Assay Detail
Functional
CHEMBL1268149
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Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Human immunodeficiency virus 1 |
| Cell Type | MT4 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Target
Human immunodeficiency virus 1 (CHEMBL378) ↗| Type | ORGANISM |
| Organism | Human immunodeficiency virus 1 |
Publication
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 7.50 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18442 | PLERIXAFOR | 4.0 | 1 | 8.10 |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 8.00 |
| CHEMBL204656 | ELVITEGRAVIR | 4.0 | 1 | 7.82 |
| CHEMBL414850 | — | — | 1 | 7.75 |
| CHEMBL129 | ZIDOVUDINE | 4.0 | 1 | 7.66 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 7.41 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 6.96 |
| CHEMBL259011 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18442 | PLERIXAFOR | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL254316 | RALTEGRAVIR | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL204656 | ELVITEGRAVIR | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL414850 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL129 | ZIDOVUDINE | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL163 | RITONAVIR | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL57 | NEVIRAPINE | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL259011 | — | EC50 | = | 520.0 | nM | 6.28 |