Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H18ClN5O2.ClH |
Molecular Weight | 396.271 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.NC1=C2C(COC3=CC(Cl)=CC=C3)=NN(C4CCOCC4)C2=NC=N1
InChI
InChIKey=QZXZQMUZEHTFHD-UHFFFAOYSA-N
InChI=1S/C17H18ClN5O2.ClH/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12;/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21);1H
Molecular Formula | C17H18ClN5O2 |
Molecular Weight | 359.81 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
PF 4800567 is a drug developed by Pfizer which acts as a selective potent inhibitor of CK1epsilon (IC(50) = 32 nM) with greater than 20-fold selectivity over CK1delta, and has mainly been used in the study of the casein kinase 1 enzymes in the regulation of circadian rhythm, as well as showing potential neuroprotective effects. PF 4800567 was found in animal studies to enhance responses to certain drugs of abuse such as methamphetamine and fentanyl, which suggests a role for CK1-ε in negative regulation of sensitivity to stimulant and opioid drugs.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22089318
Curator's Comment: Mice harboring a null allele of Csnk1e showed an increase in locomotor activity following MA administration. Consistent with this result, coadministration of a PF-4800567 increased the locomotor stimulant response to both MA and fentanyl.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4937 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19458106 |
32.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. | 2009 Aug |
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Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. | 2010 Aug 24 |
|
IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ɛ and Wnt/β-catenin independent inhibition of mitotic spindle formation. | 2011 Jun 2 |
|
Csnk1e is a genetic regulator of sensitivity to psychostimulants and opioids. | 2012 Mar |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22089318
Mice: 40 mg/kg, i.p.
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20696890
A significant lengthening of the period was observed at 1 uM
PF 4800567 (approximately 10-fold CK1ε IC50; approximately 0.5-
fold CK1δ IC50) in WT (0.9 ± 0.13 h increase in period) but not
Ck1ε −/− -derived primary lung fibroblast cells (0.3 ± 0.3 h).
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 19:23:35 GMT 2023
by
admin
on
Sat Dec 16 19:23:35 GMT 2023
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Record UNII |
BHN7WPV2AE
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Record Status |
Validated (UNII)
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Record Version |
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BHN7WPV2AE
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1391052-28-0
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71751553
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admin on Sat Dec 16 19:23:36 GMT 2023 , Edited by admin on Sat Dec 16 19:23:36 GMT 2023
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PARENT -> SALT/SOLVATE |
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