Assay Detail
Binding
CHEMBL889184
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Inhibition of human recombinant FLAG-IKKepsilon by TR-FRET assay
34
Total Activities
34
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Inhibitor of nuclear factor kappa-B kinase subunit epsilon (CHEMBL3529) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.20 | 7.40 |
| pIC50 | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL373751 | GSK-319347A | — | 1 | 7.40 |
| CHEMBL397009 | — | — | 1 | 5.80 |
| CHEMBL230911 | GSK-625137A | — | 1 | 5.40 |
| CHEMBL231614 | — | — | 1 | - |
| CHEMBL231512 | — | — | 1 | - |
| CHEMBL231211 | — | — | 1 | - |
| CHEMBL231210 | — | — | 1 | - |
| CHEMBL231108 | — | — | 1 | - |
| CHEMBL389086 | — | — | 1 | - |
| CHEMBL231126 | — | — | 1 | - |
| CHEMBL268885 | GSK-711701A | — | 1 | - |
| CHEMBL397668 | — | — | 1 | - |
| CHEMBL231013 | GSK-605714A | — | 1 | - |
| CHEMBL230913 | — | — | 1 | - |
| CHEMBL230912 | — | — | 1 | - |
| CHEMBL388033 | — | — | 1 | - |
| CHEMBL230810 | — | — | 1 | - |
| CHEMBL230809 | — | — | 1 | - |
| CHEMBL230808 | — | — | 1 | - |
| CHEMBL397008 | — | — | 1 | - |
| CHEMBL230699 | — | — | 1 | - |
| CHEMBL230597 | GSK-586581A | — | 1 | - |
| CHEMBL230595 | — | — | 1 | - |
| CHEMBL230488 | — | — | 1 | - |
| CHEMBL230276 | — | — | 1 | - |
| CHEMBL230055 | — | — | 1 | - |
| CHEMBL231623 | GSK-620503A | — | 1 | - |
| CHEMBL231521 | — | — | 1 | - |
| CHEMBL207940 | — | — | 1 | - |
| CHEMBL230592 | GSK-635416A | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL373751 | GSK-319347A | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL397009 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL230911 | GSK-625137A | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL230913 | — | pIC50 | - | — | - | |
| CHEMBL231129 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL231013 | GSK-605714A | pIC50 | - | — | - | |
| CHEMBL397668 | — | pIC50 | - | — | - | |
| CHEMBL268885 | GSK-711701A | pIC50 | - | — | - | |
| CHEMBL231126 | — | pIC50 | - | — | - | |
| CHEMBL389086 | — | pIC50 | - | — | - | |
| CHEMBL231108 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL231210 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL231211 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL231512 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL231614 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230047 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL426532 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL388646 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230912 | — | pIC50 | - | — | - | |
| CHEMBL388033 | — | pIC50 | - | — | - | |
| CHEMBL230810 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230809 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230808 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL397008 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230699 | — | pIC50 | - | — | - | |
| CHEMBL230597 | GSK-586581A | IC50 | > | 15848.93 | nM | - |
| CHEMBL230595 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230488 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230276 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230055 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL231623 | GSK-620503A | IC50 | > | 15848.93 | nM | - |
| CHEMBL231521 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL207940 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230592 | GSK-635416A | pIC50 | - | — | - |