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Literature summary extracted from

  • Ganellin, C.R.; Bishop, P.B.; Bambal, R.B.; Chan, S.M.; Law, J.K.; Marabout, B.; Luthra, P.M.; Moore, A.N.; Peschard, O.; Bourgeat, P.; Rose, C.; Vargas, F.; Schwartz, J.C.
    Inhibitors of tripeptidyl peptidase II. 2. Generation of the first novel lead inhibitor of cholecystokinin-8-inactivating peptidase: a strategy for the design of peptidase inhibitors (2000), J. Med. Chem., 43, 664-674.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.14.10 (2S)-2-[[(2S)-2-aminobutanoyl]amino]butanoic acid
-
 Rattus norvegicus
3.4.14.10 (2S)-2-[[(2S)-2-aminobutanoyl]amino]pentanoic acid
-
 Rattus norvegicus
3.4.14.10 (S)-valinyl-(S)-phenylalaninol amide
-
 Rattus norvegicus
3.4.14.10 2-(2-amino-3-methyl-butyrylamino)-4-phenyl-butyric acid
-
 Rattus norvegicus
3.4.14.10 2-amino-3-methyl-N-(3-phenyl-propyl)-butyramide
-
 Rattus norvegicus
3.4.14.10 2-amino-3-methyl-N-phenethyl-butyramide
-
 Rattus norvegicus
3.4.14.10 2-amino-N-benzyl-3-methyl-butyramide
-
 Rattus norvegicus
3.4.14.10 Ala-Ala-Ala-OH
-
 Rattus norvegicus
3.4.14.10 Ala-Ala-OH
-
 Rattus norvegicus
3.4.14.10 Ala-Ala-Pro-Ala-OH
-
 Rattus norvegicus
3.4.14.10 Ala-Phe-OH
-
 Rattus norvegicus
3.4.14.10 Ala-Pro-Ala-OH
-
 Rattus norvegicus
3.4.14.10 Ala-Pro-OH
-
 Rattus norvegicus
3.4.14.10 Asp-Tyr-Met-OH
-
 Rattus norvegicus
3.4.14.10 butabindide a potent reversible competitive and selective inhibitor Rattus norvegicus
3.4.14.10 butyloxycarbonyl-Val-Nle-OH
-
 Rattus norvegicus
3.4.14.10 CH3-Nle-Nle-NHCH3
-
 Rattus norvegicus
3.4.14.10 CH3CO-Val-Nvl-OH
-
 Rattus norvegicus
3.4.14.10 CH3OCO-Val-Nvl-OH
-
 Rattus norvegicus
3.4.14.10 Gly-Gly-Phe-OH
-
 Rattus norvegicus
3.4.14.10 Gly-Phe-OH
-
 Rattus norvegicus
3.4.14.10 Gly-Trp-Met-OH
-
 Rattus norvegicus
3.4.14.10 Gly-Trp-OH
-
 Rattus norvegicus
3.4.14.10 Gly-Tyr-OH
-
 Rattus norvegicus
3.4.14.10 Gly-Val-Phe-OH
-
 Rattus norvegicus
3.4.14.10 Ile-Pro-Ile-OH
-
 Rattus norvegicus
3.4.14.10 Met-Met-OH
-
 Rattus norvegicus
3.4.14.10 Met-Tyr-OH
-
 Rattus norvegicus
3.4.14.10 Nle-Nle-NHCH3
-
 Rattus norvegicus
3.4.14.10 Nle-Nle-OH
-
 Rattus norvegicus
3.4.14.10 PhCH2-Val-Nvl-OH
-
 Rattus norvegicus
3.4.14.10 PhCH2OCO-Val-Nle-O(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 PhCH2OCO-Val-Val-OH
-
 Rattus norvegicus
3.4.14.10 Val-(4-PhCH2O)Phe-OH
-
 Rattus norvegicus
3.4.14.10 Val-(beta-naphthyl)Ala-OH
-
 Rattus norvegicus
