Potency data for probe BI-3802 and control BI-5273


In vitro potency


Target name Target information Species Assay description BI-3802 BI-5273 Publication of assay conditions
BCL6, BCL6 recombinant protein expressed in E.coli; aa 5-129 with mutations C8Q, C67R, C84N Homo sapiens BCL6:BCOR ULight TR-FRET: The BCOR ULight protein uses a C-terminal ULight tag (Perkin Elmer). With affinities of approximately 3 nM, the assay wall of this assay is reached, limiting the accuracy. IC50 ≤ 3 nM IC50 = 10162 nM PMID: 28930682
BCL6 protein from Prive lab Homo sapiens SPR (BCL6), Ontario institute for cancer research: Method: AVITAG (Biotin) on proteins N-terminus, Protein immobilized with a Streptavidin (SA) chip, (1300RU-2900 RU) were captured in different experiments, Biacore T200 was used with Biacore T200 evaluation software for analysis, HBS-P running buffer with 5% DMSO Kd = 1.409 µM ± 0.450 µM
BCL6B protein from Prive lab Homo sapiens SPR (BCL6B), Ontario institute for cancer research: Method: AVITAG (Biotin) on proteins N-terminus, Protein immobilized with a Streptavidin (SA) chip, (1300RU-2900 RU) were captured in different experiments, Biacore T200 was used with Biacore T200 evaluation software for analysis, HBS-P running buffer with 5% DMSO Kd = no binding
ZBTB32 protein from Prive lab Homo sapiens SPR (ZBTB32), Ontario institute for cancer research: Method: AVITAG (Biotin) on proteins N-terminus, Protein immobilized with a Streptavidin (SA) chip, (1300RU-2900 RU) were captured in different experiments, Biacore T200 was used with Biacore T200 evaluation software for analysis, HBS-P running buffer with 5% DMSO Kd = no binding
ZBTB16 protein from Prive lab Homo sapiens SPR (ZBTB16), Ontario institute for cancer research: Method: AVITAG (Biotin) on proteins N-terminus, Protein immobilized with a Streptavidin (SA) chip, (1300RU-2900 RU) were captured in different experiments, Biacore T200 was used with Biacore T200 evaluation software for analysis, HBS-P running buffer with 5% DMSO Kd = no binding
ZBTB17 protein from Prive lab Homo sapiens SPR (ZBTB17), Ontario institute for cancer research: Method: AVITAG (Biotin) on proteins N-terminus, Protein immobilized with a Streptavidin (SA) chip, (1300RU-2900 RU) were captured in different experiments, Biacore T200 was used with Biacore T200 evaluation software for analysis, HBS-P running buffer with 5% DMSO Kd = no binding

In cell potency


Target name Target information Species Assay description BI-3802 BI-5273 Publication of assay conditions
BCL6 Homo sapiens BCL6::NCOR LUMIER in cells IC50 = 43 nM PMID: 28930682
BCL6 Homo sapiens BCL6 protein degradation in SU-DHL-4 cells AC50 = 20 nM AC50 = inactive PMID: 28930682