Assay Detail
Binding
CHEMBL1120949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of LFA1-mediated human T cell proliferation assessed as [3H]thymidine uptake after 4 days by mixed lymphocyte reaction assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | T-cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.75 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094115 | — | — | 1 | 7.30 |
| CHEMBL1098726 | — | — | 1 | 7.22 |
| CHEMBL1095138 | — | — | 1 | 7.16 |
| CHEMBL1098727 | — | — | 1 | 7.10 |
| CHEMBL1096039 | — | — | 1 | 7.10 |
| CHEMBL1094128 | — | — | 1 | 7.10 |
| CHEMBL1098760 | — | — | 1 | 7.00 |
| CHEMBL1094753 | — | — | 1 | 6.85 |
| CHEMBL1094116 | — | — | 1 | 6.85 |
| CHEMBL1096088 | — | — | 1 | 6.77 |
| CHEMBL1097384 | — | — | 1 | 6.70 |
| CHEMBL1099103 | — | — | 1 | 6.62 |
| CHEMBL1097733 | — | — | 1 | 6.58 |
| CHEMBL1096053 | — | — | 1 | 6.57 |
| CHEMBL1098437 | — | — | 1 | 6.55 |
| CHEMBL1098761 | — | — | 1 | 6.55 |
| CHEMBL214529 | — | — | 1 | 6.55 |
| CHEMBL1094431 | — | — | 1 | 6.51 |
| CHEMBL1094127 | — | — | 1 | 6.40 |
| CHEMBL1095148 | — | — | 1 | 6.39 |
| CHEMBL1098071 | — | — | 1 | 5.90 |
| CHEMBL1096040 | — | — | 1 | - |
| CHEMBL1095137 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094115 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1098726 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1095138 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1098727 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1096039 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1094128 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1098760 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1094753 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1094116 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1096088 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1097384 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1099103 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1097733 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1096053 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1098437 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1098761 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL214529 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1094431 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1094127 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1095148 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1098071 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL1096040 | — | IC50 | - | — | - | |
| CHEMBL1095137 | — | IC50 | - | — | - |