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Assay Detail

CHEMBL1026025

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

Binding
Inhibition of exogenously transfected human Gli1-mediated transcriptional activity in mouse C3H10T1/2 cells after 24 hrs by luciferase reporter gene assay
18
Total Activities
18
Compounds Tested
2
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 GLI1 (CHEMBL5461)
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
Inhibition 14 - -
IC50 4 5.02 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL561023 1 5.16
CHEMBL551292 1 5.03
CHEMBL560356 1 4.94
CHEMBL562034 1 4.94
CHEMBL559433 1 -
CHEMBL562355 1 -
CHEMBL563827 1 -
CHEMBL152297 1 -
CHEMBL539668 1 -
CHEMBL538430 1 -
CHEMBL571903 1 -
CHEMBL541007 1 -
CHEMBL562096 1 -
CHEMBL558674 1 -
CHEMBL562217 1 -
CHEMBL552295 1 -
CHEMBL75435 DEXKETOPROFEN 4.0 1 -
CHEMBL254129 CYCLOPAMINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL561023 IC50 = 6900.0 nM 5.16
CHEMBL551292 IC50 = 9400.0 nM 5.03
CHEMBL560356 IC50 = 11400.0 nM 4.94
CHEMBL562034 IC50 = 11400.0 nM 4.94
CHEMBL559433 Inhibition - % -
CHEMBL562355 Inhibition - % -
CHEMBL563827 Inhibition - % -
CHEMBL152297 Inhibition - % -
CHEMBL539668 Inhibition - % -
CHEMBL538430 Inhibition - % -
CHEMBL571903 Inhibition - % -
CHEMBL541007 Inhibition - % -
CHEMBL562096 Inhibition - % -
CHEMBL558674 Inhibition - % -
CHEMBL562217 Inhibition - % -
CHEMBL552295 Inhibition - % -
CHEMBL75435 DEXKETOPROFEN Inhibition - % -
CHEMBL254129 CYCLOPAMINE Inhibition - % -