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Assay Detail

CHEMBL5654572

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

Binding
Inhibition of human PRMT5
1
Total Activities
1
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 5 (CHEMBL1795116)
Type SINGLE PROTEIN
Organism Homo sapiens

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 1 6.30 6.30

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2169919 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2169919 IC50 = 500.0 nM 6.30