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Assay Detail

CHEMBL3744150

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

Binding
Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein smoothened (CHEMBL5971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of novel N-3-benzimidazolephenylbisamide derivatives for antiproliferative and Hedgehog pathway inhibitory activity
Sun C, Li Y, Shi A, Zhang J, Li Y, Zhao M, Zhang L, Zheng H, Meng Y, Ding H, Song H
Medchemcomm (2015) 6 : 1137 -1142
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.47 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473417 VISMODEGIB 4.0 1 8.22
CHEMBL3741651 1 7.72
CHEMBL3740447 1 7.38
CHEMBL2031084 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473417 VISMODEGIB IC50 = 6.0 nM 8.22
CHEMBL3741651 IC50 = 19.0 nM 7.72
CHEMBL3740447 IC50 = 42.0 nM 7.38
CHEMBL2031084 IC50 = 281.0 nM 6.55