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Potency data for probe BAY-826 and control BAY-309


In vitro potency


Target name Target information Species Assay description Probe result (SD) Control result (SD) Publication of assay conditions
TEK Bacterial; Partial (N804/T1112) Homo sapiens KINOMEScan (DiscoveRx Corp) with TEK Kd = 1.600 nM PMID: 27787897
TIE1 Bacterial; Partial (T819/A1138) Homo sapiens KINOMEScan (DiscoveRx Corp) with TIE1 Kd = 0.900 nM PMID: 27787897
DDR1 Bacterial; Partial (R565/V876) Homo sapiens KINOMEScan (DiscoveRx Corp) with DDR1 Kd = 0.400 nM PMID: 27787897
DDR2 Mammalian; Partial (V555/E855) Homo sapiens KINOMEScan (DiscoveRx Corp) with DDR2 Kd = 1.300 nM PMID: 27787897
STK10 Bacterial; Partial (E16/V314) Homo sapiens KINOMEScan (DiscoveRx Corp) with STK10 Kd = 5.900 nM PMID: 27787897
TEK Homo sapiens Bayer in-house kinase assay with TEK IC50 = 0.450 nM
KDR Mammalian; Partial (R787/P1253) Homo sapiens KINOMEScan (DiscoveRx Corp) with KDR Kd = 1.600 µM
FGFR1 Homo sapiens Bayer in-house kinase assay with FGFR1 IC50 > 10 µM
PDGFRB Homo sapiens Bayer in-house kinase assay with PDGFRB IC50 > 20 µM
FLT4 Homo sapiens Bayer in-house kinase assay with FLT4 IC50 = 0.440 µM
FGFR3 Homo sapiens Bayer in-house kinase assay with FGER3 IC50 > 10 µM
TEK Bacterial; Partial (N804/T1112) Homo sapiens KINOMEScan (DiscoveRx Corp) with TEK Kd > 20 µM

In cell potency


Target name Target information Species Assay description Probe result (SD) Control result (SD) Publication of assay conditions
TEK Homo sapiens Cellular mechanistic assay: inhibition of TEK autophosphorylation in human umbilical vein endothelial cells (HUVEC), pTEK-ELISA EC50 = 1.300 nM PMID: 27787897
TEK Homo sapiens NanoBRET assay (SGC Frankfurt) with TEK EC50 = 1.700 nM ± 0.230 nM (n=3)
TIE1 Homo sapiens NanoBRET assay (SGC Frankfurt) with TIE1 EC50 = 11 nM ± 5.600 nM (n=3)
DDR1 Homo sapiens NanoBRET assay (SGC Frankfurt) with DDR1 EC50 = 1.500 nM ± 0.220 nM (n=3)
DDR2 Homo sapiens NanoBRET assay (SGC Frankfurt) with DDR2 EC50 = 0.540 nM ± 0.047 nM (n=3)
STK10 Homo sapiens NanoBRET assay (SGC Frankfurt) with STK10 EC50 = 110 nM ± 2.100 nM (n=3)
EPHB6 Homo sapiens NanoBRET assay (SGC Frankfurt) with EPHB6 EC50 = 12 µM ± 0.970 µM (n=3)
LYN Homo sapiens NanoBRET assay (SGC Frankfurt) with LYN EC50 = 7.400 µM ± 0.450 µM (n=3)
TEK Homo sapiens NanoBRET assay (SGC Frankfurt) with TEK EC50 = 3.300 µM ± 0.340 µM (n=3)
TIE1 Homo sapiens NanoBRET assay (SGC Frankfurt) with TIE1 EC50 = 2.600 µM ± 0.550 µM (n=3)
DDR1 Homo sapiens NanoBRET assay (SGC Frankfurt) with DDR1 EC50 = 200 nM ± 32.000 nM (n=3)
DDR2 Homo sapiens NanoBRET assay (SGC Frankfurt) with DDR2 EC50 = 2.700 µM ± 1.200 µM (n=3)
STK10 Homo sapiens NanoBRET assay (SGC Frankfurt) with STK10 EC50 = 3.200 µM ± 0.440 µM (n=3)
EPHB6 Homo sapiens NanoBRET assay (SGC Frankfurt) with EPHB6 EC50 = 27 µM ± 5.800 µM (n=3)
LYN Homo sapiens NanoBRET assay (SGC Frankfurt) with LYN EC50 > 50 µM (n=3)