Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5511283

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

Binding
Binding affinity to human NSD3 PWWP1 domain (263 to 398 residues) expressed in Escherichia coli Bl21 (DE3) gold cells assessed as dissociation constant measured upto 180 secs by SPR analysis
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone-lysine N-methyltransferase NSD3 (CHEMBL3108646)
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
Kd 9 5.75 6.90
pKd 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4778517 1 6.90
CHEMBL5559507 1 4.60
CHEMBL5563959 1 -
CHEMBL5560105 1 -
CHEMBL5517868 1 -
CHEMBL5559177 1 -
CHEMBL5561556 1 -
CHEMBL5527939 1 -
CHEMBL5542933 1 -
CHEMBL5556168 1 -
CHEMBL5542423 1 -
CHEMBL5566275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4778517 Kd = 125.89 nM 6.90
CHEMBL5559507 Kd = 25118.86 nM 4.60
CHEMBL5563959 pKd - -
CHEMBL5560105 pKd - -
CHEMBL5517868 Kd > 31622.78 nM -
CHEMBL5559177 Kd > 31622.78 nM -
CHEMBL5561556 pKd - -
CHEMBL5527939 Kd > 31622.78 nM -
CHEMBL5542933 Kd > 31622.78 nM -
CHEMBL5556168 Kd > 31622.78 nM -
CHEMBL5542423 Kd > 31622.78 nM -
CHEMBL5566275 Kd > 31622.78 nM -