Assay Detail
Binding
CHEMBL1039956
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Inhibition of HIV1 JRFL gp120/CD4 interaction in human HeLa67 cells assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HeLa67 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug candidate that demonstrates antiviral activity in HIV-1-infected subjects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 8.25 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL238103 | — | — | 1 | 9.06 |
| CHEMBL337301 | — | — | 1 | 8.83 |
| CHEMBL585487 | — | — | 1 | 8.80 |
| CHEMBL442078 | — | — | 1 | 8.77 |
| CHEMBL567570 | — | — | 1 | 8.40 |
| CHEMBL583867 | — | — | 1 | 7.67 |
| CHEMBL585498 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL238103 | — | EC50 | = | 0.88 | nM | 9.06 |
| CHEMBL337301 | — | EC50 | = | 1.47 | nM | 8.83 |
| CHEMBL585487 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL442078 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL567570 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL583867 | — | EC50 | = | 21.6 | nM | 7.67 |
| CHEMBL585498 | — | EC50 | = | 575.9 | nM | 6.24 |