Assay Detail
Binding
CHEMBL3888055
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FL5.12 Cellular Assay: The efficacy of the compounds of Formula (I) can also be determined in cell-based killing assays using a variety of cell lines and mouse tumor models. For example, their activity on cell viability can be assessed on a panel of cultured tumorigenic and non-tumorigenic cell lines, as well as primary mouse or human cell populations. In one exemplary set of conditions, mouse FL5.12 cells transfected with Bcl-XL were cultured under standard conditions in RPMI with 2 mM glutamine, 1% 100 mM sodium pyruvate, 2% 1 M HEPES, 4 uL/L of beta;-mercaptoethanol, 1% penicillin-streptomycin, 10% FBS, and 10% WEHI-3B conditioned media (for IL-3). For assaying the compound activity, the cells were exchanged into an IL-3-depleted deprivation media, which was identical to the growth media except for the absence of FBS and WEHI-3B conditional media, for 2 days. Then the cells were exchanged to 3% FBS assay media (RPMI with 2 mM glutamine, 1% 100 mM sodium pyruvate, 2% 1 M HEPES, 4 uL/L of beta;-mercaptoethanol, 1% penicillin-streptomycin, 10% FBS, and 10% WEHI-3B conditioned media (for IL-3).
172
Total Activities
172
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 172 | 7.22 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3964488 | — | — | 1 | 10.00 |
| CHEMBL3978558 | — | — | 1 | 9.70 |
| CHEMBL3945285 | — | — | 1 | 9.70 |
| CHEMBL3945287 | — | — | 1 | 9.52 |
| CHEMBL3930283 | — | — | 1 | 9.30 |
| CHEMBL3929193 | — | — | 1 | 9.22 |
| CHEMBL3923735 | — | — | 1 | 9.05 |
| CHEMBL3914767 | — | — | 1 | 9.00 |
| CHEMBL3913717 | — | — | 1 | 9.00 |
| CHEMBL3924846 | — | — | 1 | 9.00 |
| CHEMBL3971522 | — | — | 1 | 8.70 |
| CHEMBL3919588 | — | — | 1 | 8.40 |
| CHEMBL4111466 | — | — | 1 | 8.40 |
| CHEMBL3946359 | — | — | 1 | 8.30 |
| CHEMBL3930937 | — | — | 1 | 8.22 |
| CHEMBL3920915 | — | — | 1 | 8.22 |
| CHEMBL3950423 | — | — | 1 | 8.15 |
| CHEMBL3923925 | — | — | 1 | 8.15 |
| CHEMBL3926315 | — | — | 1 | 8.10 |
| CHEMBL3941020 | — | — | 1 | 8.10 |
| CHEMBL3921464 | — | — | 1 | 8.05 |
| CHEMBL3911895 | — | — | 1 | 8.05 |
| CHEMBL3939320 | — | — | 1 | 8.00 |
| CHEMBL3968809 | — | — | 1 | 8.00 |
| CHEMBL3985366 | — | — | 1 | 8.00 |
| CHEMBL3907071 | — | — | 1 | 7.96 |
| CHEMBL3984574 | — | — | 1 | 7.96 |
| CHEMBL3951689 | — | — | 1 | 7.92 |
| CHEMBL3920602 | — | — | 1 | 7.92 |
| CHEMBL3964249 | — | — | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3964488 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3945285 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3978558 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3945287 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3930283 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3929193 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3923735 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3914767 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3913717 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3924846 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3971522 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4111466 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3919588 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3946359 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3930937 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3920915 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3923925 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3950423 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3941020 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3926315 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3921464 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3911895 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3939320 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3985366 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3968809 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3984574 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3907071 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3964249 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3920602 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3951689 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3935328 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3892280 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3895034 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3963138 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3922702 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3971433 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3914056 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3901090 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3938659 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3924869 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3965661 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3908449 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3939902 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3964142 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4113873 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3945826 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3932865 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3940367 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3941341 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3891330 | — | EC50 | = | 51.0 | nM | 7.29 |