Assay Detail
Binding
CHEMBL890063
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Inhibition of HIV1 integrase strand transfer activity
31
Total Activities
31
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 | Autocuration |
Target
Human immunodeficiency virus type 1 integrase (CHEMBL3471) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.84 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216874 | — | — | 1 | 8.00 |
| CHEMBL232226 | — | — | 1 | 8.00 |
| CHEMBL232446 | — | — | 1 | 8.00 |
| CHEMBL232228 | — | — | 1 | 7.70 |
| CHEMBL226916 | — | — | 1 | 7.70 |
| CHEMBL390433 | — | — | 1 | 7.70 |
| CHEMBL232444 | — | — | 1 | 7.70 |
| CHEMBL234707 | — | — | 1 | 7.52 |
| CHEMBL437361 | — | — | 1 | 7.40 |
| CHEMBL232629 | — | — | 1 | 7.40 |
| CHEMBL232630 | — | — | 1 | 7.30 |
| CHEMBL438113 | — | — | 1 | 7.30 |
| CHEMBL232227 | — | — | 1 | 7.30 |
| CHEMBL277754 | — | — | 1 | 7.16 |
| CHEMBL398211 | — | — | 1 | 7.16 |
| CHEMBL437708 | — | — | 1 | 7.07 |
| CHEMBL232435 | — | — | 1 | 7.05 |
| CHEMBL388419 | — | — | 1 | 7.00 |
| CHEMBL232437 | — | — | 1 | 6.96 |
| CHEMBL389093 | — | — | 1 | 6.89 |
| CHEMBL232445 | — | — | 1 | 6.80 |
| CHEMBL232025 | — | — | 1 | 6.70 |
| CHEMBL234922 | — | — | 1 | 6.68 |
| CHEMBL232436 | — | — | 1 | 6.26 |
| CHEMBL234923 | — | — | 1 | 6.21 |
| CHEMBL234921 | — | — | 1 | 6.21 |
| CHEMBL373760 | — | — | 1 | 6.00 |
| CHEMBL388420 | — | — | 1 | 5.60 |
| CHEMBL232024 | — | — | 1 | 4.78 |
| CHEMBL398210 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216874 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL232226 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL232446 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL232228 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL226916 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL390433 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL232444 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL234707 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL437361 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL232629 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL232630 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL438113 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL232227 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL277754 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL398211 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL437708 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL232435 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL388419 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL232437 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL389093 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL232445 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL232025 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL234922 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL232436 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL234923 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL234921 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL373760 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL388420 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL232024 | — | IC50 | = | 16600.0 | nM | 4.78 |
| CHEMBL398210 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL373761 | — | IC50 | = | 50000.0 | nM | 4.30 |