Assay Detail
Binding
CHEMBL4835526
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Binding affinity to human recombinant His-tagged Keap1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by surface plasmon resonance method
18
Total Activities
18
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 |
Target
Kelch-like ECH-associated protein 1 (CHEMBL2069156) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 18 | 3.05 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4865680 | — | — | 1 | 5.54 |
| CHEMBL4871793 | — | — | 1 | 3.66 |
| CHEMBL4876857 | — | — | 1 | 3.38 |
| CHEMBL4849223 | — | — | 1 | 3.15 |
| CHEMBL181686 | — | — | 1 | 3.02 |
| CHEMBL4859873 | — | — | 1 | 3.00 |
| CHEMBL193664 | — | — | 1 | 3.00 |
| CHEMBL83148 | PHENYL(PHENYLSULFONYL)AMINE | — | 1 | 2.96 |
| CHEMBL4867889 | — | — | 1 | 2.96 |
| CHEMBL1945331 | — | — | 1 | 2.92 |
| CHEMBL57394 | — | — | 1 | 2.92 |
| CHEMBL4879253 | — | — | 1 | 2.85 |
| CHEMBL4870439 | — | — | 1 | 2.82 |
| CHEMBL1452067 | — | — | 1 | 2.70 |
| CHEMBL4856558 | — | — | 1 | 2.64 |
| CHEMBL851 | PHENYL PROPIONIC ACID | — | 1 | 2.50 |
| CHEMBL24367 | — | — | 1 | 2.43 |
| CHEMBL3086212 | — | — | 1 | 2.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4865680 | — | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL4871793 | — | Kd | = | 220000.0 | nM | 3.66 |
| CHEMBL4876857 | — | Kd | = | 420000.0 | nM | 3.38 |
| CHEMBL4849223 | — | Kd | = | 700000.0 | nM | 3.15 |
| CHEMBL181686 | — | Kd | = | 960000.0 | nM | 3.02 |
| CHEMBL4859873 | — | Kd | = | 1000000.0 | nM | 3.00 |
| CHEMBL193664 | — | Kd | = | 990000.0 | nM | 3.00 |
| CHEMBL83148 | PHENYL(PHENYLSULFONYL)AMINE | Kd | = | 1100000.0 | nM | 2.96 |
| CHEMBL4867889 | — | Kd | = | 1100000.0 | nM | 2.96 |
| CHEMBL1945331 | — | Kd | = | 1200000.0 | nM | 2.92 |
| CHEMBL57394 | — | Kd | = | 1200000.0 | nM | 2.92 |
| CHEMBL4879253 | — | Kd | = | 1400000.0 | nM | 2.85 |
| CHEMBL4870439 | — | Kd | = | 1500000.0 | nM | 2.82 |
| CHEMBL1452067 | — | Kd | = | 2000000.0 | nM | 2.70 |
| CHEMBL4856558 | — | Kd | = | 2300000.0 | nM | 2.64 |
| CHEMBL851 | PHENYL PROPIONIC ACID | Kd | = | 3200000.0 | nM | 2.50 |
| CHEMBL24367 | — | Kd | = | 3700000.0 | nM | 2.43 |
| CHEMBL3086212 | — | Kd | = | 3900000.0 | nM | 2.41 |