Assay Detail
Binding
CHEMBL907140
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Inhibition of HIV integrase by strand transfer assay
15
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Human immunodeficiency virus type 1 integrase (CHEMBL3471) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.18 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216874 | — | — | 1 | 8.00 |
| CHEMBL386710 | — | — | 3 | 7.70 |
| CHEMBL386515 | — | — | 1 | 7.30 |
| CHEMBL217020 | — | — | 1 | 7.30 |
| CHEMBL217285 | — | — | 1 | 7.22 |
| CHEMBL217566 | — | — | 1 | 7.22 |
| CHEMBL385951 | — | — | 1 | 7.16 |
| CHEMBL216317 | — | — | 1 | 7.10 |
| CHEMBL437708 | — | — | 1 | 7.07 |
| CHEMBL407451 | — | — | 1 | 6.70 |
| CHEMBL216373 | — | — | 1 | 6.70 |
| CHEMBL217776 | — | — | 1 | 6.70 |
| CHEMBL216389 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216874 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL386710 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL386710 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL386515 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL217020 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL217285 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL217566 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL386710 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL385951 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL216317 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL437708 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL407451 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL216373 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL217776 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL216389 | — | IC50 | = | 210.0 | nM | 6.68 |