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1-pyridine-2-aldoxime 1'-(pyridine-4-aldoxime) dimethyl ether dichloride
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HS-3, complete inhibition at 0.5 mM
2-pyridine aldoxime
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31% inhibition at 1 mM
3-hydroxy-DL-kynurenine
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50% inhibition at 0.2 mM, Ki: 8 mM
3-hydroxykynurenine
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potent inhibitor
3-pyridine aldoxime O-n-propyl ether
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43% inhibition at 1 mM
3-pyridine aldoxime O-phenyl ether
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61% inhibition at 1 mM
acetone
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inhibition up to 10%, v/v
arsenate
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strong inhibition for formamidase I, slight inhibition for formamidase II at 1 mM
ascorbate
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50% inhibition at 10 mM
Ba2+
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strong inhibition at 1 mM
bis(4-nitrophenyl)phosphate
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slight inhibition at 1 mM after 30 min preincubation
bromphenol blue
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50% inhibition at 0.024 mM after 5 min preincubation
Carbaryl
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moderately potent teratogen, Kd: 0.085 mM
diethyl dicarbonate
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90% inhibition at 0.5 mM
diethyl-(4-nitrophenyl)-phosphate
diisopropylfluorophosphate
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complete inhibition at 0.01 mM
dimethyl sulfoxide
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inhibition up to 10%, v/v
dioxane
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inhibition up to 10%, v/v
EDTA
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0.1 mM, complete inactivation
Fe2+
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31% inhibition only for formamidase II at 1 mM
hydrosulfite
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strong inhibition at 1 mM
iodoacetamide
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slight inhibition at 1 mM for both formamidases I and II
isoleucine
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19% inhibition at 20 mM
L-tryptophan
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non-competitive inhibition, Ki: 5.24 mM
methionine
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20% inhibition at 20 mM
methyl parathion
O,O-dimethyl-O-4-nitrophenyl phosphorothioate
methyl-triphenyl phosphonium bromide
-
-
Mg2+
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moderate inhibition at 1 mM
N,N-Dimethylformamide
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inhibition up to 10%, v/v
N-acetylanthranilic acid
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15% inhibition at 6.7 mM
N-ethyloxycarbonyl-2-ethyloxy-1,2-dihydroquinoline
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53% inhibition at 1 mM
N-formyl-o-aminotoluene
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45% inhibition at 6.7 mM
NaCN
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31% inhibition at 5 mM
NH2OH*HCl
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14% inhibition at 3 mM
O,O-Diethyl-O-(4-nitrophenyl)phosphate
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E600, complete inhibition at 1 mM
o-aminobenzamidine
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62% inhibition at 0.5 mM
p-chloromercuribenzoate
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strong inhibition at 0.1 mM for both formamidases I and II
p-hydroxymercuribenzoate
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complete inhibition at 1 mM
p-nitrophenyldiethyl phosphoric acid
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92% inhibition at 10 mM
phenyl saligenin cyclic phosphate
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Kd: 0.00083 mM
phenylmethylsulfonyl fluoride
PMSF
binding structure analysis, overview
Salicyl aldoxime
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71% inhibition at 1 mM
tetraethyl diphosphate
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Kd: 67 mM
tetraheptylammonium bromide
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94% inhibition at 2.5 mM
tetrahexylammonium bromide
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56% inhibition at 5 mM
tetraoctylammoniumbromide
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94% inhibition at 2.5 mM
tetraphenyl phosphonium bromide
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22% inhibition at 5 mM
threonine
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19% inhibition at 20 mM
trimethyl-n-decylammonium bromide
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65% inhibition at 5 mM
trimethyl-n-decylammonium chloride
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65% inhibition at 5 mM
trimethyl-n-hexadecylammonium bromide
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100% inhibition at 5 mM
trimethylhexadecylammonium chloride
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100% inhibition at 5 mM
trimethylphenylammonium bromide
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20% inhibition at 5 mM
trimethylphenylammonium chloride
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20% inhibition at 5 mM
valine
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slight inhibition at 20 mM
2-aminoacetophenone
active site of the BaKynB-2-aminoacetophenone complex, structure, overview
2-aminoacetophenone
binding structure, overview
2-aminoacetophenone
binding structure, overview
Ag+
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complete inhibition at 0.1 mM
Ag+
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complete inhibition at 0.05 mM
Ag+
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complete inhibition at 0.01 mM
Ag+
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76% inhibition at 0.1 mM
anthranilic acid
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9% inhibition at 0.5-1 mM
anthranilic acid
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29% inhibition at 1-2 mM
anthranilic acid
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Ki: 1.6 mM
anthranilic acid
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45% inhibition at 0.5 mM
Co2+
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moderate inhibition at 1 mM
Co2+
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moderate inhibition at 1 mM
Co2+
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moderate inhibitor
Cu2+
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21% inhibition at 0.1 mM
Cu2+
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strong inhibition at 0.25 mM, more inhibition for formamidase I than formamidase II
Cu2+
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moderate inhibition at 1 mM
Cu2+
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moderate inhibitor
Cu2+
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31% inhibition at 1 mM
Cu2+
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complete inhibition at 1 mM
diazinon
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diazoxon
