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Assay Detail

CHEMBL4701074

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

Binding
Binding affinity to wild-type human partial length KIT (I571 to D952 residues) expressed in bacterial expression system by Kinomescan method
1
Total Activities
1
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

Mast/stem cell growth factor receptor Kit (CHEMBL1936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Ma B,Bohnert T,Otipoby KL,Tien E,Arefayene M,Bai J,Bajrami B,Bame E,Chan TR,Humora M,MacPhee JM,Marcotte D,Mehta D,Metrick CM,Moniz G,Polack E,Poreci U,Prefontaine A,Sheikh S,Schroeder P,Smirnakis K,Zhang L,Zheng F,Hopkins BT
J Med Chem (2020) 63 : 12526 -12541
PubMed 32696648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 6.82 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4755663 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4755663 Kd = 150.0 nM 6.82