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Ogerin

2D structure
Target GPR68 
Mode of action Positive allosteric modulator
Control ZINC32547799
Recommended cellular usage concentration ≤ 1 µM
In vivo use Yes
Synonyms ZINC67740571
Donated by UNC


Probe criteria


Selectivity within target family: > 30-fold Surpasses criterion: Screened for radioligand binding modulation of CNS GPCRs and toxic pharmacological off-targets. Minimal activity at all targets (pKi> 7)
Clean PDSP scan except for one off-target: HTR2B Ki =496.36 nM.
Selectivity outside target family Coming soon
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion:Ogerin modulates proton-mediated calcium mobilization (@10 μM): pEC50 6.83 ± 0.06 (in FLIPR-TETRA assay); decreases contextual memory retrieval.
Control compound (100 times less potent than the probe) ZINC32547799: no measurable effect on learning and memory in wild-type mice; Clean PDSP scan with one exception: HTR1A Ki = 849.86 nM