|BGS ▲||Aliases||Bcl2domain Protein Name||Entrez Gene Symbol
|BCL2||Bcl-2; PPP1R50||apoptosis regulator Bcl-2 alpha isoform [Homo sapiens]||BCL2
|BCL2A1||GRS; BFL1; ACC-1; ACC-2; HBPA1; BCL2L5||BCL2-related protein A1||BCL2A1
|BCLW||BCLW; BCL-W; PPP1R51; BCL2-L-2||BCL2-like 2||BCL2L2
|BCLXL||BCLX; BCL2L; BCLXL; BCLXS; Bcl-X; bcl-xL; bcl-xS; PPP1R52; BCL-XL/S||BCL2-like 1||BCL2L1
|MCL1||TM; EAT; MCL1L; MCL1S; Mcl-1; BCL2L3; MCL1-ES; bcl2-L-3; mcl1/EAT||myeloid cell leukemia 1||MCL1
Targeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia. Andrew W.Roberts, John Seymour, et al. N ENGL J MED. 2016 Jan 11. 1-12
Clearance of senescent cells by ABT263 rejuvenates aged hematopoietic stem cells in mice. Jianhui Chang, Daohong Zhou et al., Nat.Med. 2016 Jan. 22 (1). 78-83
DiscoverX also offers cell-based services for multiple BCL2 family members including BCL2, BCLXL and MCL1. Learn more
Platform Benefit & Technology Details
Menu of fully validated quantitative ligand binding assays for anti-apoptotic BCL2 family targets
Measure potency and selectivity in the same assay format enabling inter-protein inhibitor potency rank-ordering and SAR
Screen, profile and measure Kds in one flexible format in high and low-throughput modes
Broad dynamic range for accurate affinity measurements (tight binding limit <70 pM)
How the Technology Works
Compounds interacting with the BCL2 family protein prevent binding of these proteins to an immobilized known peptide ligand and reduce the amount of target protein captured on the solid support (Panels A & B). Conversely, test molecules that do not bind the BCL2 family protein have no effect on the amount of target protein captured on the solid support (Panel C). Screening “hits” are identified by measuring the amount of BCL2 family protein captured in test versus control samples by using a quantitative, precise and ultra-sensitive qPCR method that detects the associated DNA label (Panel D). In a similar manner, dissociation constants (Kds) for test compound-BCL2 family protein interactions are calculated by measuring the amount of target protein captured on the solid support as a function of the test compound concentration. Assay conditions are optimized for the measurement of true thermodynamic test compound Kd values.
Available BCL2 Services
Standard Turnaround Time
bcl2MAX: Screen compounds across all our available assays for BCL2 family targets.
bcl2KdELECT: Measure test compound(s) Kd values against custom-selected BCL2 family targets or all available BCL2 family targets.
bcl2ELECT: Screen collections of chemical assets or small number of compounds across one or more custom-selected BCL2 family targets.
: 15 business days for all services. 72 hour TAT available.
Data Analysis & Interpretation
Percent of Control (%Ctrl)
The results for single concentration (primary screen) binding interactions for tested compound(s) are reported in your study report and spreadsheets as '%Ctrl' and is calculated in the following manner:
test compound = client supplied compound
negative control = DMSO (100% control)
positive control = control compound (0% control)
Binding Constant (Kd)
The results for an 11-point dose response curve compound/kinase interactions are reported in your study report and spreadsheets as Kd, which are values derived using the Hill equation:
The Hill Slope is set to -1. Curves are fitted using a non-linear least square fit with the Levenberg-Marquardt algorithm.