Literature summary for 3.4.21.37 extracted from

Kapui, Z.; Varga, M.; Urban-Szabo, K.; Mikus, E.; Szabo, T.; Szeredi, J.; Batori, S.; Finance, O.; Aranyi, P.
Biochemical and pharmacological characterization of 2-(9-(2-piperidinoethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yloxymethyl)-4 -(1-methylethyl)-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide (SSR69071), a novel, orally active elastase inhibitor (2003), J. Pharmacol. Exp. Ther., 305, 451-459.

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Application

Application	Comment	Organism
medicine	imbalance between elastase and its endogenous inhibitors may result in several pathophysiological states such as chronic obstructive pulmonary disease, asthma, emphysema, cystic fibrosis and chronic inflammatory diseases. An orally active leukocyte elastase can be useful for the treatment of these diseases. SSR69071 is a selective, orally active, and potent inhibitor of leukocyte elastase with good penetration in respiratory tissues	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
SSR69071	i.e. 2-(9-(2-piperidinoethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yloxymethyl)-4-(1-methylethyl)-6-methoxy-1,2-benzisothiazol-3-one-1,1-dioxide, a selective, orally active, and potent inhibitor of leukocyte elastase with good penetration in respiratory tissues	Homo sapiens
SSR69071	-	Mus musculus
SSR69071	-	Oryctolagus cuniculus
SSR69071	-	Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
additional information	Homo sapiens	imbalance between elastase and its endogenous inhibitors may result in several pathophysiological states such as chronic obstructive pulmonary disease, asthma, emphysema, cystic fibrosis and chronic inflammatory diseases	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Mus musculus	-	-	-
Oryctolagus cuniculus	-	-	-
Rattus norvegicus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
sputum	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	imbalance between elastase and its endogenous inhibitors may result in several pathophysiological states such as chronic obstructive pulmonary disease, asthma, emphysema, cystic fibrosis and chronic inflammatory diseases	Homo sapiens	?	-	?

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0000000168	-	SSR69071	pH 7.8	Homo sapiens
0.00000168	-	SSR69071	pH 7.8	Mus musculus
0.00000301	-	SSR69071	pH 7.8	Rattus norvegicus
0.000005571	-	ZD8321	pH 7.8	Homo sapiens
0.00003475	-	ZD8321	pH 7.8	Mus musculus
0.000058	-	SSR69071	pH 7.8	Oryctolagus cuniculus
0.00006	-	ZD8321	pH 7.8	Rattus norvegicus
0.000139	-	ZD8321	pH 7.8	Oryctolagus cuniculus

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Release 2023.1 (January 2023)