Literature summary for 3.4.23.46 extracted from

Fobare, W.F.; Solvibile, W.R.; Robichaud, A.J.; Malamas, M.S.; Manas, E.; Turner, J.; Hu, Y.; Wagner, E.; Chopra, R.; Cowling, R.; Jin, G.; Bard, J.
Thiophene substituted acylguanidines as BACE1 inhibitors (2007), Bioorg. Med. Chem. Lett., 17, 5353-5356.

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Application

Application	Comment	Organism
pharmacology	design of inhibitor drugs for treatment of Alzheimer disease	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
inhibitor binding site depicted, enhanced affinity by propyloxyphenyl substituent and projection into the S1-S3 pocket of the BACE1 site confirmed, molecular surface model and stereoview indicated	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
additional information	design of selective non-peptidic small molecule inhibitors of beta-secretase BACE1, substitution of a thiophene ring for the key pyrrole nucleus in a series of substituted acylguanidines performed	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P56817	-	-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg]	Specific Activity Maximum [µmol/min/mg]	Comment	Organism
additional information	-	generation of selective non-peptidic small molecule inhibitors of BACE1, reagents and synthetic route summarized	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	non-peptidic small molecule inhibitors of beta-secretase BACE1 generated, inhibitory activities analyzed by BACE1-FRET assay	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
BACE1	-	Homo sapiens
beta-secretase	-	Homo sapiens

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Release 2023.1 (January 2023)