Assay Detail
Binding
CHEMBL4375395
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of integrin alphavbeta8 (unknown origin) expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP1 (242 to 252 amino acids) incubated for 30 mins by fluorescent probe BCECF-AM based fluorescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | K562 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Profile of a Highly Selective Quaternized Pyrrolidine Betaine α<sub>v</sub>β<sub>6</sub> Integrin Inhibitor-(3<i>S</i>)-3-(3-(3,5-Dimethyl-1<i>H</i>-pyrazol-1-yl)phenyl)-4-((1<i>S</i> and 1<i>R</i>,3<i>R</i>)-1-methyl-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-ium-1-yl)butanoate Synthesized by Stereoselective Methylation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.24 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4446267 | — | — | 1 | 8.00 |
| CHEMBL4239085 | — | — | 1 | 8.00 |
| CHEMBL4246089 | GSK-3008348 | 1.0 | 1 | 7.80 |
| CHEMBL4238909 | — | — | 1 | 7.80 |
| CHEMBL4573716 | — | — | 1 | 7.20 |
| CHEMBL4468357 | — | — | 1 | 7.10 |
| CHEMBL4593110 | — | — | 1 | 7.00 |
| CHEMBL4446786 | — | — | 1 | 6.90 |
| CHEMBL4589933 | — | — | 1 | 6.70 |
| CHEMBL4516070 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4446267 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4239085 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4246089 | GSK-3008348 | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4238909 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4573716 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4468357 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4593110 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4446786 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4589933 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4516070 | — | IC50 | = | 1258.93 | nM | 5.90 |