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Literature summary for 3.4.14.10 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

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

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

Ki Value [mM]

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