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Assay Detail

CHEMBL4835009

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.
Langston SP, Grossman S, England D, Afroze R, Bence N, Bowman D, Bump N, Chau R, Chuang BC, Claiborne C, Cohen L, Connolly K, Duffey M, Durvasula N, Freeze S, Gallery M, Galvin K, Gaulin J, Gershman R, Greenspan P, Grieves J, Guo J, Gulavita N, Hailu S, He X, Hoar K, Hu Y, Hu Z, Ito M, Kim MS, Lane SW, Lok D, Lublinsky A, Mallender W, McIntyre C, Minissale J, Mizutani H, Mizutani M, Molchinova N, Ono K, Patil A, Qian M, Riceberg J, Shindi V, Sintchak MD, Song K, Soucy T, Wang Y, Xu H, Yang X, Zawadzka A, Zhang J, Pulukuri SM.
J Med Chem (2021) 64 : 2501 -2520
PubMed 33631934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.07 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4862901 1 7.20
CHEMBL4870385 1 7.05
CHEMBL4856793 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4862901 EC50 = 63.0 nM 7.20
CHEMBL4870385 EC50 = 90.0 nM 7.05
CHEMBL4856793 EC50 = 110.0 nM 6.96