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Assay Detail

CHEMBL5546247

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

Binding
Displacement of FL-H3K4me3 peptide from human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assay
18
Total Activities
18
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, Selective, and Cell-Active SPIN1 Inhibitor.
Xiong Y, Greschik H, Johansson C, Seifert L, Gamble V, Park KS, Fagan V, Li F, Chau I, Vedadi M, Arrowsmith CH, Brennan P, Fedorov O, Jung M, Farnie G, Liu J, Oppermann U, Schüle R, Jin J.
J Med Chem (2024) 67 : 5837 -5853
PubMed 38533580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.08 6.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5570983 1 6.73
CHEMBL5572612 1 6.71
CHEMBL5575071 1 6.70
CHEMBL5594627 1 6.70
CHEMBL5575917 1 6.69
CHEMBL5564247 1 6.67
CHEMBL5583678 1 6.67
CHEMBL5572650 1 6.51
CHEMBL5590823 1 6.49
CHEMBL5568957 1 6.46
CHEMBL5565204 1 6.08
CHEMBL5573051 1 5.88
CHEMBL5572233 1 5.76
CHEMBL5573430 1 5.69
CHEMBL5575971 1 5.40
CHEMBL1231795 1 5.13
CHEMBL5593870 1 5.10
CHEMBL5584133 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5570983 IC50 = 187.0 nM 6.73
CHEMBL5572612 IC50 = 197.0 nM 6.71
CHEMBL5575071 IC50 = 200.0 nM 6.70
CHEMBL5594627 IC50 = 202.0 nM 6.70
CHEMBL5575917 IC50 = 203.0 nM 6.69
CHEMBL5564247 IC50 = 214.0 nM 6.67
CHEMBL5583678 IC50 = 215.0 nM 6.67
CHEMBL5572650 IC50 = 312.0 nM 6.51
CHEMBL5590823 IC50 = 326.0 nM 6.49
CHEMBL5568957 IC50 = 348.0 nM 6.46
CHEMBL5565204 IC50 = 838.0 nM 6.08
CHEMBL5573051 IC50 = 1320.0 nM 5.88
CHEMBL5572233 IC50 = 1740.0 nM 5.76
CHEMBL5573430 IC50 = 2060.0 nM 5.69
CHEMBL5575971 IC50 = 3990.0 nM 5.40
CHEMBL1231795 IC50 = 7360.0 nM 5.13
CHEMBL5593870 IC50 = 7970.0 nM 5.10
CHEMBL5584133 IC50 = 84300.0 nM 4.07