Assay Detail
Functional
CHEMBL806403
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of oncogene product p185 erbB-2 from human breast cancer cells(SK-BR-3 cells) at 50 mg/kg dose.
81
Total Activities
81
Compounds Tested
1
Activity Types
1
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | SK-BR-3 |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 81 | 6.80 | 7.92 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| DOSE | DOSE | 50.0 | mg.kg-1 | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL125509 | — | — | 1 | 7.92 |
| CHEMBL421647 | — | — | 1 | 7.92 |
| CHEMBL339975 | — | — | 1 | 7.85 |
| CHEMBL554266 | — | — | 1 | 7.77 |
| CHEMBL433670 | — | — | 1 | 7.64 |
| CHEMBL339505 | — | — | 1 | 7.58 |
| CHEMBL338002 | — | — | 1 | 7.57 |
| CHEMBL3706729 | — | — | 1 | 7.52 |
| CHEMBL109480 | TANESPIMYCIN | 3.0 | 1 | 7.51 |
| CHEMBL3706726 | — | — | 1 | 7.48 |
| CHEMBL338892 | — | — | 1 | 7.47 |
| CHEMBL339231 | — | — | 1 | 7.43 |
| CHEMBL340038 | — | — | 1 | 7.40 |
| CHEMBL332831 | — | — | 1 | 7.37 |
| CHEMBL435807 | — | — | 1 | 7.34 |
| CHEMBL124215 | — | — | 1 | 7.30 |
| CHEMBL127520 | — | — | 1 | 7.30 |
| CHEMBL339471 | — | — | 1 | 7.30 |
| CHEMBL126225 | — | — | 1 | 7.30 |
| CHEMBL123564 | — | — | 1 | 7.29 |
| CHEMBL331273 | — | — | 1 | 7.22 |
| CHEMBL3706725 | — | — | 1 | 7.18 |
| CHEMBL125767 | — | — | 1 | 7.18 |
| CHEMBL278315 | GELDANAMYCIN | 2.0 | 1 | 7.16 |
| CHEMBL63175 | — | — | 1 | 7.10 |
| CHEMBL338893 | — | — | 1 | 7.08 |
| CHEMBL334128 | — | — | 1 | 7.05 |
| CHEMBL444855 | — | — | 1 | 7.01 |
| CHEMBL2111831 | — | — | 1 | 7.00 |
| CHEMBL125638 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL125509 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL421647 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL339975 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL554266 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL433670 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL339505 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL338002 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3706729 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL109480 | TANESPIMYCIN | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3706726 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL338892 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL339231 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL340038 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL332831 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL435807 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL124215 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL126225 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL339471 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL127520 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL123564 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL331273 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3706725 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL125767 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL278315 | GELDANAMYCIN | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL63175 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL338893 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL334128 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL444855 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2111831 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL125638 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL126986 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL446166 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL123835 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL333938 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL124840 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL262808 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL338536 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL127528 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2112642 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL127356 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL333049 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL263699 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL333770 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL340169 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2112640 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3706730 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL340123 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL421636 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2111832 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL421631 | — | IC50 | = | 420.0 | nM | 6.38 |