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Assay Detail

CHEMBL4834994

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

Binding
Inhibition of NAE (unknown origin) using Nedd-8 as substrate incubated for 60 mins in presence of ATP and PPi by pyrophosphate exchange assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

NEDD8 activating enzyme (CHEMBL3831283)
Type PROTEIN COMPLEX
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
IC50 2 6.05 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4878088 1 6.52
CHEMBL4865086 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4878088 IC50 = 300.0 nM 6.52
CHEMBL4865086 IC50 = 2600.0 nM 5.58