BDBM347313 2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(4-(3-hydroxy-2,2-dimethylpropyl)-3-(trifluoromethyl)phenyl)acetamide::US9789100, Example 3

SMILES CCOc1cc(=O)[nH]cc1-c1ccc(CC(=O)Nc2ccc(CC(C)(C)CO)c(c2)C(F)(F)F)c(F)c1

InChI Key InChIKey=PCNMRGUJZFWHPU-UHFFFAOYSA-N

Data  6 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 347313   

LigandPNGBDBM347313(2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fl...)
Affinity DataIC50: 100nMAssay Description:Human RET kinase cytoplasmic domain (amino acids 658-1114 of accession number NP_000314.1) was expressed as an N-terminal GST-fusion protein using a ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/9/2019
Entry Details
Go to US Patent

LigandPNGBDBM347313(2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fl...)
Affinity DataIC50: 100nMAssay Description:Human RET kinase cytoplasmic domain (amino acids 658-1114 of accession number NP_000314.1) was expressed as an N-terminal GST-fusion protein using a ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/9/2019
Entry Details
Go to US Patent

LigandPNGBDBM347313(2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fl...)
Affinity DataIC50: 100nMAssay Description:Human RET kinase cytoplasmic domain (amino acids 658-1114 of accession number NP_000314.1) was expressed as an N-terminal GST-fusion protein using a ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/9/2019
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM347313(2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fl...)
Affinity DataIC50: 9.40nMAssay Description:Inhibition of RET phosphorylation in human TT cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetVascular endothelial growth factor receptor 2(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM347313(2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fl...)
Affinity DataIC50: 12nMAssay Description:Inhibition of human KDR using cisbio TK biotin-peptide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM347313(2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fl...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human RET using cisbio TK biotin-peptide as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by HT...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed