Assay Detail
Binding
CHEMBL4650195
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Homogeneous Time Resolved Fluorescence (HTRF) assay. Domain start/stop: L14-Q143
4
Total Activities
4
Compounds Tested
1
Activity Types
4
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Category | HTRF assay |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
EUbOPEN bromodomain assay panel
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.34 | 7.98 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Peptide | Peptide | - | — | SGRGK(ac)GGK(ac)GLGK(ac)GGAK(ac)RHRK(biotin)-acid |
| Protein Sequence | Protein Sequence | - | — | MSPILGYWKIKGLVQPTRLLLEYLEEKYEEHLYERDEGDKWRNKKFELGLEFPNLPYYIDGDVKLTQSMAIIRYIADKHNMLGGCPKERAEISMLEGAVLDIRYGVSRIAYSKDFETLKVDFLSKLPEMLKMFEDRLCHKTYLNGDHVTHPDFMLYDALDVVLYMDPMCLDAFPKLVCFKKRIEAIPQIDKYLKSSKYIAWPLQGWQATFGGGDHPPKSSSENLYFQSMLKLSAENESTPIQQLLEHFLRQLQRKDPHGFFAFPVTDAIAPGYSMIIKHPMDFGTMKDKIVANEYKSVTEFKADFKLMCDNAMTYNRPDTVYYKLAKKILHAGFKMMSKERLLALKRSMSFMQDMDFSQ |
| Refseq Start/Stop | Refseq Start/Stop | - | — | L14-Q143 |
| Target UniProt Accession | Target UniProt Accession | - | — | Q9H8M2 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3769507 | — | — | 1 | 7.98 |
| CHEMBL3133807 | — | — | 1 | 7.33 |
| CHEMBL4065619 | — | — | 1 | 7.31 |
| CHEMBL4650212 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3769507 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL3133807 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4065619 | — | IC50 | = | 49.2 | nM | 7.31 |
| CHEMBL4650212 | — | IC50 | = | 189.0 | nM | 6.72 |