Assay Detail
Binding
CHEMBL3706045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The ability of the nuclear factor-kappa B (NF-kB)-inducing kinase (NIK) to catalyze the hydrolysis of adenosine-5'-triphosphate (ATP) was monitored using the Transcreener ADP (adenosine-5'-diphosphate) assay (BellBrook Labs). Purified NIK (0.2-1 nM) derived from a baculovirus-infected insect cell expression system was incubated with test compounds for 1-3.5 hours in 50 mM 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid buffer (pH 7.2) containing 10 mM MgCl.sub.2, 2 mM dithiothreitol, 10 uM ATP, 0.01% Triton X-100, 0.1% gamma-globulins from bovine blood, 1% dimethylsulfoxide (DMSO), 12 ug/mL ADP antibody and 4 nM ADP-AlexaFluor.RTM. 633 tracer. Reactions were quenched by the addition of 20 mM 2,2',2'',2'''-(ethane-1,2-diyldinitrilo)tetraacetic acid and 0.01% Brij 35. The tracer bound to the antibody was displaced by the ADP generated during the NIK reaction, which causes a decrease in fluorescence polarization that was measured by laser excitation.
815
Total Activities
608
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase kinase kinase 14 (CHEMBL5888) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tricyclic compounds and methods of use therefor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 815 | 7.97 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3696534 | — | — | 1 | 10.40 |
| CHEMBL3696579 | — | — | 1 | 10.26 |
| CHEMBL4115488 | — | — | 2 | 10.00 |
| CHEMBL3934782 | — | — | 2 | 10.00 |
| CHEMBL3700218 | — | — | 2 | 10.00 |
| CHEMBL3700225 | — | — | 2 | 10.00 |
| CHEMBL3696555 | — | — | 1 | 9.92 |
| CHEMBL3696576 | — | — | 1 | 9.92 |
| CHEMBL3696586 | — | — | 1 | 9.80 |
| CHEMBL4112609 | — | — | 1 | 9.70 |
| CHEMBL3692395 | — | — | 1 | 9.70 |
| CHEMBL4113253 | — | — | 1 | 9.70 |
| CHEMBL3696652 | — | — | 1 | 9.70 |
| CHEMBL4110869 | — | — | 1 | 9.70 |
| CHEMBL3700272 | — | — | 1 | 9.70 |
| CHEMBL3696566 | — | — | 1 | 9.62 |
| CHEMBL3957252 | — | — | 2 | 9.54 |
| CHEMBL4109262 | — | — | 2 | 9.54 |
| CHEMBL4098056 | — | — | 1 | 9.52 |
| CHEMBL3692450 | — | — | 1 | 9.52 |
| CHEMBL4113471 | — | — | 1 | 9.52 |
| CHEMBL3696699 | — | — | 1 | 9.52 |
| CHEMBL3696721 | — | — | 2 | 9.52 |
| CHEMBL3696722 | — | — | 2 | 9.52 |
| CHEMBL3700328 | — | — | 1 | 9.52 |
| CHEMBL4111969 | — | — | 1 | 9.51 |
| CHEMBL3696558 | — | — | 2 | 9.48 |
| CHEMBL3696560 | — | — | 2 | 9.48 |
| CHEMBL3700232 | — | — | 3 | 9.48 |
| CHEMBL3700298 | — | — | 2 | 9.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3696534 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL3696579 | — | Ki | = | 0.055 | nM | 10.26 |
| CHEMBL3934782 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3700225 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4115488 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3700218 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3696576 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL3696555 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL3696586 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL3692395 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4113253 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3700272 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3696652 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4110869 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4112609 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3696566 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL4109262 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL3957252 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL4113471 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3696722 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3696699 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3696721 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4098056 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3692450 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3700328 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4111969 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL3700232 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL3700299 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL3700298 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL3696558 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL3696560 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL3700227 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL3700221 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL3700277 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3700276 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3696659 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3692522 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3700329 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3700197 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3692439 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3700192 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4113023 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4109556 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3696671 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3696672 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3696705 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3696553 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3700327 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3696655 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL3696533 | — | Ki | = | 0.53 | nM | 9.28 |