BDBM313137 1-(6,7-dimethoxyquinazolin-4-yl)-N3-(4-(1-methylpiperidin-4-yl)phenyl)-1H-1,2,4-triazole-3,5-diamine::US10166216, Compound 168

SMILES COc1cc2ncnc(-n3nc(Nc4ccc(cc4)C4CCN(C)CC4)nc3N)c2cc1OC

InChI Key InChIKey=WUUMPUXBJDJUOV-UHFFFAOYSA-N

Data  1 IC50  3 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 4 hits for monomerid = 313137   

TargetVascular endothelial growth factor receptor 2(Human)
Rigel Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM313137(US10166216, Compound 168 | 1-(6,7-dimethoxyquinazo...)
Affinity DataEC50:  14nMAssay Description:Inhibition of VEGF stimulated VEGFR2 phosphorylation at Y165 residues in HUVEC preincubated for 1 hr followed by VEGF addition measured after 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetTyrosine-protein kinase receptor UFO(Human)
Rigel Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM313137(US10166216, Compound 168 | 1-(6,7-dimethoxyquinazo...)
Affinity DataEC50:  16nMAssay Description:Inhibition of Axl in human HeLa cells assessed as reduction in AKT phosphorylation at Ser 473 residues pre-incubated for 1 hr before preclustered ant...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetTyrosine-protein kinase receptor UFO(Human)
Rigel Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM313137(US10166216, Compound 168 | 1-(6,7-dimethoxyquinazo...)
Affinity DataIC50: 1.00E+3nMAssay Description:The resulting chemiluminescence was read with a Luminomitor within 10 minutes to minimize changes in signal intensity. After reading the chemilumines...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2019
Entry Details
US Patent

TargetInsulin receptor(Human)
Rigel Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM313137(US10166216, Compound 168 | 1-(6,7-dimethoxyquinazo...)
Affinity DataEC50:  1.32E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed