5761051 | — | Ki | = | 279.0 | nM | 6.55 |
| CHEMBL5895553 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL5955884 | — | Ki | = | 289.0 | nM | 6.54 |
| CHEMBL5942506 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL4464739 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL6003154 | — | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL6023813 | — | Ki | = | 323.0 | nM | 6.49 |