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Assay Detail

CHEMBL5654576

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

Functional
Downregulation of H3K79 methylation in human A-431 cells incubated for 3 to 4 days by microscopy based analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-431
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M.
Nat Commun (2012) 3 : 1288 -1288
PubMed 23250418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.58 8.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3087498 1 8.58
CHEMBL2169919 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3087498 IC50 = 2.65 nM 8.58
CHEMBL2169919 IC50 = 264.0 nM 6.58