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Assay Detail

CHEMBL5539300

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

Binding
Inhibition of MLL1/WDR5 (unknown origin) protein-protein interaction incubated for 60 mins by HTRF analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone-lysine N-methyltransferase 2A/WDR5 (CHEMBL3883320)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach.
Qin S, Feng L, Zhao Q, Yan Z, Lyu X, Li K, Mu B, Chen Y, Lu W, Wang C, Suo Y, Yue J, Cui M, Li Y, Zhao Y, Duan Z, Zhu J, Lu X.
J Med Chem (2024) 67 : 1079 -1092
PubMed 38166388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.42 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4588661 1 8.17
CHEMBL5562523 1 8.07
CHEMBL5573350 1 8.01
CHEMBL5579746 1 7.95
CHEMBL5572054 1 7.81
CHEMBL5565914 1 7.76
CHEMBL5576035 1 7.73
CHEMBL5575058 1 7.60
CHEMBL5572530 1 7.57
CHEMBL5571097 1 7.49
CHEMBL5579685 1 7.40
CHEMBL5595245 1 7.39
CHEMBL5592145 1 7.38
CHEMBL5590145 1 7.30
CHEMBL5591718 1 7.12
CHEMBL5574146 1 7.07
CHEMBL5579747 1 6.83
CHEMBL5562904 1 6.66
CHEMBL5573257 1 6.62
CHEMBL5574810 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4588661 IC50 = 6.8 nM 8.17
CHEMBL5562523 IC50 = 8.6 nM 8.07
CHEMBL5573350 IC50 = 9.8 nM 8.01
CHEMBL5579746 IC50 = 11.3 nM 7.95
CHEMBL5572054 IC50 = 15.5 nM 7.81
CHEMBL5565914 IC50 = 17.2 nM 7.76
CHEMBL5576035 IC50 = 18.8 nM 7.73
CHEMBL5575058 IC50 = 25.2 nM 7.60
CHEMBL5572530 IC50 = 26.9 nM 7.57
CHEMBL5571097 IC50 = 32.4 nM 7.49
CHEMBL5579685 IC50 = 39.5 nM 7.40
CHEMBL5595245 IC50 = 40.5 nM 7.39
CHEMBL5592145 IC50 = 41.6 nM 7.38
CHEMBL5590145 IC50 = 50.0 nM 7.30
CHEMBL5591718 IC50 = 75.8 nM 7.12
CHEMBL5574146 IC50 = 84.6 nM 7.07
CHEMBL5579747 IC50 = 148.7 nM 6.83
CHEMBL5562904 IC50 = 220.7 nM 6.66
CHEMBL5573257 IC50 = 239.2 nM 6.62
CHEMBL5574810 IC50 = 319.0 nM 6.50