3.4.14.10 Val-(S)-cyclohexylalanyl-NH(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 Val-(S)-cyclohexylalanyl-OH
-
 Rattus norvegicus
3.4.14.10 Val-Ala-OH
-
 Rattus norvegicus
3.4.14.10 Val-Met-OH
-
 Rattus norvegicus
3.4.14.10 Val-Nle-NH(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 Val-Nle-NH(CH2)3Ph
-
 Rattus norvegicus
3.4.14.10 Val-Nle-NHCH3
-
 Rattus norvegicus
3.4.14.10 Val-Nle-O(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 Val-Nle-OH
-
 Rattus norvegicus
3.4.14.10 Val-Nvl-NH(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 Val-Nvl-NHCH3
-
 Rattus norvegicus
3.4.14.10 Val-Nvl-OH
-
 Rattus norvegicus
3.4.14.10 Val-Phe-NH(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 Val-Phe-NH(CH2)CH3
-
 Rattus norvegicus
3.4.14.10 Val-Phe-NHCH3
-
 Rattus norvegicus
3.4.14.10 Val-Phe-O(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 Val-Phe-O(CH2)CH3
-
 Rattus norvegicus
3.4.14.10 Val-Phe-OCH3
-
 Rattus norvegicus
3.4.14.10 Val-Phe-OH
-
 Rattus norvegicus
3.4.14.10 Val-phenylglycine-NHCH3
-
 Rattus norvegicus
3.4.14.10 Val-phenylglycine-OH
-
 Rattus norvegicus
3.4.14.10 Val-Tyr-NHCH3
-
 Rattus norvegicus
3.4.14.10 Val-Tyr-OH
-
 Rattus norvegicus
3.4.14.10 Val-Val-NHCH3
-
 Rattus norvegicus
3.4.14.10 Val-Val-OH
-
 Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
3.4.14.10 Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.14.10 Ala-Ala-Phe 7-amido-4-methylcoumarin + H2O
-
 Rattus norvegicus Ala-Ala-Phe + 7-amino-4-methylcoumarin
-
 ?
3.4.14.10 cholecystokinin-8-sulfate + H2O
-
 Rattus norvegicus Asp-Tyr(SO3H)-Met-OH + Gly-Trp-Met-Asp-Phe-NH2
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.14.10 additional information
-
 additional information Ki-value above 5 mM: Met-Met-OH, Asp-Tyr-OH, PhCH2-Val-Nvl-OH, PhCH2OCO-Val-Nvl-OH, CH3-Nl2-Nle-OCH3. Ki-value above 3.0 mM: CH3-Nle-Nle-NHCH3, PhCH2-Nle-Nle-NHCH3, PhCH2OCO-Val-Nle-O(CH2)3CH3. Ki-value above 0.5 mM: CH3CO-Val-Nvl-OH Rattus norvegicus
3.4.14.10 0.001
-
 Ile-Pro-Ile-OH
-
 Rattus norvegicus
3.4.14.10 0.003
-
 Val-Nvl-NH(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 0.003
-
 Ala-Pro-Ala-OH
-
 Rattus norvegicus
3.4.14.10 0.009
-
 Nle-Nle-NHCH3
-
 Rattus norvegicus
3.4.14.10 0.011
-
 Val-TyrNHCH3
-
 Rattus norvegicus
3.4.14.10 0.014
-
 Val-Nle-NH(CH2)3Ph
-
 Rattus norvegicus
3.4.14.10 0.014
-
 Ala-Ala-Ala-OH
-
 Rattus norvegicus
3.4.14.10 0.02
-
 Gly-Trp-Met-OH
-
 Rattus norvegicus
3.4.14.10 0.02
-
