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

CHEMBL3801642

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

Binding
Binding affinity to human poly His-tagged WDR5 (1 to 334 residues) expressed in Escherichia coli BL21(DE3)-V2R-pRARE2 cells by surface plasmon resonance analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

WD repeat-containing protein 5 (CHEMBL1075317)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).
Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R.
J Med Chem (2016) 59 : 2478 -2496
PubMed 26958703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 14 6.98 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3798846 1 7.52
CHEMBL3799608 1 7.52
CHEMBL3799704 1 7.40
CHEMBL3798198 1 7.40
CHEMBL3799127 1 7.40
CHEMBL3799275 1 7.30
CHEMBL3799840 1 7.30
CHEMBL3800054 1 7.30
CHEMBL3797967 1 6.68
CHEMBL3798578 1 6.48
CHEMBL3797611 1 6.47
CHEMBL2337032 1 6.42
CHEMBL3800271 1 6.41
CHEMBL3798573 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3798846 Kd = 30.0 nM 7.52
CHEMBL3799608 Kd = 30.0 nM 7.52
CHEMBL3799704 Kd = 40.0 nM 7.40
CHEMBL3798198 Kd = 40.0 nM 7.40
CHEMBL3799127 Kd = 40.0 nM 7.40
CHEMBL3799275 Kd = 50.0 nM 7.30
CHEMBL3799840 Kd = 50.0 nM 7.30
CHEMBL3800054 Kd = 50.0 nM 7.30
CHEMBL3797967 Kd = 210.0 nM 6.68
CHEMBL3798578 Kd = 330.0 nM 6.48
CHEMBL3797611 Kd = 340.0 nM 6.47
CHEMBL2337032 Kd = 380.0 nM 6.42
CHEMBL3800271 Kd = 390.0 nM 6.41
CHEMBL3798573 Kd = 720.0 nM 6.14