Assay Detail
Binding
CHEMBL977319
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Displacement of [3H]PDBu from RasGRP3 expressed in cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Conformationally constrained analogues of diacylglycerol. 30. An investigation of diacylglycerol-lactones containing heteroaryl groups reveals compounds with high selectivity for Ras guanyl nucleotide-releasing proteins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.45 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL519741 | — | — | 1 | 9.74 |
| CHEMBL530110 | — | — | 1 | 9.70 |
| CHEMBL488872 | — | — | 1 | 9.28 |
| CHEMBL488667 | — | — | 1 | 9.15 |
| CHEMBL472007 | — | — | 1 | 9.14 |
| CHEMBL472522 | — | — | 1 | 8.80 |
| CHEMBL529000 | — | — | 1 | 8.77 |
| CHEMBL488674 | — | — | 1 | 8.48 |
| CHEMBL472521 | — | — | 1 | 8.43 |
| CHEMBL488675 | — | — | 1 | 8.42 |
| CHEMBL488871 | — | — | 1 | 8.34 |
| CHEMBL488668 | — | — | 1 | 8.17 |
| CHEMBL487473 | — | — | 1 | 8.09 |
| CHEMBL511472 | — | — | 1 | 7.96 |
| CHEMBL472523 | — | — | 1 | 7.86 |
| CHEMBL488509 | — | — | 1 | 7.76 |
| CHEMBL487483 | — | — | 1 | 7.62 |
| CHEMBL488707 | — | — | 1 | 7.49 |
| CHEMBL470094 | — | — | 1 | 7.45 |
| CHEMBL443643 | — | — | 1 | 7.36 |
| CHEMBL487822 | — | — | 1 | 7.27 |
| CHEMBL488670 | — | — | 1 | 7.27 |
| CHEMBL487484 | — | — | 1 | 7.23 |
| CHEMBL471316 | — | — | 1 | 7.09 |
| CHEMBL512538 | — | — | 1 | 7.08 |
| CHEMBL472183 | — | — | 1 | 6.86 |
| CHEMBL511847 | — | — | 1 | 6.17 |
| CHEMBL528323 | — | — | 1 | 6.04 |
| CHEMBL530337 | — | — | 1 | 5.86 |
| CHEMBL472351 | — | — | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL519741 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL530110 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL488872 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL488667 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL472007 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL472522 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL529000 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL488674 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL472521 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL488675 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL488871 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL488668 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL487473 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL511472 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL472523 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL488509 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL487483 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL488707 | — | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL470094 | — | Ki | = | 35.8 | nM | 7.45 |
| CHEMBL443643 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL487822 | — | Ki | = | 54.2 | nM | 7.27 |
| CHEMBL488670 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL487484 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL471316 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL512538 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL472183 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL511847 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL528323 | — | Ki | = | 907.0 | nM | 6.04 |
| CHEMBL530337 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL472351 | — | Ki | = | 1410.0 | nM | 5.85 |
| CHEMBL488506 | — | Ki | = | 1970.0 | nM | 5.71 |
| CHEMBL471142 | — | Ki | = | 2040.0 | nM | 5.69 |
| CHEMBL488671 | — | Ki | = | 2360.0 | nM | 5.63 |
| CHEMBL513379 | — | Ki | = | 2470.0 | nM | 5.61 |
| CHEMBL486457 | — | Ki | = | 3660.0 | nM | 5.44 |
| CHEMBL472006 | — | Ki | = | 5500.0 | nM | 5.26 |