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Literature summary for 3.5.1.98 extracted from

  • Shultz, M.; Fan, J.; Chen, C.; Cho, Y.S.; Davis, N.; Bickford, S.; Buteau, K.; Cao, X.; Holmqvist, M.; Hsu, M.; Jiang, L.; Liu, G.; Lu, Q.; Patel, C.; Suresh, J.R.; Selvaraj, M.; Urban, L.; Wang, P.; Yan-Neale, Y.; Whitehead, L.; Zhang, H.; Zhou, L.; Atadja, P.
    The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors (2011), Bioorg. Med. Chem. Lett., 21, 4909-4912.
    View publication on PubMed
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Cloned(Commentary)

Cloned (Comment) Organism
isoform HDAC1 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E)-N-hydroxy-3-[2-[(4-methoxyphenyl)sulfonyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide anti-proliferative activity in human HCT116 cell line, IC50 0.93 microM Homo sapiens
(2E)-N-hydroxy-3-[2-[2-(1H-indol-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide anti-proliferative activity in human HCT116 cell line, IC50 0.22 microM Homo sapiens
(2E)-N-hydroxy-3-[2-[2-(2-methyl-1H-indol-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide anti-proliferative activity in human HCT116 cell line, IC50 0.1042microM. Compound has a reasonable combination of potency, solubility and human microsomal stability to justify further investigation Homo sapiens
(2E)-N-hydroxy-3-[2-[2-(pyrazolo[1,5-a]pyridin-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide anti-proliferative activity in human HCT116 cell line, IC50 0.53 microM. Compound has a reasonable combination of potency, solubility and human microsomal stability to justify further investigation Homo sapiens
N-hydroxy-3-[2-[(2-methyl-1H-indol-3-yl)acetyl]-2,3-dihydro-1H-isoindol-5-yl]propanamide anti-proliferative activity in human HCT116 cell line, IC50 0.19 microM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HCT-116 cell
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000016
-
 isoform HDAC1, pH not specified in the publication, temperature not specified in the publication Homo sapiens (2E)-N-hydroxy-3-[2-[2-(1H-indol-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
0.00002
-
 isoform HDAC1, pH not specified in the publication, temperature not specified in the publication Homo sapiens N-hydroxy-3-[2-[(2-methyl-1H-indol-3-yl)acetyl]-2,3-dihydro-1H-isoindol-5-yl]propanamide
0.000026
-
 isoform HDAC1, pH not specified in the publication, temperature not specified in the publication Homo sapiens (2E)-N-hydroxy-3-[2-[2-(2-methyl-1H-indol-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
0.000078
-
 isoform HDAC1, pH not specified in the publication, temperature not specified in the publication Homo sapiens (2E)-N-hydroxy-3-[2-[2-(pyrazolo[1,5-a]pyridin-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
0.00093
-
 isoform HDAC1, pH not specified in the publication, temperature not specified in the publication Homo sapiens (2E)-N-hydroxy-3-[2-[(4-methoxyphenyl)sulfonyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide