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Assay Detail

CHEMBL1026048

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

Binding
Inhibition of exogenously transfected human Gli2 delta-N-mediated transcriptional activity in mouse C3H10T1/2 cells after 24 hrs by luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C3H 10T1/2
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Zinc finger protein GLI2 (CHEMBL5119)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships and cancer-cell selective toxicity of novel inhibitors of glioma-associated oncogene homologue 1 (Gli1) mediated transcription.
Mahindroo N, Connelly MC, Punchihewa C, Kimura H, Smeltzer MP, Wu S, Fujii N.
J Med Chem (2009) 52 : 4277 -4287
PubMed 19545120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.57 4.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL551292 1 4.69
CHEMBL561023 1 4.62
CHEMBL560356 1 4.53
CHEMBL562034 1 4.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL551292 IC50 = 20500.0 nM 4.69
CHEMBL561023 IC50 = 23900.0 nM 4.62
CHEMBL560356 IC50 = 29400.0 nM 4.53
CHEMBL562034 IC50 = 35200.0 nM 4.45