Assay Detail
Binding
CHEMBL4043711
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Inhibition of HIV1 protease using fluorogenic substrate by continuous fluorometric assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design of novel HIV-1 protease inhibitors incorporating isophthalamide-derived P2-P3 ligands: Synthesis, biological evaluation and X-ray structural studies of inhibitor-HIV-1 protease complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.93 | 10.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1323 | DARUNAVIR | 4.0 | 1 | 10.80 |
| CHEMBL3683778 | — | — | 1 | 10.60 |
| CHEMBL3683774 | — | — | 1 | 9.97 |
| CHEMBL3627879 | — | — | 1 | 9.68 |
| CHEMBL4072694 | — | — | 1 | 9.40 |
| CHEMBL4099188 | — | — | 1 | 9.39 |
| CHEMBL4096744 | — | — | 1 | 9.31 |
| CHEMBL4092187 | — | — | 1 | 9.29 |
| CHEMBL4070536 | — | — | 1 | 9.28 |
| CHEMBL3683757 | — | — | 1 | 9.20 |
| CHEMBL4069842 | — | — | 1 | 9.19 |
| CHEMBL4091454 | — | — | 1 | 9.12 |
| CHEMBL4060650 | — | — | 1 | 9.10 |
| CHEMBL4081160 | — | — | 1 | 9.10 |
| CHEMBL4088865 | — | — | 1 | 8.79 |
| CHEMBL4060839 | — | — | 1 | 8.60 |
| CHEMBL3683771 | — | — | 1 | 8.29 |
| CHEMBL4089041 | — | — | 1 | 7.63 |
| CHEMBL3683777 | — | — | 1 | 7.51 |
| CHEMBL3683772 | — | — | 1 | 7.16 |
| CHEMBL3683775 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1323 | DARUNAVIR | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL3683778 | — | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL3683774 | — | Ki | = | 0.107 | nM | 9.97 |
| CHEMBL3627879 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL4072694 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4099188 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL4096744 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL4092187 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL4070536 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL3683757 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL4069842 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL4091454 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL4060650 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL4081160 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL4088865 | — | Ki | = | 1.61 | nM | 8.79 |
| CHEMBL4060839 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3683771 | — | Ki | = | 5.08 | nM | 8.29 |
| CHEMBL4089041 | — | Ki | = | 23.6 | nM | 7.63 |
| CHEMBL3683777 | — | Ki | = | 30.8 | nM | 7.51 |
| CHEMBL3683772 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3683775 | — | Ki | = | 629.0 | nM | 6.20 |