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Assay Detail

CHEMBL4834989

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

Binding
Inhibition of recombinant UAE (unknown origin) in presence of ATP at Km concentration by HTRF assay
63
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 63 6.52 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4878088 1 7.24
CHEMBL4852015 1 6.33
CHEMBL4860471 1 6.31
CHEMBL4878832 1 6.21
CHEMBL4849766 1 -
CHEMBL4856040 1 -
CHEMBL4862248 2 -
CHEMBL4861509 1 -
CHEMBL4862587 1 -
CHEMBL4848140 1 -
CHEMBL4873487 1 -
CHEMBL4858933 1 -
CHEMBL4867650 1 -
CHEMBL4862901 1 -
CHEMBL4858495 1 -
CHEMBL4873956 1 -
CHEMBL4865157 1 -
CHEMBL4869956 1 -
CHEMBL4860960 1 -
CHEMBL4872222 1 -
CHEMBL4876899 1 -
CHEMBL4848114 1 -
CHEMBL4852516 1 -
CHEMBL4854038 1 -
CHEMBL4877684 1 -
CHEMBL4864361 1 -
CHEMBL4850183 1 -
CHEMBL4860917 1 -
CHEMBL4856793 2 -
CHEMBL4848442 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4878088 IC50 = 58.0 nM 7.24
CHEMBL4852015 IC50 = 468.0 nM 6.33
CHEMBL4860471 IC50 = 492.0 nM 6.31
CHEMBL4878832 IC50 = 616.0 nM 6.21
CHEMBL4858495 IC50 > 1000.0 nM -
CHEMBL4862322 IC50 > 1000.0 nM -
CHEMBL4873956 IC50 > 1000.0 nM -
CHEMBL4865157 IC50 > 1000.0 nM -
CHEMBL4856040 IC50 > 1000.0 nM -
CHEMBL4861656 IC50 > 1000.0 nM -
CHEMBL4851718 IC50 > 1000.0 nM -
CHEMBL4869144 IC50 > 1000.0 nM -
CHEMBL4865086 IC50 > 1000.0 nM -
CHEMBL4849931 IC50 > 1000.0 nM -
CHEMBL4869112 IC50 > 1000.0 nM -
CHEMBL4853650 IC50 > 1000.0 nM -
CHEMBL4865609 IC50 > 1000.0 nM -
CHEMBL4855027 IC50 > 1000.0 nM -
CHEMBL4866833 IC50 > 1000.0 nM -
CHEMBL4864280 IC50 > 1000.0 nM -
CHEMBL4869340 IC50 > 1000.0 nM -
CHEMBL4859486 IC50 > 1000.0 nM -
CHEMBL4870385 IC50 > 1000.0 nM -
CHEMBL4866755 IC50 > 1000.0 nM -
CHEMBL4865787 IC50 > 1000.0 nM -
CHEMBL4861240 IC50 > 1000.0 nM -
CHEMBL4869021 IC50 > 1000.0 nM -
CHEMBL4872222 IC50 > 1000.0 nM -
CHEMBL4852516 IC50 > 1000.0 nM -
CHEMBL4856793 IC50 > 1000.0 nM -
CHEMBL4856793 IC50 > 1000.0 nM -
CHEMBL4860917 IC50 > 1000.0 nM -
CHEMBL4850183 IC50 > 1000.0 nM -
CHEMBL4864361 IC50 > 1000.0 nM -
CHEMBL4877684 IC50 > 1000.0 nM -
CHEMBL4854038 IC50 > 1000.0 nM -
CHEMBL4848114 IC50 > 1000.0 nM -
CHEMBL4848442 IC50 > 1000.0 nM -
CHEMBL4876899 IC50 > 1000.0 nM -
CHEMBL4862901 IC50 > 1000.0 nM -
CHEMBL4860960 IC50 > 1000.0 nM -
CHEMBL4869956 IC50 > 1000.0 nM -
CHEMBL4849766 IC50 > 1000.0 nM -
CHEMBL4862248 IC50 > 1000.0 nM -
CHEMBL4861509 IC50 > 1000.0 nM -
CHEMBL4862587 IC50 > 1000.0 nM -
CHEMBL4848140 IC50 > 1000.0 nM -
CHEMBL4873487 IC50 > 1000.0 nM -
CHEMBL4858933 IC50 > 1000.0 nM -
CHEMBL4867650 IC50 > 1000.0 nM -