Assay Detail

CHEMBL5730056

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding

Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Representative compounds were serially diluted in dimethyl sulfoxide (DMSO) starting at 50 uM (2x starting concentration; 10% DMSO) and 10 uL were transferred into a 384-well plate. Then 10 uL of a protein/probe/antibody mix was added to each well at final concentrations listed in TABLE 1. Protein:GST-Bcl-2, Probe: F-Bak Peptide Probe Acetyl-GQVGRQLAIIGDK(6-FAM)INR-amide(SEQ ID NO: 1), Protein(nM): 1, Probe (nM): 100, Antibody: Tb-anit-GST, Antibody (nm): 1. The samples are then mixed on a shaker for 1 minute and incubated for an additional 3 hours at room temperature. For each assay, the probe/antibody and protein/probe/antibody were included on each assay plate as negative and positive controls, respectively. Fluorescence was measured on the ENVISION plate reader (Perkin Elmer) using a 340/35 nm excitation filter and 520/525 (F-Bak peptide) and 495/510 nm (Tb-labeled anti-Histidine antibody) emission filters.

ChEMBL ↗

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Target

Apoptosis regulator Bcl-2 (CHEMBL4860) ↗

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Primary target Apoptosis regulator Bcl-2

CHEMBL4860

Anchored from Assay target.

Protein identity Apoptosis regulator Bcl-2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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1080

Total Activities

346

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Apoptosis regulator Bcl-2 (CHEMBL4860) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases

(2015)

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	360	10.02	11.00
kon	360	-	-
k_off	360	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3961644	—	—	3	11.00
CHEMBL3952489	—	—	3	11.00
CHEMBL3985475	—	—	6	11.00
CHEMBL3900365	—	—	3	10.96
CHEMBL3891622	—	—	6	10.96
CHEMBL3948837	—	—	6	10.92
CHEMBL3902290	—	—	3	10.92
CHEMBL3963984	—	—	3	10.92
CHEMBL3925316	—	—	3	10.89
CHEMBL3916807	—	—	3	10.89
CHEMBL3901126	—	—	3	10.89
CHEMBL3973960	—	—	6	10.89
CHEMBL3977292	—	—	6	10.89
CHEMBL3901940	—	—	6	10.85
CHEMBL3978223	—	—	6	10.85
CHEMBL3976783	—	—	3	10.85
CHEMBL3952871	—	—	3	10.85
CHEMBL3955355	—	—	3	10.82
CHEMBL3957494	—	—	3	10.80
CHEMBL3958014	—	—	3	10.80
CHEMBL3918493	—	—	3	10.80
CHEMBL3907059	—	—	3	10.80
CHEMBL3906596	—	—	3	10.80
CHEMBL3970500	—	—	3	10.77
CHEMBL3920717	—	—	3	10.77
CHEMBL3944117	—	—	3	10.77
CHEMBL3936791	—	—	3	10.77
CHEMBL3921409	—	—	3	10.77
CHEMBL3972476	—	—	3	10.77
CHEMBL3894139	—	—	3	10.74

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3961644	—	Ki	=	0.01	nM	11.00
CHEMBL3985475	—	Ki	=	0.01	nM	11.00
CHEMBL3952489	—	Ki	=	0.01	nM	11.00
CHEMBL3900365	—	Ki	=	0.011	nM	10.96
CHEMBL3891622	—	Ki	=	0.011	nM	10.96
CHEMBL3902290	—	Ki	=	0.012	nM	10.92
CHEMBL3948837	—	Ki	=	0.012	nM	10.92
CHEMBL3963984	—	Ki	=	0.012	nM	10.92
CHEMBL3973960	—	Ki	=	0.013	nM	10.89
CHEMBL3925316	—	Ki	=	0.013	nM	10.89
CHEMBL3977292	—	Ki	=	0.013	nM	10.89
CHEMBL3901126	—	Ki	=	0.013	nM	10.89
CHEMBL3916807	—	Ki	=	0.013	nM	10.89
CHEMBL3952871	—	Ki	=	0.014	nM	10.85
CHEMBL3978223	—	Ki	=	0.014	nM	10.85
CHEMBL3901940	—	Ki	=	0.014	nM	10.85
CHEMBL3976783	—	Ki	=	0.014	nM	10.85
CHEMBL3955355	—	Ki	=	0.015	nM	10.82
CHEMBL3918493	—	Ki	=	0.016	nM	10.80
CHEMBL3958014	—	Ki	=	0.016	nM	10.80
CHEMBL3957494	—	Ki	=	0.016	nM	10.80
CHEMBL3907059	—	Ki	=	0.016	nM	10.80
CHEMBL3906596	—	Ki	=	0.016	nM	10.80
CHEMBL3972476	—	Ki	=	0.017	nM	10.77
CHEMBL3936791	—	Ki	=	0.017	nM	10.77
CHEMBL3921409	—	Ki	=	0.017	nM	10.77
CHEMBL3920717	—	Ki	=	0.017	nM	10.77
CHEMBL3944117	—	Ki	=	0.017	nM	10.77
CHEMBL3970500	—	Ki	=	0.017	nM	10.77
CHEMBL3894139	—	Ki	=	0.018	nM	10.74
CHEMBL3907400	—	Ki	=	0.018	nM	10.74
CHEMBL3913948	—	Ki	=	0.019	nM	10.72
CHEMBL3950070	—	Ki	=	0.021	nM	10.68
CHEMBL3932065	—	Ki	=	0.021	nM	10.68
CHEMBL3965909	—	Ki	=	0.021	nM	10.68
CHEMBL3963537	—	Ki	=	0.022	nM	10.66
CHEMBL3921856	—	Ki	=	0.022	nM	10.66
CHEMBL3982090	—	Ki	=	0.023	nM	10.64
CHEMBL3972115	—	Ki	=	0.023	nM	10.64
CHEMBL3966962	—	Ki	=	0.023	nM	10.64
CHEMBL3920620	—	Ki	=	0.023	nM	10.64
CHEMBL3974238	—	Ki	=	0.024	nM	10.62
CHEMBL3933894	—	Ki	=	0.024	nM	10.62
CHEMBL3983051	—	Ki	=	0.024	nM	10.62
CHEMBL3895321	—	Ki	=	0.026	nM	10.59
CHEMBL3926563	—	Ki	=	0.026	nM	10.59
CHEMBL3956368	—	Ki	=	0.029	nM	10.54
CHEMBL3936894	—	Ki	=	0.029	nM	10.54
CHEMBL3920467	—	Ki	=	0.03	nM	10.52
CHEMBL3918688	—	Ki	=	0.03	nM	10.52