BDBM24498 3-(3-fluoro-4-{[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)-1-(2-phenylacetyl)thiourea::CHEMBL254760::US10464902, MGCD-265::thieno[3,2-b]pyridine-based inhibitor, 10a

SMILES Cn1cnc(c1)-c1cc2nccc(Oc3ccc(NC(=S)NC(=O)Cc4ccccc4)cc3F)c2s1

InChI Key InChIKey=UFICVEHDQUKCEA-UHFFFAOYSA-N

Data  2 KI  10 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 12 hits for monomerid = 24498   

TargetHepatocyte growth factor receptor(Human)
Methylgene

LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 29nMpH: 7.5 T: 2°CAssay Description:Inhibition of kinase activity was measured in a DELFIA assay (Perkin-Elmer). The substrate poly (Glu4, Tyr) was immobilized onto black high-binding p...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/16/2008
Entry Details Article
PubMed
LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 10nMAssay Description:Inhibition of kinase activity was measured in a DELFIA assay (Perkin-Elmer). The substrate poly (Glu4, Tyr) was immobilized onto black high-binding p...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/16/2008
Entry Details Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Methylgene

LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 29nMAssay Description:Inhibition of c-Met (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Methylgene

LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 37nMAssay Description:Inhibition of GST-fused recombinant c-Met catalytic domain expressed in baculovirus-infected Trichoplusia ni Hi5 cells after 30 mins by DELFIA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 26nMAssay Description:Inhibition of GST-fused recombinant VGFR2 catalytic domain expressed in baculovirus-infected Sf9 cells after 10 mins by DELFIA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Methylgene

LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 50nMAssay Description:Inhibition of TPR-fused Met phosphorylation expressed in human 293T cells by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Methylgene

LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 1nMAssay Description:Inhibition of MET (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2017
Entry Details Article
PubMed
LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 1nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2017
Entry Details Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Methylgene

LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 37nMAssay Description:Inhibition of human c-METMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Methylgene

LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataIC50: 37nMAssay Description:Inhibition of GST-tagged c-Met expressed in Sf9 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataKi:  3nMAssay Description:Compounds 2-4 and cabozantinib were each tested for binding of c-Met, VEGFR2, TIE2 and the control compound, staurosporine. Specifically, each compou...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/8/2020
Entry Details
Go to US Patent

TargetSmoothened homolog(Human)
University of Campania Luigi Vanvitelli

Curated by ChEMBL
LigandPNGBDBM24498(CHEMBL254760 | 3-(3-fluoro-4-{[2-(1-methyl-1H-imid...)
Affinity DataKi:  42nMAssay Description:Displacement of [3H]-cyclopamine from human wild-type SMO receptor expressed in HEK293T cell membranes by liquid scintillation spectrometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/28/2019
Entry Details Article
PubMed