1383376-93-9
Chemical Structure
PF-5236216
- CAS No.: 1383376-93-9
- Formula:C18H15FN4O
- Molecular Weight:322.34
IUPAC Name: 4-(3-(4-fluorophenyl)-1-methyl-1H-pyrazol-4-yl)-6-methyl-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one
InChIKey: NGDXEOHYWJHBTJ-UHFFFAOYSA-N
SMILES: O=C1C2=C(C3=CN(C)N=C3C4=CC=C(F)C=C4)C=CN=C2CN1C
Biological Activity: PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies[1].
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PF-5236216 | PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies. | |||||||||||||||||||||
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Keywords
