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Assay Detail

CHEMBL5659516

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Binding
Inhibition of PRMT5 in human Z138 cells assessed as effect on SDMA level incubated for 3 days by ELISA analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Z138
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing.
Gerhart SV, Kellner WA, Thompson C, Pappalardi MB, Zhang XP, Montes de Oca R, Penebre E, Duncan K, Boriack-Sjodin A, Le B, Majer C, McCabe MT, Carpenter C, Johnson N, Kruger RG, Barbash O.
Sci Rep (2018) 8 : 9711 -9711
PubMed 29946150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.64 8.68

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
CHEMBL4542380 1 8.68
CHEMBL4466233 PEMRAMETOSTAT 2.0 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4542380 EC50 = 2.1 nM 8.68
CHEMBL4466233 PEMRAMETOSTAT EC50 = 2.5 nM 8.60