Assay Detail
Binding
CHEMBL5368302
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Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
GNE-235: A Lead Compound Selective for the Second Bromodomain of PBRM1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 26 | 6.54 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5428009 | — | — | 1 | 8.30 |
| CHEMBL5409404 | — | — | 1 | 8.22 |
| CHEMBL5406315 | — | — | 1 | 8.05 |
| CHEMBL5401472 | — | — | 1 | 7.82 |
| CHEMBL5431862 | — | — | 1 | 7.82 |
| CHEMBL5424811 | — | — | 1 | 7.40 |
| CHEMBL5411199 | — | — | 1 | 7.16 |
| CHEMBL5398829 | — | — | 1 | 7.05 |
| CHEMBL5426305 | — | — | 1 | 6.85 |
| CHEMBL5415064 | — | — | 1 | 6.84 |
| CHEMBL5421138 | — | — | 1 | 6.55 |
| CHEMBL5177096 | — | — | 1 | 6.52 |
| CHEMBL5425250 | — | — | 1 | 6.47 |
| CHEMBL5412292 | — | — | 1 | 6.46 |
| CHEMBL5441040 | — | — | 1 | 6.36 |
| CHEMBL5415253 | — | — | 1 | 6.25 |
| CHEMBL5415396 | — | — | 1 | 6.22 |
| CHEMBL5415837 | — | — | 1 | 6.10 |
| CHEMBL5394310 | — | — | 1 | 6.10 |
| CHEMBL5395676 | — | — | 1 | 5.85 |
| CHEMBL5396881 | — | — | 1 | 5.60 |
| CHEMBL5406457 | — | — | 1 | 5.55 |
| CHEMBL5399079 | — | — | 1 | 5.45 |
| CHEMBL5401735 | — | — | 1 | 5.10 |
| CHEMBL5402159 | — | — | 1 | 5.08 |
| CHEMBL5431005 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5428009 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL5409404 | — | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL5406315 | — | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL5401472 | — | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL5431862 | — | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL5424811 | — | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL5411199 | — | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL5398829 | — | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL5426305 | — | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL5415064 | — | Kd | = | 145.0 | nM | 6.84 |
| CHEMBL5421138 | — | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL5177096 | — | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL5425250 | — | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL5412292 | — | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL5441040 | — | Kd | = | 440.0 | nM | 6.36 |
| CHEMBL5415253 | — | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL5415396 | — | Kd | = | 600.0 | nM | 6.22 |
| CHEMBL5415837 | — | Kd | = | 800.0 | nM | 6.10 |
| CHEMBL5394310 | — | Kd | = | 800.0 | nM | 6.10 |
| CHEMBL5395676 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL5396881 | — | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL5406457 | — | Kd | = | 2800.0 | nM | 5.55 |
| CHEMBL5399079 | — | Kd | = | 3550.0 | nM | 5.45 |
| CHEMBL5401735 | — | Kd | = | 8000.0 | nM | 5.10 |
| CHEMBL5402159 | — | Kd | = | 8400.0 | nM | 5.08 |
| CHEMBL5431005 | — | Kd | = | 14000.0 | nM | 4.85 |