Assay Detail
Binding
CHEMBL4052392
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Inhibition of HIV1 3B reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay
51
Total Activities
51
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
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 51 | 7.23 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4094163 | — | — | 1 | 8.57 |
| CHEMBL3929927 | — | — | 1 | 8.37 |
| CHEMBL4066621 | — | — | 1 | 8.33 |
| CHEMBL129 | ZIDOVUDINE | 4.0 | 1 | 8.32 |
| CHEMBL4059713 | — | — | 1 | 8.23 |
| CHEMBL4075243 | — | — | 1 | 8.10 |
| CHEMBL4084357 | — | — | 1 | 8.06 |
| CHEMBL4090492 | — | — | 1 | 8.06 |
| CHEMBL4062507 | — | — | 1 | 8.05 |
| CHEMBL4101895 | — | — | 1 | 7.97 |
| CHEMBL4088003 | — | — | 1 | 7.83 |
| CHEMBL4090441 | — | — | 1 | 7.64 |
| CHEMBL4085465 | — | — | 1 | 7.60 |
| CHEMBL4060732 | — | — | 1 | 7.58 |
| CHEMBL4080133 | — | — | 1 | 7.57 |
| CHEMBL308954 | ETRAVIRINE | 4.0 | 1 | 7.53 |
| CHEMBL4104988 | — | — | 1 | 7.49 |
| CHEMBL4082607 | — | — | 1 | 7.42 |
| CHEMBL4083835 | — | — | 1 | 7.39 |
| CHEMBL4101836 | — | — | 1 | 7.25 |
| CHEMBL4094991 | — | — | 1 | 7.21 |
| CHEMBL4078474 | — | — | 1 | 7.17 |
| CHEMBL4102745 | — | — | 1 | 7.14 |
| CHEMBL4078540 | — | — | 1 | 7.07 |
| CHEMBL4086331 | — | — | 1 | 7.05 |
| CHEMBL4077355 | — | — | 1 | 7.03 |
| CHEMBL4096564 | — | — | 1 | 6.99 |
| CHEMBL4067573 | — | — | 1 | 6.97 |
| CHEMBL4076005 | — | — | 1 | 6.97 |
| CHEMBL4069411 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4094163 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3929927 | — | EC50 | = | 4.25 | nM | 8.37 |
| CHEMBL4066621 | — | EC50 | = | 4.67 | nM | 8.33 |
| CHEMBL129 | ZIDOVUDINE | EC50 | = | 4.79 | nM | 8.32 |
| CHEMBL4059713 | — | EC50 | = | 5.82 | nM | 8.23 |
| CHEMBL4075243 | — | EC50 | = | 7.89 | nM | 8.10 |
| CHEMBL4084357 | — | EC50 | = | 8.73 | nM | 8.06 |
| CHEMBL4090492 | — | EC50 | = | 8.68 | nM | 8.06 |
| CHEMBL4062507 | — | EC50 | = | 8.85 | nM | 8.05 |
| CHEMBL4101895 | — | EC50 | = | 10.8 | nM | 7.97 |
| CHEMBL4088003 | — | EC50 | = | 14.8 | nM | 7.83 |
| CHEMBL4090441 | — | EC50 | = | 22.7 | nM | 7.64 |
| CHEMBL4085465 | — | EC50 | = | 25.2 | nM | 7.60 |
| CHEMBL4060732 | — | EC50 | = | 26.3 | nM | 7.58 |
| CHEMBL4080133 | — | EC50 | = | 26.7 | nM | 7.57 |
| CHEMBL308954 | ETRAVIRINE | EC50 | = | 29.4 | nM | 7.53 |
| CHEMBL4104988 | — | EC50 | = | 32.4 | nM | 7.49 |
| CHEMBL4082607 | — | EC50 | = | 37.8 | nM | 7.42 |
| CHEMBL4083835 | — | EC50 | = | 40.6 | nM | 7.39 |
| CHEMBL4101836 | — | EC50 | = | 56.9 | nM | 7.25 |
| CHEMBL4094991 | — | EC50 | = | 61.4 | nM | 7.21 |
| CHEMBL4078474 | — | EC50 | = | 68.3 | nM | 7.17 |
| CHEMBL4102745 | — | EC50 | = | 72.3 | nM | 7.14 |
| CHEMBL4078540 | — | EC50 | = | 85.2 | nM | 7.07 |
| CHEMBL4086331 | — | EC50 | = | 89.5 | nM | 7.05 |
| CHEMBL4077355 | — | EC50 | = | 93.6 | nM | 7.03 |
| CHEMBL4096564 | — | EC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4067573 | — | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4076005 | — | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4069411 | — | EC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4094095 | — | EC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4093229 | — | EC50 | = | 263.0 | nM | 6.58 |
| CHEMBL223228 | EFAVIRENZ | EC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4085345 | — | EC50 | = | 646.0 | nM | 6.19 |
| CHEMBL4075094 | — | EC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL4062672 | — | EC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4061597 | — | EC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL4072495 | — | EC50 | = | 3680.0 | nM | 5.43 |
| CHEMBL4100811 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4063892 | — | EC50 | > | 4930.0 | nM | - |
| CHEMBL4095529 | — | EC50 | > | 3450.0 | nM | - |
| CHEMBL4089725 | — | EC50 | > | 2770.0 | nM | - |
| CHEMBL4079259 | — | EC50 | > | 5150.0 | nM | - |
| CHEMBL4061608 | — | EC50 | > | 20100.0 | nM | - |
| CHEMBL4093101 | — | EC50 | >= | 4160.0 | nM | - |
| CHEMBL57 | NEVIRAPINE | EC50 | > | 15000.0 | nM | - |
| CHEMBL4065430 | — | EC50 | >= | 5260.0 | nM | - |
| CHEMBL4074049 | — | EC50 | > | 3690.0 | nM | - |
| CHEMBL4097283 | — | EC50 | > | 707.0 | nM | - |
| CHEMBL4089717 | — | EC50 | > | 1170.0 | nM | - |