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Assay Detail

CHEMBL4041200

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

Binding
Displacement of [3H]-cyclopamine from human wild-type SMO receptor expressed in HEK293T cell membranes by liquid scintillation spectrometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein smoothened (CHEMBL5971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer.
Morgillo F, Amendola G, Della Corte CM, Giacomelli C, Botta L, Di Maro S, Messere A, Ciaramella V, Taliani S, Marinelli L, Trincavelli ML, Martini C, Novellino E, Ciardiello F, Cosconati S.
J Med Chem (2017) 60 : 7447 -7458
PubMed 28787156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.30 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254760 1 7.38
CHEMBL1230609 FORETINIB 2.0 1 7.22
CHEMBL1614725 TAK-285 1.0 1 -
CHEMBL1779065 1 -
CHEMBL1796172 1 -
CHEMBL4101154 1 -
CHEMBL460702 BMS-777607 2.0 1 -
CHEMBL1852688 INFIGRATINIB 4.0 1 -
CHEMBL2029988 CEP-32496 2.0 1 -
CHEMBL4105444 1 -
CHEMBL386051 1 -
CHEMBL223360 LINIFANIB 3.0 1 -
CHEMBL254129 CYCLOPAMINE 1 -
CHEMBL473417 VISMODEGIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254760 Ki = 41.7 nM 7.38
CHEMBL1230609 FORETINIB Ki = 59.7 nM 7.22
CHEMBL1614725 TAK-285 Ki - -
CHEMBL1779065 Ki - -
CHEMBL1796172 Ki - -
CHEMBL4101154 Ki - -
CHEMBL460702 BMS-777607 Ki - -
CHEMBL1852688 INFIGRATINIB Ki - -
CHEMBL2029988 CEP-32496 Ki - -
CHEMBL4105444 Ki - -
CHEMBL386051 Ki - -
CHEMBL223360 LINIFANIB Ki - -
CHEMBL254129 CYCLOPAMINE Ki - -
CHEMBL473417 VISMODEGIB Ki - -