Assay Detail
Binding
CHEMBL4201009
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GCK (unknown origin) by radiometric biochemical kinase assay
30
Total Activities
30
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
Mitogen-activated protein kinase kinase kinase kinase 2 (CHEMBL5330) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.63 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4214342 | — | — | 1 | 9.00 |
| CHEMBL4202685 | — | — | 1 | 8.70 |
| CHEMBL4207036 | — | — | 1 | 8.70 |
| CHEMBL4213673 | — | — | 1 | 8.30 |
| CHEMBL4207100 | — | — | 1 | 8.30 |
| CHEMBL4217421 | — | — | 1 | 8.22 |
| CHEMBL4214863 | — | — | 1 | 8.15 |
| CHEMBL1214141 | — | — | 1 | 8.10 |
| CHEMBL4209948 | — | — | 1 | 8.10 |
| CHEMBL4207753 | — | — | 1 | 8.10 |
| CHEMBL4211976 | — | — | 1 | 8.00 |
| CHEMBL4213019 | — | — | 1 | 7.85 |
| CHEMBL4216786 | — | — | 1 | 7.80 |
| CHEMBL4212663 | — | — | 1 | 7.77 |
| CHEMBL4212150 | — | — | 1 | 7.62 |
| CHEMBL4211880 | — | — | 1 | 7.57 |
| CHEMBL459850 | — | — | 1 | 7.55 |
| CHEMBL4215989 | — | — | 1 | 7.48 |
| CHEMBL4203337 | — | — | 1 | 7.47 |
| CHEMBL4212809 | — | — | 1 | 7.41 |
| CHEMBL4210482 | — | — | 1 | 7.38 |
| CHEMBL4218831 | — | — | 1 | 7.35 |
| CHEMBL1214142 | — | — | 1 | 7.33 |
| CHEMBL4215916 | — | — | 1 | 7.26 |
| CHEMBL4213945 | — | — | 1 | 7.20 |
| CHEMBL4205942 | — | — | 1 | 7.14 |
| CHEMBL4206139 | — | — | 1 | 6.78 |
| CHEMBL4210185 | — | — | 1 | 6.30 |
| CHEMBL4211395 | — | — | 1 | 6.03 |
| CHEMBL4209082 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4214342 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4202685 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4207036 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4213673 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4207100 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4217421 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4214863 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1214141 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4209948 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4207753 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4211976 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4213019 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4216786 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4212663 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4212150 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4211880 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL459850 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4215989 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4203337 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4212809 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4210482 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4218831 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1214142 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4215916 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4213945 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4205942 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4206139 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4210185 | — | IC50 | = | 497.0 | nM | 6.30 |
| CHEMBL4211395 | — | IC50 | = | 925.0 | nM | 6.03 |
| CHEMBL4209082 | — | IC50 | = | 1080.0 | nM | 5.97 |