Assay Detail
Binding
CHEMBL974552
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Inhibition of human CDK4/GST-cyclin D1 expressed in Sf9 cells assessed as retinoblastoma GST-RB152 phosphorylation
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 4.63 | 6.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL258765 | FASCAPLYSIN CHLORIDE | — | 1 | 6.26 |
| CHEMBL213805 | — | — | 1 | 5.22 |
| CHEMBL463383 | — | — | 1 | 5.05 |
| CHEMBL498710 | — | — | 1 | 5.04 |
| CHEMBL458075 | — | — | 1 | 4.96 |
| CHEMBL498521 | — | — | 1 | 4.95 |
| CHEMBL456995 | — | — | 1 | 4.92 |
| CHEMBL496481 | — | — | 1 | 4.82 |
| CHEMBL456121 | — | — | 1 | 4.82 |
| CHEMBL521733 | — | — | 1 | 4.80 |
| CHEMBL456584 | — | — | 1 | 4.77 |
| CHEMBL496482 | — | — | 1 | 4.75 |
| CHEMBL455931 | — | — | 1 | 4.75 |
| CHEMBL457190 | — | — | 1 | 4.72 |
| CHEMBL456964 | — | — | 1 | 4.70 |
| CHEMBL498520 | — | — | 1 | 4.68 |
| CHEMBL456378 | — | — | 1 | 4.68 |
| CHEMBL456113 | — | — | 1 | 4.66 |
| CHEMBL457401 | — | — | 1 | 4.64 |
| CHEMBL456143 | — | — | 1 | 4.62 |
| CHEMBL525921 | — | — | 1 | 4.62 |
| CHEMBL463384 | — | — | 1 | 4.60 |
| CHEMBL457191 | — | — | 1 | 4.60 |
| CHEMBL515356 | — | — | 1 | 4.58 |
| CHEMBL457179 | — | — | 1 | 4.58 |
| CHEMBL456760 | — | — | 1 | 4.58 |
| CHEMBL509499 | — | — | 1 | 4.57 |
| CHEMBL456112 | — | — | 1 | 4.55 |
| CHEMBL515051 | — | — | 1 | 4.52 |
| CHEMBL517154 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL258765 | FASCAPLYSIN CHLORIDE | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL213805 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL463383 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL498710 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL458075 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL498521 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL456995 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL496481 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL456121 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL521733 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL456584 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL455931 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL496482 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL457190 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL456964 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL498520 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL456378 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL456113 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL457401 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL456143 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL525921 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL457191 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL463384 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL515356 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL457179 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL456760 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL509499 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL456112 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL515051 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL517154 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL456796 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL498705 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL515674 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL457390 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL497454 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL525530 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL457180 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL527039 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL525538 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL456759 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL458076 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL456965 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL456797 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL498130 | — | IC50 | = | 86000.0 | nM | 4.07 |