Assay Detail
Binding
CHEMBL2329083
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat recombinant GST-fused DYRK1A expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate after 30 mins by scintillation counting analysis in presence of [gamma-33P]-ATP
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL5508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.07 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2321961 | — | — | 1 | 6.96 |
| CHEMBL2321958 | — | — | 1 | 6.89 |
| CHEMBL1233659 | — | — | 1 | 6.68 |
| CHEMBL2321952 | — | — | 1 | 6.51 |
| CHEMBL2321878 | — | — | 1 | 6.39 |
| CHEMBL2321962 | — | — | 1 | 6.22 |
| CHEMBL2321959 | — | — | 1 | 6.20 |
| CHEMBL2321948 | — | — | 1 | 5.96 |
| CHEMBL2321945 | — | — | 1 | 5.89 |
| CHEMBL2321964 | — | — | 1 | 5.80 |
| CHEMBL409450 | 6BIO | — | 1 | 5.77 |
| CHEMBL373834 | — | — | 1 | 5.72 |
| CHEMBL2321968 | — | — | 1 | 5.70 |
| CHEMBL2321965 | — | — | 1 | 5.68 |
| CHEMBL2321974 | — | — | 1 | 5.58 |
| CHEMBL2321963 | — | — | 1 | 5.16 |
| CHEMBL2321967 | — | — | 1 | - |
| CHEMBL375870 | — | — | 1 | - |
| CHEMBL2321947 | — | — | 1 | - |
| CHEMBL2321957 | — | — | 1 | - |
| CHEMBL2321956 | — | — | 1 | - |
| CHEMBL2321955 | — | — | 1 | - |
| CHEMBL2321954 | — | — | 1 | - |
| CHEMBL2321953 | — | — | 1 | - |
| CHEMBL2321951 | — | — | 1 | - |
| CHEMBL213454 | — | — | 1 | - |
| CHEMBL2321949 | — | — | 1 | - |
| CHEMBL2321960 | — | — | 1 | - |
| CHEMBL2321946 | — | — | 1 | - |
| CHEMBL2322019 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2321961 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2321958 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1233659 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2321952 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2321878 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2321962 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2321959 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2321948 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2321945 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2321964 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL409450 | 6BIO | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL373834 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2321968 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2321965 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2321974 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2321963 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2321969 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321970 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321971 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321972 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321973 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321975 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2322019 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321946 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321960 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321949 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL213454 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321951 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321953 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321954 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321955 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321956 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321957 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321947 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL375870 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2321967 | — | IC50 | > | 10000.0 | nM | - |