BDBM282825 6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H- imidazol-5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile::US10287295, Example 32'::US11352360, Example 32'::US9884868, Example 32'

SMILES OCCn1cnc(c1-c1ccc2ncc(C#N)n2n1)-c1ccc(F)c(Cl)c1

InChI Key InChIKey=VZZBCNXVZFAIQX-UHFFFAOYSA-N

Data  2 KI  18 IC50  1 EC50

PDB links: 1 PDB ID matches this monomer.

  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 10 hits for monomerid = 282825   

TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataKi:  0.800nMAssay Description:Inhibition of TGFBR1 in human whole blood assessed as apparent inhibition constant by measuring reduction in TGFbeta-induced SMAD phosphorylationMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Mus musculus)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataKi:  1.40nMAssay Description:Inhibition of TGFBR1 in mouse whole blood assessed as apparent inhibition constant by measuring reduction in TGFbeta-induced SMAD phosphorylationMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataIC50:  350nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mink Mv1Lu cells assessed as reduction in SMAD nuclear translocation preincubated for 1 hr followed by ...More data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataIC50:  190nMAssay Description:Inhibition of TGFBR1 in TGFbeta-stimulated human NHLF cells assessed as reduction in SMAD2 nuclear translocationMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataIC50:  150nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated human T cells assessed as reduction in SMAD3 phosphorylation preincubated for 1 hr followed by TGFbeta-...More data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Mus musculus)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataIC50:  50nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mouse NIH3T3 cells assessed as reduction in SMAD3 phosphorylationMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataIC50:  230nMAssay Description:Inhibition of TGFbetaR1 in anti-CD3/anti-CD28/IL-2/TGFbeta -stimulated human Treg cells assessed as downregulation of FOXP3 expression incubated for ...More data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataIC50:  1.80nMAssay Description:Assays for the compounds reported below were conducted in 1536-well plates and 2 mL reactions are prepared from addition of HIS-TGF-βR1 T204D or...More data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataIC50:  1.80nMpH: 7.4 T: 2°CAssay Description:Assays for the compounds reported below were conducted in 1536-well plates and 2 mL reactions are prepared from addition of HIS-TGF-βR1 T204D or...More data for this Ligand-Target Pair