Assay Detail
Binding
CHEMBL734032
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Inhibitory concentration against Mitogen activated protein kinase kinase kinase 1 was determined using Raf/MEK1 coupled assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.30 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL106489 | — | — | 1 | 9.00 |
| CHEMBL105642 | — | — | 1 | 8.70 |
| CHEMBL105220 | — | — | 1 | 8.70 |
| CHEMBL102374 | — | — | 1 | 8.70 |
| CHEMBL318804 | — | — | 1 | 8.70 |
| CHEMBL105442 | CI-1040 | 2.0 | 1 | 8.70 |
| CHEMBL103045 | — | — | 1 | 8.52 |
| CHEMBL414139 | — | — | 1 | 8.40 |
| CHEMBL323515 | — | — | 1 | 8.40 |
| CHEMBL322857 | — | — | 1 | 8.30 |
| CHEMBL318326 | — | — | 1 | 8.10 |
| CHEMBL102786 | — | — | 1 | 8.05 |
| CHEMBL321045 | — | — | 1 | 8.00 |
| CHEMBL321078 | — | — | 1 | 7.55 |
| CHEMBL320688 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL106489 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL105642 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL105220 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL102374 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL318804 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL105442 | CI-1040 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL103045 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL414139 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL323515 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL322857 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL318326 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL102786 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL321045 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL321078 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL320688 | — | IC50 | = | 212.0 | nM | 6.67 |