Assay Detail
Binding
CHEMBL4397086
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of Tat-mediated HIV1 transcription in HEK293- FlpIn-FM cells harboring LTR driven CBR reporter co-expressing CMV driven CBG reporter assessed as LTR-driven gene expression incubated for 48 hr using Chroma-Glo substrate by luciferase dual reporter cellular assay
102
Total Activities
102
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 | 102 | 5.34 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4526214 | — | — | 1 | 6.10 |
| CHEMBL4446565 | — | — | 1 | 6.05 |
| CHEMBL4457218 | — | — | 1 | 5.92 |
| CHEMBL4450433 | — | — | 1 | 5.89 |
| CHEMBL4439301 | — | — | 1 | 5.89 |
| CHEMBL4531178 | — | — | 1 | 5.85 |
| CHEMBL4582511 | — | — | 1 | 5.82 |
| CHEMBL4437258 | — | — | 1 | 5.77 |
| CHEMBL4552693 | — | — | 1 | 5.72 |
| CHEMBL4540359 | — | — | 1 | 5.66 |
| CHEMBL4463956 | — | — | 1 | 5.64 |
| CHEMBL4555472 | — | — | 1 | 5.58 |
| CHEMBL4465487 | — | — | 1 | 5.58 |
| CHEMBL4464874 | — | — | 1 | 5.57 |
| CHEMBL4450555 | — | — | 1 | 5.57 |
| CHEMBL4458012 | — | — | 1 | 5.55 |
| CHEMBL4445805 | — | — | 1 | 5.54 |
| CHEMBL4575028 | — | — | 1 | 5.54 |
| CHEMBL4576878 | — | — | 1 | 5.52 |
| CHEMBL4460170 | — | — | 1 | 5.51 |
| CHEMBL4439569 | — | — | 1 | 5.48 |
| CHEMBL4463494 | — | — | 1 | 5.44 |
| CHEMBL4465202 | — | — | 1 | 5.44 |
| CHEMBL4531268 | — | — | 1 | 5.43 |
| CHEMBL4467303 | — | — | 1 | 5.43 |
| CHEMBL4437444 | — | — | 1 | 5.37 |
| CHEMBL4435131 | — | — | 1 | 5.33 |
| CHEMBL4547664 | — | — | 1 | 5.33 |
| CHEMBL4445251 | — | — | 1 | 5.33 |
| CHEMBL4522266 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4526214 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4446565 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4457218 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4450433 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4439301 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4531178 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4582511 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4437258 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4552693 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4540359 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4463956 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4465487 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4555472 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4464874 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4450555 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4458012 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4445805 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4575028 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4576878 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4460170 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4439569 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4465202 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4463494 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4531268 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4467303 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4437444 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4547664 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4522266 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4445251 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4435131 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4559333 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4532989 | — | EC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL4528111 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4439266 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1386792 | — | EC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4546726 | — | EC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4441342 | — | EC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4585376 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4549436 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4538496 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4586673 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4464671 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4446113 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4464472 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4436830 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4519327 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4447567 | — | EC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4583543 | — | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4534433 | — | EC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4541346 | — | EC50 | > | 40000.0 | nM | - |