Assay Detail
ADMET
CHEMBL4397085
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Activation of non-specific gene expression in HEK293- FlpIn-FM cells harboring LTR driven CBR reporter co-expressing CMV driven CBG reporter assessed as CMV driven gene expression incubated for 48 hr using Chroma-Glo substrate by luciferase dual reporter cellular assay
103
Total Activities
102
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
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 | 103 | 4.96 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4446565 | — | — | 1 | 5.70 |
| CHEMBL4437258 | — | — | 1 | 5.68 |
| CHEMBL4526214 | — | — | 1 | 5.57 |
| CHEMBL4450433 | — | — | 1 | 5.54 |
| CHEMBL4576878 | — | — | 1 | 5.41 |
| CHEMBL4531268 | — | — | 1 | 5.40 |
| CHEMBL4465487 | — | — | 1 | 5.39 |
| CHEMBL4458012 | — | — | 1 | 5.30 |
| CHEMBL4460170 | — | — | 1 | 5.24 |
| CHEMBL4457218 | — | — | 1 | 5.21 |
| CHEMBL4528111 | — | — | 1 | 5.15 |
| CHEMBL4445251 | — | — | 1 | 5.14 |
| CHEMBL4575028 | — | — | 1 | 5.08 |
| CHEMBL4582511 | — | — | 1 | 5.00 |
| CHEMBL4437444 | — | — | 1 | 4.96 |
| CHEMBL4532989 | — | — | 1 | 4.85 |
| CHEMBL4540359 | — | — | 1 | 4.82 |
| CHEMBL4465202 | — | — | 1 | 4.58 |
| CHEMBL4519327 | — | — | 1 | 4.57 |
| CHEMBL4450555 | — | — | 1 | 4.51 |
| CHEMBL4439266 | — | — | 1 | 4.50 |
| CHEMBL4586673 | — | — | 1 | 4.50 |
| CHEMBL4464874 | — | — | 2 | 4.47 |
| CHEMBL4464671 | — | — | 1 | 4.47 |
| CHEMBL4446113 | — | — | 1 | 4.42 |
| CHEMBL4436830 | — | — | 1 | 4.41 |
| CHEMBL4547664 | — | — | 1 | 4.41 |
| CHEMBL4583543 | — | — | 1 | - |
| CHEMBL4464472 | — | — | 1 | - |
| CHEMBL4570111 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4446565 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4437258 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4526214 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4450433 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4576878 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4531268 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4465487 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4458012 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4460170 | — | EC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4457218 | — | EC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4528111 | — | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4445251 | — | EC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4575028 | — | EC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4582511 | — | EC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4437444 | — | EC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL4532989 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4540359 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4465202 | — | EC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4519327 | — | EC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4450555 | — | EC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4586673 | — | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4439266 | — | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4464874 | — | EC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4464671 | — | EC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4464874 | — | EC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4446113 | — | EC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL4436830 | — | EC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL4547664 | — | EC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL4545696 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4450163 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4554681 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4454101 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4466564 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4445805 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4579415 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4541304 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4454779 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4442612 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4470014 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4475991 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL1506392 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4541893 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4546726 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL1386792 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4435131 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4552693 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4452854 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4462844 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4453396 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4553355 | — | EC50 | > | 40000.0 | nM | - |