Assay Detail
ADMET
CHEMBL4628023
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His-tagged Abl (2 to 1130 residues) expressed in baculovirus expression system using FAM-labelled P2 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 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 6.84 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.92 |
| CHEMBL4633069 | — | — | 1 | 6.85 |
| CHEMBL4642181 | — | — | 1 | 6.48 |
| CHEMBL4638783 | — | — | 1 | 5.10 |
| CHEMBL4648729 | — | — | 1 | - |
| CHEMBL4638611 | — | — | 1 | - |
| CHEMBL4646469 | — | — | 1 | - |
| CHEMBL4639891 | — | — | 1 | - |
| CHEMBL4637487 | — | — | 1 | - |
| CHEMBL4642587 | — | — | 1 | - |
| CHEMBL4637172 | — | — | 1 | - |
| CHEMBL4642089 | — | — | 1 | - |
| CHEMBL4632839 | — | — | 1 | - |
| CHEMBL4642128 | — | — | 1 | - |
| CHEMBL4638092 | — | — | 1 | - |
| CHEMBL4637818 | — | — | 1 | - |
| CHEMBL4649103 | — | — | 1 | - |
| CHEMBL4638350 | — | — | 1 | - |
| CHEMBL4649346 | — | — | 1 | - |
| CHEMBL4643586 | — | — | 1 | - |
| CHEMBL4635318 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255863 | NILOTINIB | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4633069 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4642181 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL4638783 | — | IC50 | = | 7950.0 | nM | 5.10 |
| CHEMBL4648729 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638611 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4646469 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639891 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637487 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4642587 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637172 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4642089 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4632839 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4642128 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638092 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637818 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649103 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638350 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649346 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643586 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4635318 | — | IC50 | > | 10000.0 | nM | - |