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Assay Detail

CHEMBL4377290

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

Binding
Inhibition of biotin-H3(1-23)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 90 mins by AlphaLISA assay
5
Total Activities
5
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

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
IC50 5 6.56 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3109630 1 7.14
CHEMBL4552020 1 7.11
CHEMBL4588285 1 6.47
CHEMBL1231795 1 5.50
CHEMBL4450765 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3109630 IC50 = 72.0 nM 7.14
CHEMBL4552020 IC50 = 77.0 nM 7.11
CHEMBL4588285 IC50 = 338.0 nM 6.47
CHEMBL1231795 IC50 = 3200.0 nM 5.50
CHEMBL4450765 IC50 - -