Assay Detail
Binding
CHEMBL4397105
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as LTR-driven gene expression incubated for 48 hr by FACSCalibur flow cytometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Protein Tat (CHEMBL4011) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1) |
Publication
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.54 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | 6.89 |
| CHEMBL343448 | ROMIDEPSIN | 4.0 | 1 | 6.66 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 5.64 |
| CHEMBL4446565 | — | — | 1 | 5.51 |
| CHEMBL2132936 | — | — | 1 | 5.09 |
| CHEMBL4540359 | — | — | 1 | 5.00 |
| CHEMBL4460170 | — | — | 1 | 4.96 |
| CHEMBL4445805 | — | — | 1 | 4.60 |
| CHEMBL4583543 | — | — | 1 | - |
| CHEMBL4467303 | — | — | 1 | - |
| CHEMBL4549436 | — | — | 1 | - |
| CHEMBL4435131 | — | — | 1 | - |
| CHEMBL4552693 | — | — | 1 | - |
| CHEMBL4465202 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483254 | PANOBINOSTAT | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL343448 | ROMIDEPSIN | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL98 | VORINOSTAT | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4446565 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2132936 | — | EC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL4540359 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4460170 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4445805 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4583543 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4467303 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4549436 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4435131 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4552693 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4465202 | — | EC50 | > | 40000.0 | nM | - |