Assay Detail
Binding
CHEMBL4236899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay
30
Total Activities
29
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 | Intermediate |
Publication
Discovery of ( S)-3-(3-(3,5-Dimethyl-1 H-pyrazol-1-yl)phenyl)-4-(( R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 8.27 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4237498 | — | — | 1 | 9.00 |
| CHEMBL4246111 | — | — | 1 | 8.80 |
| CHEMBL4243686 | — | — | 1 | 8.80 |
| CHEMBL4243367 | — | — | 1 | 8.80 |
| CHEMBL4249172 | — | — | 1 | 8.80 |
| CHEMBL4244784 | — | — | 2 | 8.70 |
| CHEMBL4245368 | — | — | 1 | 8.70 |
| CHEMBL4251444 | — | — | 1 | 8.60 |
| CHEMBL4242732 | — | — | 1 | 8.60 |
| CHEMBL4239085 | — | — | 1 | 8.60 |
| CHEMBL4249629 | — | — | 1 | 8.60 |
| CHEMBL4240155 | — | — | 1 | 8.60 |
| CHEMBL4241584 | — | — | 1 | 8.50 |
| CHEMBL4238909 | — | — | 1 | 8.40 |
| CHEMBL4248589 | — | — | 1 | 8.40 |
| CHEMBL4237919 | — | — | 1 | 8.40 |
| CHEMBL4237868 | — | — | 1 | 8.40 |
| CHEMBL4242175 | — | — | 1 | 8.40 |
| CHEMBL4241824 | GSK-3008348 FREE BASE | 1.0 | 1 | 8.40 |
| CHEMBL4242635 | — | — | 1 | 8.40 |
| CHEMBL4247149 | — | — | 1 | 8.40 |
| CHEMBL4245829 | — | — | 1 | 8.20 |
| CHEMBL4250148 | — | — | 1 | 8.10 |
| CHEMBL4242263 | — | — | 1 | 8.10 |
| CHEMBL4238556 | — | — | 1 | 7.90 |
| CHEMBL4247617 | — | — | 1 | 7.40 |
| CHEMBL4238482 | — | — | 1 | 7.30 |
| CHEMBL4239588 | — | — | 1 | 6.80 |
| CHEMBL4248953 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4237498 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4246111 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4243686 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4243367 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4249172 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4244784 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4244784 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4245368 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4240155 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4242732 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4239085 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4251444 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4249629 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4241584 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4247149 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4248589 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4237919 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4237868 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4242635 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4241824 | GSK-3008348 FREE BASE | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4238909 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4242175 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4245829 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4250148 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4242263 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4238556 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4247617 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4238482 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4239588 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4248953 | — | IC50 | = | 6309.57 | nM | 5.20 |