Assay Detail
Binding
CHEMBL4136669
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Inhibition of HIV1 protease expressed in Escherichia coli using Val-Ser-Gln-Asn-(beta-naphtyl)Ala-Pro-Ile-Val as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by mass spectrometric method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 10.34 | 10.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4177355 | — | — | 1 | 10.92 |
| CHEMBL1323 | DARUNAVIR | 4.0 | 1 | 10.89 |
| CHEMBL1163 | ATAZANAVIR | 4.0 | 1 | 10.40 |
| CHEMBL3828743 | — | — | 1 | 9.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4177355 | — | IC50 | = | 0.012 | nM | 10.92 |
| CHEMBL1323 | DARUNAVIR | IC50 | = | 0.013 | nM | 10.89 |
| CHEMBL1163 | ATAZANAVIR | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3828743 | — | IC50 | = | 0.7 | nM | 9.15 |