Assay Detail
Binding
CHEMBL4332388
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Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA
16
Total Activities
16
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 reverse transcriptase (CHEMBL247) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.60 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 8.15 |
| CHEMBL2364608 | DORAVIRINE | 4.0 | 1 | 7.72 |
| CHEMBL4448359 | — | — | 1 | 6.28 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 6.22 |
| CHEMBL4461473 | — | — | 1 | 6.03 |
| CHEMBL4471313 | — | — | 1 | 6.00 |
| CHEMBL4530139 | — | — | 1 | 5.90 |
| CHEMBL4467417 | — | — | 1 | 5.90 |
| CHEMBL4577434 | — | — | 1 | 5.68 |
| CHEMBL4469538 | — | — | 1 | 4.71 |
| CHEMBL4434794 | — | — | 1 | 4.52 |
| CHEMBL4579228 | — | — | 1 | 4.49 |
| CHEMBL4582364 | — | — | 1 | 4.20 |
| CHEMBL4453611 | — | — | 1 | 4.14 |
| CHEMBL4576491 | — | — | 1 | 4.03 |
| CHEMBL4550743 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL223228 | EFAVIRENZ | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2364608 | DORAVIRINE | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4448359 | — | IC50 | = | 522.0 | nM | 6.28 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 595.0 | nM | 6.22 |
| CHEMBL4461473 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4471313 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4530139 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4467417 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4577434 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL4469538 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL4434794 | — | IC50 | = | 30100.0 | nM | 4.52 |
| CHEMBL4579228 | — | IC50 | = | 32500.0 | nM | 4.49 |
| CHEMBL4582364 | — | IC50 | = | 63400.0 | nM | 4.20 |
| CHEMBL4453611 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL4576491 | — | IC50 | = | 92500.0 | nM | 4.03 |
| CHEMBL4550743 | — | IC50 | = | 133000.0 | nM | - |