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P-10358

Smith et al. IC50 0.10 microM for AChE 0.08 microM for BChE selectivity 1.25 11 time less potent than heptastigmine and 2.5 more potent than Tacrine

General

Type : Carbamate,Indole,Pyridine

Chemical_Nomenclature : [1-[(3-fluoropyridin-4-yl)amino]-3-methylindol-5-yl] N-methylcarbamate

Canonical SMILES : CC1=CN(C2=C1C=C(C=C2)OC(=O)NC)NC3=C(C=NC=C3)F

InChI : InChI=1S\/C16H15FN4O2\/c1-10-9-21(20-14-5-6-19-8-13(14)17)15-4-3-11(7-12(10)15)23-16(22)18-2\/h3-9H,1-2H3,(H,18,22)(H,19,20)

InChIKey : GUHMRCCRDRBMHO-UHFFFAOYSA-N

Other name(s) : 1-((3-Fluoro-4-pyridinyl)amino)-3-methyl-1H-indol-5-ol methylcarbamate (ester),1H-Indol-5-ol, 1-((3-fluoro-4-pyridinyl)amino)-3-methyl-, methylcarbamate (ester)

MW : 314.314

Formula : C16H15FN4O2

CAS_number : 188240-59-7

PubChem : 3075612

UniChem : GUHMRCCRDRBMHO-UHFFFAOYSA-N

Target

Families : P-10358 ligand of proteins in family
ACHE BCHE

References (2)

Title : Central and peripheral activity of cholinesterase inhibitors as revealed by yawning and fasciculation in rats - Ogura_2001_Eur.J.Pharmacol_415_157
Author(s) : Ogura H , Kosasa T , Kuriya Y , Yamanishi Y
Ref : European Journal of Pharmacology , 415 :157 , 2001
Abstract : Ogura_2001_Eur.J.Pharmacol_415_157
ESTHER : Ogura_2001_Eur.J.Pharmacol_415_157
PubMedSearch : Ogura_2001_Eur.J.Pharmacol_415_157
PubMedID: 11274994

Title : Pharmacological activity and safety profile of P10358, a novel, orally active acetylcholinesterase inhibitor for Alzheimer's disease - Smith_1997_J.Pharmacol.Exp.Ther_280_710
Author(s) : Smith CP , Bores GM , Petko W , Li M , Selk DE , Rush DK , Camacho F , Winslow JT , Fishkin R , Cunningham DM , Brooks KM , Roehr J , Hartman HB , Davis L , Vargas HM
Ref : Journal of Pharmacology & Experimental Therapeutics , 280 :710 , 1997
Abstract : Smith_1997_J.Pharmacol.Exp.Ther_280_710
ESTHER : Smith_1997_J.Pharmacol.Exp.Ther_280_710
PubMedSearch : Smith_1997_J.Pharmacol.Exp.Ther_280_710
PubMedID: 9023283 
Array
(
    [id] => 4473
    [inhibitor] => P-10358
    [type] => Array
        (
            [0] => Carbamate
            [1] => Indole
            [2] => Pyridine
        )

    [other_name] => Array
        (
            [0] => 1-((3-Fluoro-4-pyridinyl)amino)-3-methyl-1H-indol-5-ol methylcarbamate (ester)
            [1] => 1H-Indol-5-ol, 1-((3-fluoro-4-pyridinyl)amino)-3-methyl-, methylcarbamate (ester)
        )

    [chemical_nomenclature] => [1-[(3-fluoropyridin-4-yl)amino]-3-methylindol-5-yl] N-methylcarbamate
    [formula] => C16H15FN4O2
    [cas_number] => 188240-59-7
    [mw] => 314.314
    [pick_me_to_call] => display_script
    [kinetic_parameter] => 
    [paper] => Ogura_2001_Eur.J.Pharmacol_415_157 || Smith_1997_J.Pharmacol.Exp.Ther_280_710
    [comment] => Smith et al. IC50 0.10 microM for AChE 0.08 microM for BChE selectivity 1.25 11 time less potent than heptastigmine and 2.5 more potent than Tacrine
    [gene_locus] => 
    [kin_inhibitor] => 
    [cid] => 3075612
    [family] => ACHE || BCHE
    [inchikey] => GUHMRCCRDRBMHO-UHFFFAOYSA-N
    [canonicalsmiles] => CC1=CN(C2=C1C=C(C=C2)OC(=O)NC)NC3=C(C=NC=C3)F
    [inchi] => InChI=1S\/C16H15FN4O2\/c1-10-9-21(20-14-5-6-19-8-13(14)17)15-4-3-11(7-12(10)15)23-16(22)18-2\/h3-9H,1-2H3,(H,18,22)(H,19,20)
    [wikipedia] => 
    [iupharlig] => 
    [structure] => 
    [substrate] => 
    [interact_gene_locus] => 
    [mutation] => 
    [comment2] => 
    [extoxnet] => 
    [news] => 
    [theoretical_model] => 
)