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Assay Detail

CHEMBL5050108

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

Binding
Binding affinity to CRBN (unknown origin) measured by Fluorescent Polarization assay
12
Total Activities
12
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

Protein cereblon (CHEMBL3763008)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
Alcock LJ, Chang Y, Jarusiewicz JA, Actis M, Nithianantham S, Mayasundari A, Min J, Maxwell D, Hunt J, Smart B, Yang JJ, Nishiguchi G, Fischer M, Mullighan CG, Rankovic Z.
ACS Med Chem Lett (2022) 13 : 475 -482
PubMed 35300081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.36 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5090416 1 10.70
CHEMBL4744617 1 9.51
CHEMBL5078429 1 9.35
CHEMBL5082689 1 8.95
CHEMBL4742130 1 8.81
CHEMBL5090604 1 8.42
CHEMBL5074539 1 7.82
CHEMBL5073737 1 7.72
CHEMBL5082136 1 7.71
CHEMBL5092577 1 7.70
CHEMBL5077200 1 7.62
CHEMBL5094176 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5090416 IC50 = 0.02 nM 10.70
CHEMBL4744617 IC50 = 0.31 nM 9.51
CHEMBL5078429 IC50 = 0.45 nM 9.35
CHEMBL5082689 IC50 = 1.13 nM 8.95
CHEMBL4742130 IC50 = 1.55 nM 8.81
CHEMBL5090604 IC50 = 3.81 nM 8.42
CHEMBL5074539 IC50 = 15.0 nM 7.82
CHEMBL5073737 IC50 = 19.0 nM 7.72
CHEMBL5082136 IC50 = 19.6 nM 7.71
CHEMBL5092577 IC50 = 20.2 nM 7.70
CHEMBL5077200 IC50 = 23.9 nM 7.62
CHEMBL5094176 IC50 = 1045.0 nM 5.98