Assay Detail
Binding
CHEMBL2187614
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of PKA expressed in Escherichia coli assessed as fluorescence labeled peptide substrate phosphorylation after 60 mins in presence of ATP
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.40 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177387 | — | — | 1 | 8.00 |
| CHEMBL2177381 | — | — | 1 | 7.77 |
| CHEMBL2177385 | — | — | 1 | 7.48 |
| CHEMBL2177388 | — | — | 1 | 7.46 |
| CHEMBL2178598 | — | — | 1 | 7.12 |
| CHEMBL2177361 | — | — | 1 | 6.99 |
| CHEMBL2178597 | — | — | 1 | 6.82 |
| CHEMBL2177379 | — | — | 1 | 6.57 |
| CHEMBL2177378 | — | — | 1 | 6.53 |
| CHEMBL2177371 | — | — | 1 | 6.38 |
| CHEMBL2177368 | — | — | 1 | 6.36 |
| CHEMBL2177372 | — | — | 1 | 6.31 |
| CHEMBL2177382 | — | — | 1 | 6.27 |
| CHEMBL2177362 | — | — | 1 | 6.25 |
| CHEMBL2177367 | — | — | 1 | 6.18 |
| CHEMBL2177366 | — | — | 1 | 6.18 |
| CHEMBL2177373 | — | — | 1 | 6.16 |
| CHEMBL2177374 | — | — | 1 | 6.11 |
| CHEMBL2177389 | — | — | 1 | 6.02 |
| CHEMBL2177377 | — | — | 1 | 6.00 |
| CHEMBL2177363 | — | — | 1 | 5.92 |
| CHEMBL2177364 | — | — | 1 | 5.89 |
| CHEMBL2177375 | — | — | 1 | 5.88 |
| CHEMBL2177370 | — | — | 1 | 5.87 |
| CHEMBL2177380 | — | — | 1 | 5.81 |
| CHEMBL2177369 | — | — | 1 | 5.80 |
| CHEMBL2177365 | — | — | 1 | 5.67 |
| CHEMBL2177390 | IPATASERTIB | 3.0 | 1 | 5.51 |
| CHEMBL2177383 | — | — | 1 | - |
| CHEMBL2177376 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177387 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2177381 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2177385 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2177388 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2178598 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2177361 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2178597 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL2177379 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL2177378 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL2177371 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL2177368 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL2177372 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2177382 | — | IC50 | = | 541.0 | nM | 6.27 |
| CHEMBL2177362 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL2177367 | — | IC50 | = | 662.0 | nM | 6.18 |
| CHEMBL2177366 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL2177373 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2177374 | — | IC50 | = | 777.0 | nM | 6.11 |
| CHEMBL2177389 | — | IC50 | = | 957.0 | nM | 6.02 |
| CHEMBL2177377 | — | IC50 | = | 1004.0 | nM | 6.00 |
| CHEMBL2177363 | — | IC50 | = | 1196.0 | nM | 5.92 |
| CHEMBL2177364 | — | IC50 | = | 1277.0 | nM | 5.89 |
| CHEMBL2177375 | — | IC50 | = | 1315.0 | nM | 5.88 |
| CHEMBL2177370 | — | IC50 | = | 1364.0 | nM | 5.87 |
| CHEMBL2177380 | — | IC50 | = | 1552.0 | nM | 5.81 |
| CHEMBL2177369 | — | IC50 | = | 1595.0 | nM | 5.80 |
| CHEMBL2177365 | — | IC50 | = | 2136.0 | nM | 5.67 |
| CHEMBL2177390 | IPATASERTIB | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2177383 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2177376 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2177386 | — | IC50 | > | 2000.0 | nM | - |