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T-10430

2D structure
Target LTB4R2 
Mode of action Agonist
Control T-10404
Recommended cellular usage concentration ≤ 100 nM
In vivo use yes
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Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: IC50 = 31 nM (Tag-lite assay)
Selectivity within target family: > 30-fold LTB4R , AGTR1: Both show no effect in IP-One assay at up to 50 µM
Selectivity outside target family No activity except for LTB4R2 in GPCR screen (314 receptors, Ca2+ Aequorin assay) at 1 µM
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion:IP-One assay: EC50 = 19.4 nM, cAMP assay: EC50 = 0.51 nM
Control compound (100 times less potent than the probe) T-10404: no effect in IP-One assay at up to 100 µM for LTB4R2 and LTB4R; cAMP assay: EC50 = 560 nM (> 1000 fold)