Assay Detail
Binding
CHEMBL4187320
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Inhibition of recombinant wild-type HIV-1 3B reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis
22
Total Activities
22
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 |
Target
Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Structural optimization of N1-aryl-benzimidazoles for the discovery of new non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.86 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 7.72 |
| CHEMBL4218333 | — | — | 1 | 7.33 |
| CHEMBL4203336 | — | — | 1 | 7.30 |
| CHEMBL4211084 | — | — | 1 | 7.06 |
| CHEMBL4211907 | — | — | 1 | 7.04 |
| CHEMBL3114049 | — | — | 1 | 6.92 |
| CHEMBL4207026 | — | — | 1 | 6.89 |
| CHEMBL3114034 | — | — | 1 | 6.75 |
| CHEMBL4202681 | — | — | 1 | 6.65 |
| CHEMBL4218422 | — | — | 1 | 6.12 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.81 |
| CHEMBL4210982 | — | — | 1 | 5.26 |
| CHEMBL4204242 | — | — | 1 | 5.23 |
| CHEMBL4211390 | — | — | 1 | 5.12 |
| CHEMBL4213853 | — | — | 1 | 4.80 |
| CHEMBL4214858 | — | — | 1 | 4.80 |
| CHEMBL3114032 | — | — | 1 | 4.73 |
| CHEMBL4203211 | — | — | 1 | 4.67 |
| CHEMBL4205972 | — | — | 1 | 4.33 |
| CHEMBL3114057 | — | — | 1 | 4.29 |
| CHEMBL4216358 | — | — | 1 | 4.22 |
| CHEMBL3114045 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL223228 | EFAVIRENZ | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4218333 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4203336 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4211084 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4211907 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3114049 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4207026 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3114034 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4202681 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL4218422 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4210982 | — | IC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL4204242 | — | IC50 | = | 5840.0 | nM | 5.23 |
| CHEMBL4211390 | — | IC50 | = | 7680.0 | nM | 5.12 |
| CHEMBL4213853 | — | IC50 | = | 15740.0 | nM | 4.80 |
| CHEMBL4214858 | — | IC50 | = | 15670.0 | nM | 4.80 |
| CHEMBL3114032 | — | IC50 | = | 18510.0 | nM | 4.73 |
| CHEMBL4203211 | — | IC50 | = | 21340.0 | nM | 4.67 |
| CHEMBL4205972 | — | IC50 | = | 47300.0 | nM | 4.33 |
| CHEMBL3114057 | — | IC50 | = | 51930.0 | nM | 4.29 |
| CHEMBL4216358 | — | IC50 | = | 60610.0 | nM | 4.22 |
| CHEMBL3114045 | — | IC50 | = | 162170.0 | nM | - |