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Assay Detail

CHEMBL4377295

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

Binding
Inhibition of C-terminal Halo Tag-histone H3.3/N-terminal Nano Luciferase-fused full length SPIN1 (unknown origin) transfected in human U2OS cells assessed as reduction in SPIN1 and histone H3 interaction incubated for 24 hrs by NanoBRET assay
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Spindlin-1 (CHEMBL4523509)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).
Xiong Y, Greschik H, Johansson C, Seifert L, Bacher J, Park KS, Babault N, Martini M, Fagan V, Li F, Chau I, Christott T, Dilworth D, Barsyte-Lovejoy D, Vedadi M, Arrowsmith CH, Brennan P, Fedorov O, Jung M, Farnie G, Liu J, Oppermann U, Schüle R, Jin J.
J Med Chem (2019) 62 : 8996 -9007
PubMed 31260300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 2 - -
IC50 1 5.50 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4552020 2 5.50
CHEMBL4450765 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4552020 IC50 = 3200.0 nM 5.50
CHEMBL4552020 Inhibition - % -
CHEMBL4450765 Inhibition - % -