BDBM412734 N-(3-fluoropyridin-4-yl)-2-(6-methylpyridin-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine::US10399987, Example 1

SMILES Cc1cccc(n1)-c1nc(Nc2ccncc2F)c2cc[nH]c2n1

InChI Key InChIKey=GAWGUDTUQRRPQK-UHFFFAOYSA-N

Data  1 KI  5 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 6 hits for monomerid = 412734   

TargetTGF-beta receptor type-1(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM412734(US10399987, Example 1 | N-(3-fluoropyridin-4-yl)-2...)
Affinity DataIC50: 5.10nMAssay Description:Inhibition of TGFbetaR1 in human primary T-cells assessed as TGFbeta-stimulated PSMAD phosphorylation preincubated for 1 hr followed by TGFbeta addit...More data for this Ligand-Target Pair
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In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetTGF-beta receptor type-1(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM412734(US10399987, Example 1 | N-(3-fluoropyridin-4-yl)-2...)
Affinity DataIC50: 7nMAssay Description:Inhibition of human His-tagged TGFbetaR1 T204D mutant expressed in Sf9 insect cells after 1 hr by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetTGF-beta receptor type-2(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM412734(US10399987, Example 1 | N-(3-fluoropyridin-4-yl)-2...)
Affinity DataIC50: 310nMAssay Description:Inhibition of wild type His-tagged TGFbetaR2 (unknown origin) after 1 hr by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetTGF-beta receptor type-1 [4-503,T204D](Human)
Bristol-Myer Squibb

US Patent
LigandPNGBDBM412734(US10399987, Example 1 | N-(3-fluoropyridin-4-yl)-2...)
Affinity DataIC50: 0.700nMAssay Description:Assays are conducted in 1536-well plates and 2 mL reactions are prepared from addition of HIS-TGFβR1 T204D or HIS-TGFβR2 WT, anti-HIS detec...More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
7/27/2020
Entry Details
Go to US Patent

TargetTGF-beta receptor type-2(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM412734(US10399987, Example 1 | N-(3-fluoropyridin-4-yl)-2...)
Affinity DataIC50: 500nMAssay Description:Assays are conducted in 1536-well plates and 2 mL reactions are prepared from addition of HIS-TGFβR1 T204D or HIS-TGFβR2 WT, anti-HIS detec...More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
7/27/2020
Entry Details
Go to US Patent

TargetTGF-beta receptor type-1(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM412734(US10399987, Example 1 | N-(3-fluoropyridin-4-yl)-2...)
Affinity DataKi:  0.140nMAssay Description:Inhibition of human His-tagged TGFbetaR1 T204D mutant expressed in Sf9 insect cells after 1 hr by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed