Assay Detail
Binding
CHEMBL1647334
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Inhibition of LFA1/ICAM1 interaction in human Hut-78 cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Hut-78 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Intercellular adhesion molecule (ICAM-1), Integrin alpha-L/beta-2 (CHEMBL2096661) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.15 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1644132 | — | — | 1 | 8.92 |
| CHEMBL1644129 | — | — | 1 | 8.30 |
| CHEMBL1222288 | — | — | 1 | 8.30 |
| CHEMBL1644131 | — | — | 1 | 8.15 |
| CHEMBL1644130 | — | — | 1 | 7.72 |
| CHEMBL1222022 | — | — | 1 | 7.66 |
| CHEMBL1644118 | — | — | 1 | 7.58 |
| CHEMBL1641627 | — | — | 1 | 7.52 |
| CHEMBL1644119 | — | — | 1 | 7.41 |
| CHEMBL1644125 | — | — | 1 | 7.23 |
| CHEMBL1644115 | — | — | 1 | 7.00 |
| CHEMBL1644120 | — | — | 1 | 6.85 |
| CHEMBL1644133 | — | — | 1 | 6.82 |
| CHEMBL1644123 | — | — | 1 | 6.77 |
| CHEMBL1644127 | — | — | 1 | 6.60 |
| CHEMBL1644126 | — | — | 1 | 6.51 |
| CHEMBL1644121 | — | — | 1 | 6.37 |
| CHEMBL1644122 | — | — | 1 | 6.25 |
| CHEMBL1644114 | — | — | 1 | 6.09 |
| CHEMBL1644113 | — | — | 1 | 6.09 |
| CHEMBL1644134 | — | — | 1 | 6.00 |
| CHEMBL1644124 | — | — | 1 | - |
| CHEMBL1644128 | — | — | 1 | - |
| CHEMBL1644117 | — | — | 1 | - |
| CHEMBL1644116 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1644132 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1644129 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1222288 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1644131 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1644130 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1222022 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1644118 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1641627 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1644119 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1644125 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1644115 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1644120 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1644133 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1644123 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1644127 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1644126 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1644121 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1644122 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1644114 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL1644113 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL1644134 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1644124 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1644128 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1644117 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1644116 | — | IC50 | > | 1000.0 | nM | - |