BDBM414765 5-(4-(Azetidin-1-ylmethyl)- 2-fluoro-6-methylphenyl)-3- (1-methyl-1H-pyrazol-4-yl)- 1H-pyrazolo[3,4-c]pyridine::US10435405, Example 182::US10934288, Example 182

SMILES Cc1cc(CN2CCC2)cc(F)c1-c1cc2c(n[nH]c2cn1)-c1cnn(C)c1

InChI Key InChIKey=DWZVSFJBZRFDFR-UHFFFAOYSA-N

Data  3 KI  9 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 = 414765   

TargetMitogen-activated protein kinase kinase kinase kinase 1(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 146nMAssay Description:Inhibition of human HPK1 in human Jurkat cells assessed as reduction in SLP76 phosphorylation incubated for 1 hr by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 302nMAssay Description:Inhibition of human HPK1 in human whole blood assessed as reduction in SLP76 phosphorylation incubated for 1 hr by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetCytochrome P450 1A2(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 1.50E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using 7- ethoxyresorufin as substrate by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetCytochrome P450 2B6(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 1.50E+4nMAssay Description:Inhibition of CYP2B6 in human liver microsomes using bupropion as substrate by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetCytochrome P450 2C8(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 1.50E+4nMAssay Description:Inhibition of CYP2C8 in human liver microsomes using amodiaquine as substrate by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetCytochrome P450 2C9(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 1.50E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetCytochrome P450 2D6(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 1.50E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetCytochrome P450 3A4(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 1.50E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetCytochrome P450 2C19(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataIC50: 1.50E+4nMAssay Description:Inhibition of CYP2C19 in human liver microsomes using S mephenytoin as substrate by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataKi:  4.10nMAssay Description:Binding affinity to recombinant human HPK1 (1 to 346 residues) expressed sf9 cells incubated for 1 hr by LanthaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataKi: <100nMAssay Description:A stock solution of 1 mM test compound was prepared in DMSO. The compound plate was prepared by 3-fold and 11-point serial dilutions. 0.1 μL of ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase kinase kinase kinase 1(Human)
Incyte Research Institute

Curated by ChEMBL
LigandPNGBDBM414765(US10435405, Example 182 | 5-(4-(Azetidin-1-ylmethy...)
Affinity DataKi: <100nMAssay Description:A stock solution of 1 mM test compound was prepared in DMSO. The compound plate was prepared by 3-fold and 11-point serial dilutions. 0.1 μL of ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/12/2021
Entry Details
Go to US Patent