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Assay Detail

CHEMBL5657204

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

Binding
Binding affinity to PRMT3 (unknown origin) assessed as dissociation constant by ITC analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
4
Assay Parameters

Assay Information

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

Target

Protein arginine N-methyltransferase 3 (CHEMBL5891)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I, Lin Y, Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon M, Lin-Jones J, Huang XP, Roth BL, Schapira M, Atadja P, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M.
Angew Chem Int Ed Engl (2015) 54 : 5166 -5170
PubMed 25728001 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 7.28 7.28

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0008116
EFO_ID EFO_ID - EFO:0001645
EFO_TERM EFO_TERM - oculopharyngeal muscular dystrophy
EFO_TERM EFO_TERM - coronary artery disease

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4072005 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4072005 Kd = 53.0 nM 7.28