Assay Detail
Binding
CHEMBL2045992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human Erg
49
Total Activities
49
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
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 5.15 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2043004 | — | — | 1 | 6.66 |
| CHEMBL2041176 | — | — | 1 | 6.43 |
| CHEMBL2041177 | — | — | 1 | 6.19 |
| CHEMBL2041172 | — | — | 1 | 6.14 |
| CHEMBL2040897 | — | — | 1 | 6.02 |
| CHEMBL2043327 | — | — | 1 | 6.00 |
| CHEMBL2041185 | — | — | 1 | 5.85 |
| CHEMBL2041175 | — | — | 1 | 5.82 |
| CHEMBL2041168 | — | — | 1 | 5.70 |
| CHEMBL2043170 | — | — | 1 | 5.62 |
| CHEMBL2041191 | — | — | 1 | 5.60 |
| CHEMBL2041173 | — | — | 1 | 5.33 |
| CHEMBL2043172 | — | — | 1 | 5.24 |
| CHEMBL2043168 | — | — | 1 | 5.19 |
| CHEMBL2043169 | — | — | 1 | 5.16 |
| CHEMBL2041181 | — | — | 1 | 5.15 |
| CHEMBL2041190 | — | — | 1 | 5.14 |
| CHEMBL2040894 | — | — | 1 | 5.11 |
| CHEMBL2041186 | — | — | 1 | 5.11 |
| CHEMBL2041164 | — | — | 1 | 5.10 |
| CHEMBL2041169 | — | — | 1 | 5.09 |
| CHEMBL2041178 | — | — | 1 | 5.07 |
| CHEMBL2041179 | — | — | 1 | 5.05 |
| CHEMBL2040895 | — | — | 1 | 5.05 |
| CHEMBL2041010 | — | — | 1 | 4.92 |
| CHEMBL2041170 | — | — | 1 | 4.89 |
| CHEMBL2043325 | — | — | 1 | 4.89 |
| CHEMBL2041174 | — | — | 1 | 4.82 |
| CHEMBL2041189 | — | — | 1 | 4.80 |
| CHEMBL2041171 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2043004 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2041176 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2041177 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2041172 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL2040897 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL2043327 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2041185 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2041175 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2041168 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2043170 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2041191 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2041173 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL2043172 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2043168 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL2043169 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2041181 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2041190 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL2040894 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL2041186 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL2041164 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL2041169 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL2041178 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2041179 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL2040895 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL2041010 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2043325 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2041170 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2041174 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2041189 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2041171 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2041187 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL2040854 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL2041183 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2041184 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2041193 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2040896 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2041188 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL2043326 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL2043328 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2041192 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL2041182 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL2041180 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL2043324 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL2041167 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL2041166 | — | IC50 | - | — | - | |
| CHEMBL2041165 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL2043171 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL2043011 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2043010 | — | IC50 | > | 30000.0 | nM | - |