Literature summary for 3.4.21.35 extracted from

Santos, J.A.; Kondo, M.Y.; Freitas, R.F.; dos Santos, M.H.; Ramalho, T.C.; Assis, D.M.; Juliano, L.; Juliano, M.A.; Puzer, L.
The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins (2016), Bioorg. Med. Chem. Lett., 26, 1485-1489 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
fukugetin	mixed-type inhibitor	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.00062	-	Abz-KLRSSQ-EDDnp	isoform KLK2, at pH 7.5 and 37°C	Homo sapiens
0.00065	-	Abz-KLRSSQ-EDDnp	isoform KLK1, at pH 7.5 and 37°C	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
Abz-KLRSSQ-EDDnp + H2O	-	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
KLK1	isoform	Homo sapiens
KLK2	isoform	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0016	-	fukugetin	isoform KLK2, at pH 7.5 and 37°C	Homo sapiens
0.0036	-	fukugetin	isoform KLK1, at pH 7.5 and 37°C	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0032	-	isoform KLK2, at pH 7.5 and 37°C	Homo sapiens	fukugetin
0.0057	-	isoform KLK1, at pH 7.5 and 37°C	Homo sapiens	fukugetin

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Release 2023.1 (January 2023)