Assay Detail
Binding
CHEMBL4670813
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CPM binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by CPM addition and measured after 1 hr by fluorescence assay
42
Total Activities
38
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transcriptional enhancer factor TEF-3 (CHEMBL4295828) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 5.41 | 6.16 |
| Inhibition | 4 | - | - |
| Ki | 1 | 4.98 | 4.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787565 | — | — | 1 | 6.16 |
| CHEMBL4763473 | — | — | 3 | 6.10 |
| CHEMBL4757924 | — | — | 1 | 6.00 |
| CHEMBL4776143 | — | — | 1 | 5.96 |
| CHEMBL4745853 | — | — | 1 | 5.92 |
| CHEMBL4757369 | — | — | 1 | 5.89 |
| CHEMBL4797833 | — | — | 1 | 5.82 |
| CHEMBL4745831 | — | — | 1 | 5.82 |
| CHEMBL4750726 | — | — | 1 | 5.77 |
| CHEMBL4789889 | — | — | 1 | 5.72 |
| CHEMBL242708 | — | — | 1 | 5.64 |
| CHEMBL4783341 | — | — | 1 | 5.62 |
| CHEMBL4744235 | — | — | 1 | 5.51 |
| CHEMBL1701986 | — | — | 2 | 5.50 |
| CHEMBL4800702 | — | — | 1 | 5.43 |
| CHEMBL4750624 | — | — | 1 | 5.40 |
| CHEMBL4750499 | — | — | 1 | 5.06 |
| CHEMBL4797545 | — | — | 1 | 5.04 |
| CHEMBL4784286 | — | — | 1 | 4.88 |
| CHEMBL4778316 | — | — | 1 | 4.78 |
| CHEMBL4757939 | — | — | 1 | 4.72 |
| CHEMBL63323 | NIFLUMIC ACID | 2.0 | 2 | 4.38 |
| CHEMBL3634672 | — | — | 1 | 4.37 |
| CHEMBL4751604 | — | — | 1 | 4.27 |
| CHEMBL4781890 | — | — | 1 | - |
| CHEMBL4759333 | — | — | 1 | - |
| CHEMBL4764516 | — | — | 1 | - |
| CHEMBL82293 | PALMITIC ACID | -1.0 | 1 | - |
| CHEMBL4760394 | — | — | 1 | - |
| CHEMBL4751406 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787565 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4763473 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4757924 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4776143 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4745853 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4757369 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4797833 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4745831 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4750726 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4789889 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL242708 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4783341 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4744235 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1701986 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1701986 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4800702 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4750624 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4750499 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4797545 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4763473 | — | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL4784286 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL4778316 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL4757939 | — | IC50 | = | 18900.0 | nM | 4.72 |
| CHEMBL63323 | NIFLUMIC ACID | IC50 | = | 41900.0 | nM | 4.38 |
| CHEMBL3634672 | — | IC50 | = | 43100.0 | nM | 4.37 |
| CHEMBL4751604 | — | IC50 | = | 53400.0 | nM | 4.27 |
| CHEMBL4798108 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4747774 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4786804 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4759934 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL63323 | NIFLUMIC ACID | Inhibition | - | % | - | |
| CHEMBL4763473 | — | Inhibition | - | % | - | |
| CHEMBL4740627 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4745654 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4782185 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL23588 | FLUFENAMIC ACID | Inhibition | - | % | - | |
| CHEMBL4751406 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL82293 | PALMITIC ACID | Inhibition | - | % | - | |
| CHEMBL4759333 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4781890 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4764516 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4760394 | — | IC50 | > | 100000.0 | nM | - |