Assay Detail
Binding
CHEMBL4308743
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of biotinylated probe from human TAF1 bromodomain 2 (1522 to 1656 residues) expressed in Escherichia coli BL21 (DE3) by alphascreen assay
33
Total Activities
33
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 |
Target
Transcription initiation factor TFIID subunit 1 (CHEMBL3217390) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.68 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4589721 | — | — | 1 | 7.80 |
| CHEMBL4534000 | — | — | 1 | 7.51 |
| CHEMBL4542872 | — | — | 1 | 7.42 |
| CHEMBL4573352 | — | — | 1 | 7.20 |
| CHEMBL4556917 | — | — | 1 | 7.14 |
| CHEMBL4474288 | — | — | 1 | 7.09 |
| CHEMBL4440443 | — | — | 1 | 7.06 |
| CHEMBL4539891 | — | — | 1 | 7.05 |
| CHEMBL4466613 | — | — | 1 | 7.03 |
| CHEMBL3609314 | — | — | 1 | 7.00 |
| CHEMBL4437749 | — | — | 1 | 6.96 |
| CHEMBL3609309 | — | — | 1 | 6.82 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 6.80 |
| CHEMBL4468126 | — | — | 1 | 6.68 |
| CHEMBL4475297 | — | — | 1 | 6.68 |
| CHEMBL4572284 | — | — | 1 | 6.62 |
| CHEMBL4447984 | — | — | 1 | 6.52 |
| CHEMBL4552957 | — | — | 1 | 6.50 |
| CHEMBL4590890 | — | — | 1 | 6.47 |
| CHEMBL3609300 | — | — | 1 | 6.39 |
| CHEMBL4524310 | — | — | 1 | 6.35 |
| CHEMBL4514849 | — | — | 1 | 6.24 |
| CHEMBL4476205 | — | — | 1 | 6.24 |
| CHEMBL4470053 | — | — | 1 | 6.14 |
| CHEMBL4521536 | — | — | 1 | 6.12 |
| CHEMBL4546931 | — | — | 1 | 6.01 |
| CHEMBL4559020 | — | — | 1 | 5.77 |
| CHEMBL4584933 | — | — | 1 | 5.34 |
| CHEMBL4457319 | — | — | 1 | - |
| CHEMBL3609315 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4589721 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4534000 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4542872 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4573352 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4556917 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4474288 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4440443 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4539891 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4466613 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3609314 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4437749 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3609309 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL513909 | BI-2536 | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4468126 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4475297 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4572284 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4447984 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4552957 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4590890 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3609300 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4524310 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4514849 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4476205 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4470053 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4521536 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4546931 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4559020 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4584933 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4457319 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3609315 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4583926 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4483587 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3609299 | — | IC50 | > | 10000.0 | nM | - |