 Val-Phe-NH(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 0.022
-
 Val-Phe-NHCH3
-
 Rattus norvegicus
3.4.14.10 0.028
-
 Val-Nvl-NH(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 0.029
-
 Val-Nle-NH(CH2)3Ph
-
 Rattus norvegicus
3.4.14.10 0.029
-
 Val-phenylglycine-OH
-
 Rattus norvegicus
3.4.14.10 0.029
-
 Gly-Val-Phe-OH
-
 Rattus norvegicus
3.4.14.10 0.033 0.086 2-amino-3-methyl-N-(3-phenyl-propyl)-butyramide
-
 Rattus norvegicus
3.4.14.10 0.046
-
 Val-Val-NHCH3
-
 Rattus norvegicus
3.4.14.10 0.05
-
 Asp-Tyr-Met-OH
-
 Rattus norvegicus
3.4.14.10 0.057
-
 Val-(S)-cyclohexylalanyl-NH(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 0.06
-
 Val-(beta-naphthyl)Ala-OH
-
 Rattus norvegicus
3.4.14.10 0.066
-
 Val-Nle-NHCH3
-
 Rattus norvegicus
3.4.14.10 0.08
-
 2-amino-N-benzyl-3-methyl-butyramide
-
 Rattus norvegicus
3.4.14.10 0.11
-
 Gly-Gly-Phe-OH
-
 Rattus norvegicus
3.4.14.10 0.114
-
 2-amino-3-methyl-N-phenethyl-butyramide
-
 Rattus norvegicus
3.4.14.10 0.114
-
 Ala-Ala-Pro-Ala-OH
-
 Rattus norvegicus
3.4.14.10 0.21
-
 Val-(4-PhCH2O)Phe-OH
-
 Rattus norvegicus
3.4.14.10 0.23
-
 Val-Phe-O(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 0.26
-
 Val-Phe-OCH3
-
 Rattus norvegicus
3.4.14.10 0.29
-
 Val-Nle-O(CH2)3CH3
-
 Rattus norvegicus
3.4.14.10 0.35
-
 Val-Phe-OH
-
 Rattus norvegicus
3.4.14.10 0.43
-
 Val-Nvl-OH
-
 Rattus norvegicus
3.4.14.10 0.47
-
 Gly-Trp-OH
-
 Rattus norvegicus
3.4.14.10 0.57
-
 2-(2-amino-3-methyl-butyrylamino)-4-phenyl-butyric acid
-
 Rattus norvegicus
3.4.14.10 0.6
-
 Val-phenylglycine-OH
-
 Rattus norvegicus
3.4.14.10 0.65
-
 Gly-Trp-OH
-
 Rattus norvegicus
3.4.14.10 0.857
-
 Val-Tyr-OH
-
 Rattus norvegicus
3.4.14.10 0.86
-
 Val-Nle-OH
-
 Rattus norvegicus
3.4.14.10 1
-
 (2S)-2-[[(2S)-2-aminobutanoyl]amino]pentanoic acid
-
 Rattus norvegicus
3.4.14.10 1.14
-
 Ala-Phe-OH
-
 Rattus norvegicus
3.4.14.10 1.4
-
 Ala-Pro-OH
-
 Rattus norvegicus
3.4.14.10 1.43
-
 Nle-Nle-OH
-
 Rattus norvegicus
3.4.14.10 1.66
-
 Val-Val-OH
-
 Rattus norvegicus
3.4.14.10 1.67
-
 Val-Val-OH
-
 Rattus norvegicus
3.4.14.10 1.67
-
 (2S)-2-[[(2S)-2-aminobutanoyl]amino]butanoic acid
-
 Rattus norvegicus
3.4.14.10 2
-
 Met-Tyr-OH
-
 Rattus norvegicus
3.4.14.10 2
-
 Val-Met-OH
-
 Rattus norvegicus
3.4.14.10 2.1
-
 (S)-valinyl-(S)-phenylalaninol amide
-
 Rattus norvegicus
3.4.14.10 3
-
 Val-(S)-cyclohexylalanyl-OH
-
 Rattus norvegicus
3.4.14.10 5
-
 Ala-Ala-OH
-
 Rattus norvegicus
3.4.14.10 9
-
 Val-Ala-OH
-
 Rattus norvegicus