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Assay Detail

CHEMBL4628152

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Binding
Inhibition of SMO D473H mutant receptor (unknown origin) assessed as inhibition of SAG-induced Hh signaling pathway by Gli luciferase reporter cell-based assay
22
Total Activities
22
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

Protein smoothened (CHEMBL5971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors.
Ji D, Zhang W, Xu Y, Zhang JJ.
Bioorg Med Chem (2020) 28 : 115354 -115354
PubMed 32063403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.24 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2142592 TALADEGIB 2.0 1 8.38
CHEMBL473417 VISMODEGIB 4.0 1 7.88
CHEMBL4632598 1 7.47
CHEMBL4644288 1 6.91
CHEMBL4635021 1 6.54
CHEMBL4639888 1 6.51
CHEMBL4632537 1 6.25
CHEMBL4645447 1 6.12
CHEMBL4641704 1 5.88
CHEMBL4646599 1 5.72
CHEMBL4644469 1 5.36
CHEMBL4647112 1 5.31
CHEMBL4632758 1 5.16
CHEMBL4649551 1 5.15
CHEMBL4633504 1 5.03
CHEMBL4642236 1 -
CHEMBL4648312 1 -
CHEMBL4642779 1 -
CHEMBL4646912 1 -
CHEMBL4639086 1 -
CHEMBL4639103 1 -
CHEMBL4641820 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2142592 TALADEGIB IC50 = 4.17 nM 8.38
CHEMBL473417 VISMODEGIB IC50 = 13.06 nM 7.88
CHEMBL4632598 IC50 = 34.09 nM 7.47
CHEMBL4644288 IC50 = 123.4 nM 6.91
CHEMBL4635021 IC50 = 285.25 nM 6.54
CHEMBL4639888 IC50 = 308.7 nM 6.51
CHEMBL4632537 IC50 = 561.9 nM 6.25
CHEMBL4645447 IC50 = 754.05 nM 6.12
CHEMBL4641704 IC50 = 1328.0 nM 5.88
CHEMBL4646599 IC50 = 1909.5 nM 5.72
CHEMBL4644469 IC50 = 4365.5 nM 5.36
CHEMBL4647112 IC50 = 4858.0 nM 5.31
CHEMBL4632758 IC50 = 6864.0 nM 5.16
CHEMBL4649551 IC50 = 7117.0 nM 5.15
CHEMBL4633504 IC50 = 9369.5 nM 5.03
CHEMBL4642236 IC50 > 10000.0 nM -
CHEMBL4648312 IC50 > 10000.0 nM -
CHEMBL4642779 IC50 > 10000.0 nM -
CHEMBL4646912 IC50 > 10000.0 nM -
CHEMBL4639086 IC50 > 10000.0 nM -
CHEMBL4639103 IC50 > 10000.0 nM -
CHEMBL4641820 IC50 > 10000.0 nM -