Assay Detail
Binding
CHEMBL889183
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Inhibition of human recombinant GST-IKKbeta by TR-FRET assay
34
Total Activities
34
Compounds Tested
1
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 beta (CHEMBL1991) ↗| 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 | 34 | 6.08 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230488 | — | — | 1 | 7.00 |
| CHEMBL230047 | — | — | 1 | 6.80 |
| CHEMBL230912 | — | — | 1 | 6.80 |
| CHEMBL230276 | — | — | 1 | 6.70 |
| CHEMBL231129 | — | — | 1 | 6.60 |
| CHEMBL397008 | — | — | 1 | 6.60 |
| CHEMBL397009 | — | — | 1 | 6.60 |
| CHEMBL426532 | — | — | 1 | 6.60 |
| CHEMBL388646 | — | — | 1 | 6.50 |
| CHEMBL231512 | — | — | 1 | 6.50 |
| CHEMBL231614 | — | — | 1 | 6.50 |
| CHEMBL230913 | — | — | 1 | 6.40 |
| CHEMBL230055 | — | — | 1 | 6.20 |
| CHEMBL231210 | — | — | 1 | 6.00 |
| CHEMBL231623 | GSK-620503A | — | 1 | 5.80 |
| CHEMBL230597 | GSK-586581A | — | 1 | 5.80 |
| CHEMBL230595 | — | — | 1 | 5.80 |
| CHEMBL231108 | — | — | 1 | 5.80 |
| CHEMBL230809 | — | — | 1 | 5.40 |
| CHEMBL230911 | GSK-625137A | — | 1 | 5.40 |
| CHEMBL231211 | — | — | 1 | 5.10 |
| CHEMBL230808 | — | — | 1 | 5.10 |
| CHEMBL230699 | — | — | 1 | 5.10 |
| CHEMBL207940 | — | — | 1 | 4.80 |
| CHEMBL230810 | — | — | 1 | - |
| CHEMBL231013 | GSK-605714A | — | 1 | - |
| CHEMBL397668 | — | — | 1 | - |
| CHEMBL268885 | GSK-711701A | — | 1 | - |
| CHEMBL373751 | GSK-319347A | — | 1 | - |
| CHEMBL231126 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230488 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL230047 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL230912 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL230276 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL231129 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL397008 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL397009 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL426532 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL388646 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL231512 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL231614 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL230913 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL230055 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL231210 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL230597 | GSK-586581A | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL230595 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL231108 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL231623 | GSK-620503A | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL230809 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL230911 | GSK-625137A | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL231211 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL230808 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL230699 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL207940 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL388033 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL230592 | GSK-635416A | IC50 | > | 15848.93 | nM | - |
| CHEMBL231521 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL389086 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL231126 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL373751 | GSK-319347A | IC50 | > | 15848.93 | nM | - |
| CHEMBL268885 | GSK-711701A | IC50 | > | 15848.93 | nM | - |
| CHEMBL397668 | — | IC50 | > | 15848.93 | nM | - |
| CHEMBL231013 | GSK-605714A | IC50 | > | 15848.93 | nM | - |
| CHEMBL230810 | — | IC50 | > | 15848.93 | nM | - |