Assay Detail
Binding
CHEMBL3583194
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Inhibition of HIV-1 integrase assessed as inhibition of 3'-processing activity using 32P-labeled DNA as substrate after 1 hr by gel-based assay in presence of Mg2+
39
Total Activities
39
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
N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.19 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497501 | — | — | 1 | 6.70 |
| CHEMBL2236601 | RDS-1984 | — | 1 | 6.16 |
| CHEMBL3582052 | — | — | 1 | 5.97 |
| CHEMBL3582057 | — | — | 1 | 5.92 |
| CHEMBL3582070 | — | — | 1 | 5.76 |
| CHEMBL3582056 | — | — | 1 | 5.40 |
| CHEMBL2236599 | — | — | 1 | 5.34 |
| CHEMBL204656 | ELVITEGRAVIR | 4.0 | 1 | 5.09 |
| CHEMBL3582072 | — | — | 1 | 5.01 |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 4.89 |
| CHEMBL3582080 | — | — | 1 | 4.75 |
| CHEMBL3582073 | — | — | 1 | 4.69 |
| CHEMBL3582071 | — | — | 1 | 4.68 |
| CHEMBL3582058 | — | — | 1 | 4.66 |
| CHEMBL3582061 | — | — | 1 | 4.57 |
| CHEMBL3582060 | — | — | 1 | 4.55 |
| CHEMBL3582082 | — | — | 1 | 4.16 |
| CHEMBL3582043 | — | — | 1 | - |
| CHEMBL3582041 | — | — | 1 | - |
| CHEMBL3582042 | — | — | 1 | - |
| CHEMBL2236603 | RDS-2161 | — | 1 | - |
| CHEMBL3582040 | — | — | 1 | - |
| CHEMBL2236602 | — | — | 1 | - |
| CHEMBL498713 | — | — | 1 | - |
| CHEMBL3582038 | — | — | 1 | - |
| CHEMBL3582039 | — | — | 1 | - |
| CHEMBL2236589 | 20, RDS-2163 | — | 1 | - |
| CHEMBL2236598 | RDS-1624 | — | 1 | - |
| CHEMBL2236600 | — | — | 1 | - |
| CHEMBL3582053 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497501 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2236601 | RDS-1984 | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3582052 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL3582057 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3582070 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL3582056 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2236599 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL204656 | ELVITEGRAVIR | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL3582072 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL3582080 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3582073 | — | IC50 | = | 20500.0 | nM | 4.69 |
| CHEMBL3582071 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3582058 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3582061 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL3582060 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3582082 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL3582081 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3582079 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL3582078 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3582077 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL3582076 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL3582075 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL3582059 | — | IC50 | > | 37000.0 | nM | - |
| CHEMBL2236588 | — | IC50 | > | 4100.0 | nM | - |
| CHEMBL3582054 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL3582053 | — | IC50 | = | 266000.0 | nM | - |
| CHEMBL2236600 | — | IC50 | > | 12300.0 | nM | - |
| CHEMBL2236598 | RDS-1624 | IC50 | > | 12300.0 | nM | - |
| CHEMBL2236589 | 20, RDS-2163 | IC50 | > | 333000.0 | nM | - |
| CHEMBL3582039 | — | IC50 | = | 125000.0 | nM | - |
| CHEMBL3582038 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL498713 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2236602 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL3582040 | — | IC50 | > | 37000.0 | nM | - |
| CHEMBL2236603 | RDS-2161 | IC50 | > | 4100.0 | nM | - |
| CHEMBL3582042 | — | IC50 | > | 37000.0 | nM | - |
| CHEMBL3582041 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL3582043 | — | IC50 | > | 37000.0 | nM | - |