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diazoxon
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highly potent teratogen, Kd: 0.15 mM
dicrotophos
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potent teratogen, Kd: 3.2 mM
dicrotophos
inhibition due to the teratogen dicrotophos occurred in yolk sac membranes during the period of embryo highest susceptibility to organophosphorus insecticide teratogens; O,O-dimethyl-O-1[E]-methyl-3-(dimethylamino)-3-oxo-1-propenyl phosphate
diethyl-(4-nitrophenyl)-phosphate
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diethyl-(4-nitrophenyl)-phosphate
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marked inhibition
Hg2+
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moderate inhibition at 1 mM
Hg2+
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57% inhibition at 0.1 mM
Hg2+
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strong inhibition for both, formamidases I and II
Hg2+
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strong inhibition at 1 mM
Hg2+
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20% inhibition at 0.05 mM
Hg2+
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complete inhibition at 1 mM
Hg2+
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complete inhibition at 0.05 mM
Hg2+
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complete inhibition at 1 mM
Hg2+
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50% inhibition at 0.1 mM
L-kynurenine
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marked inhibition above 0.1 mM
L-kynurenine
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competitive inhibition, Ki: 0.26 mM
L-kynurenine
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potent inhibitor
L-kynurenine
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15% inhibition at 0.1 mM, Ki: 0.25 mM
L-kynurenine
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strong non-competitive inhibition
Mn2+
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strong inhibition at 1 mM
Mn2+
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strong inhibition at 1 mM
Monocrotophos
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potent teratogen, Kd: 5.4 mM
N-bromosuccinimide
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N-bromosuccinimide
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marked inhibition
Na-bisulfite
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50% inhibition at 0.18 mM
Na-bisulfite
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complete inhibition at 4 mM
Na-bisulfite
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50% inhibition at 0.32 mM
Na-bisulfite
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strong inhibition 10 mM
Na-Metaarsenite
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Na-Metaarsenite
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marked inhibition
Na2S2O4
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Na2S2O4
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27% inhibition at 0.04 mM
NaAsO2
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NaAsO2
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marked inhibition
NaAsO2
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25% inhibition at 0.05 mM
NaF
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42% inhibition at 5 mM
NaF
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strong inhibition for both formamidases I and II at 1 mM
NaF
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27% inhibition at 10 mM
NaF
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at 10 mM: strong inhibition for formamidase I, slight inhibition for formamidase II
NaHSO3
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50% inhibition at 0.18 mM
NaHSO3
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complete inhibition at 4 mM
NaHSO3
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strong inhibition at 1 mM for both formamidases I and II
NaHSO3
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50% inhibition at 0.32 mM
NaHSO3
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24% inhibition at 0.04 mM
NaHSO3
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strong inhibition at at 10 mM
phenylalanine
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slight inhibition at 20 mM
phenylalanine
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slight inhibition at 20 mM
phenylmethylsulfonyl fluoride
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Kd: 3.3 mM
phenylmethylsulfonyl fluoride
-
complete inhibition at 1 mM
phenylmethylsulfonyl fluoride
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strong inhibition
Urea
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25% inhibition at 2 M
Urea
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75% inhibition at 1 M
Zn2+
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moderate inhibition at 1 mM
Zn2+
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strong inhibition at 0.1 mM, more for formamidase II than formamidase I
Zn2+
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strong inhibition at 1 mM
Zn2+
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complete inhibition of formamidase I at 1 mM, 88% inhibition of formamidase II at 1 mM
additional information
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no inhibition by PMSF
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additional information
determination and analysis of organophosphorus insecticides structural requirements to inhibit in ovo chicken embryo yolk sac membrane kynurenine formamidase, inhibition mechanism, plnED50 values, overview. The dominant electrostatic interactions are localized at nitrogen-1, nitrogen-3, nitrogen of 2-amino substituent of the pyrimidinyl of pyrimidinyl phosphorothioates, and the oxygen of crotonamide carbonyl in crotonamide phosphates. Bulkiness of the substituents at carbon-2 and carbon-6 of the pyrimidinyls and/or N-substituents and carbon-3 substituents of crotonamides are the steric structural components that contribute to in ovo inhibition of the enzyme
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additional information
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determination and analysis of organophosphorus insecticides structural requirements to inhibit in ovo chicken embryo yolk sac membrane kynurenine formamidase, inhibition mechanism, plnED50 values, overview. The dominant electrostatic interactions are localized at nitrogen-1, nitrogen-3, nitrogen of 2-amino substituent of the pyrimidinyl of pyrimidinyl phosphorothioates, and the oxygen of crotonamide carbonyl in crotonamide phosphates. Bulkiness of the substituents at carbon-2 and carbon-6 of the pyrimidinyls and/or N-substituents and carbon-3 substituents of crotonamides are the steric structural components that contribute to in ovo inhibition of the enzyme
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additional information
no inhibition by p-chloromercuribenzoate
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additional information
activity is not affected by Mn2+, Mg2+, Zn2+, Fe2+, Fe3+, ascorbic acid, cysteine, glutathione, p-chloromercuribenzoate, EDTA, KCN, K3Fe(CN)6, Na2S2O6 and sodium formate
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