Assay Detail
Binding
CHEMBL797516
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro ability to inhibit mutant P236L reverse transcriptase
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.07 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268871 | L-697661 | — | 1 | 6.96 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 6.50 |
| CHEMBL8971 | — | — | 1 | 6.19 |
| CHEMBL269591 | — | — | 1 | 5.94 |
| CHEMBL929 | DELAVIRDINE MESYLATE | 4.0 | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268871 | L-697661 | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL8971 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL269591 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL929 | DELAVIRDINE MESYLATE | IC50 | = | 18000.0 | nM | 4.75 |