Assay Detail
Binding
CHEMBL947134
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Inhibition of human recombinant CDK9/cyclin T expressed in insect cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.11 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL406463 | MERIOLIN 6 | — | 1 | 8.25 |
| CHEMBL270687 | MERIOLIN 5 | — | 1 | 8.25 |
| CHEMBL270686 | MERIOLIN 3 | — | 1 | 8.22 |
| CHEMBL406464 | MERIOLIN 4 | — | 1 | 8.15 |
| CHEMBL270897 | MERIOLIN 2 | — | 1 | 7.75 |
| CHEMBL411704 | — | — | 1 | 7.58 |
| CHEMBL405665 | MERIOLIN 1 | — | 1 | 7.58 |
| CHEMBL271597 | — | — | 1 | 7.30 |
| CHEMBL402443 | — | — | 1 | 6.66 |
| CHEMBL405200 | — | — | 1 | 6.60 |
| CHEMBL271195 | — | — | 1 | 6.00 |
| CHEMBL270926 | — | — | 1 | 5.96 |
| CHEMBL406102 | MERIOLIN 8 | — | 1 | 5.92 |
| CHEMBL405074 | MERIOLIN 7 | — | 1 | 5.28 |
| CHEMBL270346 | MERIOLIN 9 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL406463 | MERIOLIN 6 | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL270687 | MERIOLIN 5 | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL270686 | MERIOLIN 3 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL406464 | MERIOLIN 4 | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL270897 | MERIOLIN 2 | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL411704 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL405665 | MERIOLIN 1 | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL271597 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL402443 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL405200 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL271195 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL270926 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL406102 | MERIOLIN 8 | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL405074 | MERIOLIN 7 | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL270346 | MERIOLIN 9 | IC50 | > | 10000.0 | nM | - |