Assay Detail
Binding
CHEMBL4386830
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Inhibition of KIX-RLucN fused CBP (unknown origin) binding to KID-RLucC fused CREB (unknown origin) transfected in human HEK293 cells preincubated with compound 30 mins before before forskolin addition and measured after 90 mins in presence of coelenterazine by split Renilla luciferase complementation assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
SAR optimization studies on modified salicylamides as a potential treatment for acute myeloid leukemia through inhibition of the CREB pathway.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.66 | 5.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2313117 | — | — | 1 | 5.91 |
| CHEMBL4589141 | — | — | 1 | 5.82 |
| CHEMBL1448 | NICLOSAMIDE | 4.0 | 1 | 5.82 |
| CHEMBL4467546 | — | — | 1 | 5.81 |
| CHEMBL2338696 | — | — | 1 | 5.60 |
| CHEMBL4551427 | — | — | 1 | 5.52 |
| CHEMBL584646 | — | — | 1 | 5.40 |
| CHEMBL65742 | — | — | 1 | 5.39 |
| CHEMBL4442963 | — | — | 1 | - |
| CHEMBL4533737 | — | — | 1 | - |
| CHEMBL4468001 | — | — | 1 | - |
| CHEMBL4543954 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2313117 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL4589141 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL1448 | NICLOSAMIDE | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4467546 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL2338696 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL4551427 | — | IC50 | = | 3030.0 | nM | 5.52 |
| CHEMBL584646 | — | IC50 | = | 3990.0 | nM | 5.40 |
| CHEMBL65742 | — | IC50 | = | 4030.0 | nM | 5.39 |
| CHEMBL4442963 | — | IC50 | > | 7000.0 | nM | - |
| CHEMBL4533737 | — | IC50 | > | 7000.0 | nM | - |
| CHEMBL4468001 | — | IC50 | > | 7000.0 | nM | - |
| CHEMBL4543954 | — | IC50 | > | 7000.0 | nM | - |