Assay Detail
Binding
CHEMBL903665
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Inhibition of HIV1 integrase strand transfer activity
40
Total Activities
40
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
Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 5.07 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL389930 | — | — | 1 | 6.42 |
| CHEMBL225681 | — | — | 1 | 6.28 |
| CHEMBL218227 | S-1360 | 2.0 | 1 | 6.22 |
| CHEMBL226490 | — | — | 1 | 5.77 |
| CHEMBL226485 | — | — | 1 | 5.57 |
| CHEMBL226484 | — | — | 1 | 5.52 |
| CHEMBL375484 | — | — | 1 | 5.32 |
| CHEMBL375956 | — | — | 1 | 5.16 |
| CHEMBL226434 | — | — | 1 | 5.16 |
| CHEMBL226489 | — | — | 1 | 4.89 |
| CHEMBL225682 | — | — | 1 | 4.80 |
| CHEMBL389881 | — | — | 1 | 4.64 |
| CHEMBL226433 | — | — | 1 | 4.57 |
| CHEMBL389931 | — | — | 1 | 4.46 |
| CHEMBL3706873 | — | — | 1 | 4.21 |
| CHEMBL226374 | — | — | 1 | 4.19 |
| CHEMBL225669 | — | — | 1 | 4.11 |
| CHEMBL387679 | — | — | 1 | 4.00 |
| CHEMBL225661 | — | — | 1 | - |
| CHEMBL225725 | — | — | 1 | - |
| CHEMBL387677 | — | — | 1 | - |
| CHEMBL226257 | — | — | 1 | - |
| CHEMBL376550 | — | — | 1 | - |
| CHEMBL226432 | — | — | 1 | - |
| CHEMBL226375 | — | — | 1 | - |
| CHEMBL3706872 | — | — | 1 | - |
| CHEMBL3706871 | — | — | 1 | - |
| CHEMBL3706870 | — | — | 1 | - |
| CHEMBL226318 | — | — | 1 | - |
| CHEMBL226259 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL389930 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL225681 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL218227 | S-1360 | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL226490 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL226485 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL226484 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL375484 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL375956 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL226434 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL226489 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL225682 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL389881 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL226433 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL389931 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL3706873 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL226374 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL225669 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL387679 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL225823 | — | IC50 | = | 333000.0 | nM | - |
| CHEMBL436140 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL225666 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL225667 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL387678 | — | IC50 | = | 900000.0 | nM | - |
| CHEMBL225723 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL225724 | — | IC50 | = | 400000.0 | nM | - |
| CHEMBL387894 | — | IC50 | = | 203000.0 | nM | - |
| CHEMBL226473 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL226258 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL226259 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL226318 | — | IC50 | = | 415000.0 | nM | - |
| CHEMBL3706870 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3706871 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3706872 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL226375 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL226432 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL376550 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL226257 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL387677 | — | IC50 | = | 109000.0 | nM | - |
| CHEMBL225725 | — | IC50 | = | 267000.0 | nM | - |
| CHEMBL225661 | — | IC50 | > | 500000.0 | nM | - |