Assay Detail
Binding
CHEMBL4307005
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Inhibition of Akt1 (unknown origin) expressed in Escherichia coli using peptide as substrate incubated for 1 hr by HTRF assay
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
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.79 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4435124 | — | — | 1 | 9.00 |
| CHEMBL4451854 | — | — | 1 | 8.90 |
| CHEMBL4454791 | — | — | 1 | 8.74 |
| CHEMBL4444441 | — | — | 1 | 8.26 |
| CHEMBL4579551 | — | — | 1 | 8.05 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 8.02 |
| CHEMBL4438248 | — | — | 1 | 7.99 |
| CHEMBL4445702 | — | — | 1 | 7.97 |
| CHEMBL4442226 | — | — | 1 | 7.86 |
| CHEMBL2219422 | AFURESERTIB | 3.0 | 1 | 7.77 |
| CHEMBL4545734 | — | — | 1 | 7.45 |
| CHEMBL4467970 | — | — | 1 | 7.33 |
| CHEMBL4554198 | — | — | 1 | 7.31 |
| CHEMBL4455194 | — | — | 1 | 7.21 |
| CHEMBL4460688 | — | — | 1 | 7.19 |
| CHEMBL4526242 | — | — | 1 | 7.15 |
| CHEMBL4577134 | — | — | 1 | 7.00 |
| CHEMBL4461200 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4435124 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4451854 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL4454791 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4444441 | — | IC50 | = | 5.46 | nM | 8.26 |
| CHEMBL4579551 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3137336 | UPROSERTIB | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4438248 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL4445702 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL4442226 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL2219422 | AFURESERTIB | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL4545734 | — | IC50 | = | 35.3 | nM | 7.45 |
| CHEMBL4467970 | — | IC50 | = | 46.9 | nM | 7.33 |
| CHEMBL4554198 | — | IC50 | = | 48.9 | nM | 7.31 |
| CHEMBL4455194 | — | IC50 | = | 62.2 | nM | 7.21 |
| CHEMBL4460688 | — | IC50 | = | 65.2 | nM | 7.19 |
| CHEMBL4526242 | — | IC50 | = | 70.4 | nM | 7.15 |
| CHEMBL4577134 | — | IC50 | = | 99.9 | nM | 7.00 |
| CHEMBL4461200 | — | IC50 | = | 101.0 | nM | 7.00 |