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Assay Detail

CHEMBL5511287

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Binding
Inhibition of C-terminal nanoluc-tagged NSD2 PWWP1 domain (208 to 396 residues) in human U2OS cells incubated for 2 hrs by NanoBRET target engagement assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone-lysine N-methyltransferase NSD2 (CHEMBL3108645)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Novel Potent NSD2-PWWP1 Ligands Using Structure-Based Design and Computational Approaches.
Carlino L, Astles PC, Ackroyd B, Ahmed A, Chan C, Collie GW, Dale IL, O'Donovan DH, Fawcett C, di Fruscia P, Gohlke A, Guo X, Hao-Ru Hsu J, Kaplan B, Milbradt AG, Northall S, Petrović D, Rivers EL, Underwood E, Webb A.
J Med Chem (2024) 67 : 8962 -8987
PubMed 38748070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5559507 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5559507 IC50 = 3.981 nM 8.40