Assay Detail
Binding
CHEMBL4121729
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Inhibition of CAMKK2 in mouse N39 cells assessed as decrease in AMPKalpha phosphorylation at T172 preincubated for 80 mins followed by inomycin addition by ELISA
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Calcium/calmodulin-dependent protein kinase kinase 2 (CHEMBL4295888) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 6.05 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4127330 | — | — | 1 | 7.50 |
| CHEMBL4126511 | — | — | 1 | 7.20 |
| CHEMBL4128577 | — | — | 1 | 7.00 |
| CHEMBL4125774 | — | — | 1 | 6.90 |
| CHEMBL4126095 | — | — | 1 | 6.80 |
| CHEMBL4125907 | — | — | 1 | 6.80 |
| CHEMBL4129791 | — | — | 1 | 6.70 |
| CHEMBL4128939 | — | — | 1 | 6.70 |
| CHEMBL4128717 | — | — | 1 | 6.60 |
| CHEMBL4128114 | — | — | 1 | 6.50 |
| CHEMBL4128459 | — | — | 1 | 6.40 |
| CHEMBL4129219 | — | — | 1 | 6.40 |
| CHEMBL4128540 | — | — | 1 | 6.30 |
| CHEMBL4126566 | — | — | 1 | 6.20 |
| CHEMBL4129362 | — | — | 1 | 6.10 |
| CHEMBL4129590 | — | — | 1 | 6.00 |
| CHEMBL4127245 | — | — | 1 | 5.90 |
| CHEMBL558642 | GSK-650394 | — | 1 | 5.90 |
| CHEMBL4130310 | — | — | 1 | 5.70 |
| CHEMBL4129941 | — | — | 1 | 5.60 |
| CHEMBL4127977 | — | — | 1 | 5.50 |
| CHEMBL4127797 | — | — | 1 | 5.50 |
| CHEMBL4126740 | — | — | 1 | 5.40 |
| CHEMBL4128950 | — | — | 1 | 5.40 |
| CHEMBL4125686 | — | — | 1 | 5.40 |
| CHEMBL4129991 | — | — | 1 | 5.40 |
| CHEMBL4127064 | — | — | 1 | 5.20 |
| CHEMBL4129130 | — | — | 1 | 5.20 |
| CHEMBL4127076 | — | — | 1 | 5.10 |
| CHEMBL4127319 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4127330 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4126511 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4128577 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4125774 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4126095 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4125907 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4129791 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4128939 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4128717 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4128114 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4129219 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4128459 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4128540 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4126566 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4129362 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4129590 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4127245 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL558642 | GSK-650394 | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4130310 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4129941 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4127797 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4127977 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4126740 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4128950 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4125686 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4129991 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4127064 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4129130 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4127076 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4127319 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4129843 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4127140 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4126300 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4126332 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4126413 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4127557 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4130166 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4128810 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4126756 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4127640 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4129040 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4128625 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4128151 | — | IC50 | > | 10000.0 | nM | - |