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SR-302

2D structure
Target DDR1  DDR2  MAPK11  MAPK14 
Targeted domain Kinase domain (active site)
Mode of action Inhibitor (type 2, ATP competitive)
Control SR-301
Recommended cellular usage concentration 100 nM
In vivo use No
Donated by SGC-Frankfurt


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: Enzyme kinetic assay from"Reaction Biology": DDR1: IC50 = 53.3 nM (ATP conc.: 100 µM), DDR2: IC50 = 0.75 nM (ATP conc.: 5 µM), MAPK11: IC50 = 45.1 nM (ATP conc.: 50 µM), MAPK14: IC50 =6.2 nM (ATP conc.: 2.5 µM)
Selectivity within target family: > 30-fold Closest off-targets found in KinomeScan: ABL1, RIPK2, RPS6KA5, CHEK2, STK38L; for all IC50 > 25 µM (> 125 fold selective) in NanoBRET assay
Selectivity outside target family Clean PDSP scan (45 targets)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: NanoBRET assay (HEK293T cells, full-length protein): DDR1: IC50 = 23 ± 2 nM, DDR2: IC50 = 18 ± 2 nM, MAPK11: IC50 = 196 ± 8 nM, MAPK14: IC50 =125 ± 11 nM
Destabilizing effect on E-cadherin
Control compound (100 times less potent than the probe) SR-301: NanoBRET assay (HEK293T cells, full-length protein): DDR1: IC50 = 21.9 ± 5.44 µM (>850 fold), DDR2: IC50 = 15.5 ± 5.08 µM (>850 fold), MAPK11: IC50 = 1.83 µM (8- fold), MAPK14: IC50 =5.39 ± 3.10 µM (43-fold)