Assay Detail
ADMET
CHEMBL4628022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr in presence of ATP by fluorescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.00 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4632839 | — | — | 1 | 7.03 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.80 |
| CHEMBL4638350 | — | — | 1 | 6.64 |
| CHEMBL4633069 | — | — | 1 | 6.52 |
| CHEMBL4637172 | — | — | 1 | 6.46 |
| CHEMBL4642181 | — | — | 1 | 6.23 |
| CHEMBL4638092 | — | — | 1 | 6.21 |
| CHEMBL4638611 | — | — | 1 | 6.10 |
| CHEMBL4638783 | — | — | 1 | 5.83 |
| CHEMBL4637487 | — | — | 1 | 5.71 |
| CHEMBL4635318 | — | — | 1 | 5.59 |
| CHEMBL4642089 | — | — | 1 | 5.56 |
| CHEMBL4642128 | — | — | 1 | 5.54 |
| CHEMBL4648729 | — | — | 1 | 5.51 |
| CHEMBL4642587 | — | — | 1 | 5.22 |
| CHEMBL4646469 | — | — | 1 | 5.01 |
| CHEMBL4639891 | — | — | 1 | - |
| CHEMBL4637818 | — | — | 1 | - |
| CHEMBL4649103 | — | — | 1 | - |
| CHEMBL4649346 | — | — | 1 | - |
| CHEMBL4643586 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4632839 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4638350 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4633069 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4637172 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL4642181 | — | IC50 | = | 592.0 | nM | 6.23 |
| CHEMBL4638092 | — | IC50 | = | 618.0 | nM | 6.21 |
| CHEMBL4638611 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4638783 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4637487 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL4635318 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL4642089 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL4642128 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL4648729 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4642587 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4646469 | — | IC50 | = | 9870.0 | nM | 5.01 |
| CHEMBL4639891 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637818 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649103 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649346 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643586 | — | IC50 | > | 10000.0 | nM | - |