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TP-030-2

2D structure
Target RIPK1 
Targeted domain Kinase domain (allosteric pocket)
Mode of action Inhibitor (type 3, non-ATP competitive)
Control TP-030n
Orthogonal probe TP-030-1 
Recommended cellular usage concentration 100 nM
In vivo use Yes
Donated by Takeda


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: RIPK1 (h): Ki = 0.43 nM; RIPK1 (m): IC50 = 100 nM (cell free assay)
Selectivity within target family: > 30-fold No significant binding observed at 1 µM from in-house Global Kinase Panel (303 kinases)
Selectivity outside target family LeadProfilingScreen (68 targets tested; Eurofins-Panlabs): Closest off-targets in the PDSP scan are GABA/PBR Ki = 346.58 nM, HTR2A Ki = 2071.02 nM and ADRA2A Ki = 2355.74 nM
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: HT29 necroptosis: IC50 = 1.3 nM
Control compound (100 times less potent than the probe) TP-030n: RIPK1 (h): Ki = 6900 nM; RIPK1 (m): Ki > 10 µM