BDBM424454 US10508120, Compound I-1183::US10508120, Compound I-909::US10577373, Compound I-1183::US11046698, Compound I-1183::US11414431, Compound I-263

SMILES CNc1cc(Nc2cccn(-c3ccccn3)c2=O)nc2c(cnn12)C(=O)N[C@H]1CC[C@@H]1OC

InChI Key InChIKey=BWINBHTTZLVXGT-UHFFFAOYSA-N

Data  18 IC50  11 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 29 hits for monomerid = 424454   

TargetCytochrome P450 2D6(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of human CYP2D6More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of JAK1/JAK2 in IFNgamma-induced human HEK-dual cells by SEAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of JAK1/JAK2 in CD3+ human HT-29 cells assessed as inhibition of IL22-stimulated phosphorylation of STAT3More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of JAK1/JAK2 in CD3+ human PBMC assessed as inhibition of IL6-stimulated phosphorylation of STAT3More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of JAK1/JAK3 in CD3+ human PBMC assessed as inhibition of IL4-stimulated phosphorylation of STAT6More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of JAK1/JAK3 in human PBMC assessed as inhibition of IL2-stimulated phosphorylation of STAT5More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of Jak2 in human PBMC assessed as inhibition of GM-CSF-stimulated phosphorylation of STAT5More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of TYK2 dependent IFNalpha-stimulated STAT3 phosphorylation in human PBMCMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd:  2.30E+4nMAssay Description:Binding affinity to human JAK2 JH2 domain assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd:  4.98E+3nMAssay Description:Binding affinity to human JAK1 JH2 domain assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2 [5-1181](Mouse)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd:  0.0670nMAssay Description:Binding affinity to mouse TYK2 JH2 domain assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of hERG by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetCytochrome P450 1A2(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of human CYP1A2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetCytochrome P450 2C19(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 1.90E+4nMAssay Description:Inhibition of human CYP2C19More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetCytochrome P450 2C9(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of human CYP2C9More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2 [556-888](Human)
Nimbus Lakshimi

US Patent
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd: <0.200nMAssay Description:Binding constants for compounds of the present invention against the JH2 domain were determined by the following protocol for a KINOMEscan assay (Dis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/29/2020
Entry Details
Go to US Patent

TargetCytochrome P450 3A4(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of human CYP3A4 using testosterone as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetCytochrome P450 3A4(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 8.30E+3nMAssay Description:Inhibition of human CYP3A4 using midazolam as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of PDE4D (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of JAK in human PBMC cells assessed as IL-12-induced phosphorylation of STAT5 levelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of JAK in human PBMC cells assessed as GM-CSF-induced phosphorylation of STAT5 levelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataIC50: 6.70nMAssay Description:Inhibition of TYK2 in human PBMC cells assessed as IL-12 induced phosphorylation of STAT4 levelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Nimbus Therapeutics

Curated by ChEMBL
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd:  0.00400nMAssay Description:Binding affinity to human wild type TYK2 JH2 domain (G556/D888) expressed in mammalian expression systemMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2 [556-888](Human)
Nimbus Lakshimi

US Patent
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd:  0.600nMAssay Description:The binding reaction was assembled by combining 16 μl of DNA-tagged kinase extract, 3.8 μl liganded affinity beads, and 0.18 μl test c...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2022
Entry Details
Go to US Patent

TargetNon-receptor tyrosine-protein kinase TYK2 [556-888](Human)
Nimbus Lakshimi

US Patent
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd: <0.200nMAssay Description:Binding constants for compounds of the present invention against the JH2 domain were determined by the following protocol for a KINOMEscan assay (Dis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2021
Entry Details
Go to US Patent

TargetNon-receptor tyrosine-protein kinase TYK2 [556-888](Human)
Nimbus Lakshimi

US Patent
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd:  0.600nMAssay Description:Binding constants for compounds of the present invention against the JH2 domain were determined by the following protocol for a KINOMEscan assay (Dis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2021
Entry Details
Go to US Patent

TargetNon-receptor tyrosine-protein kinase TYK2 [556-888](Human)
Nimbus Lakshimi

US Patent
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd:  0.600nMAssay Description:Binding constants for compounds of the present invention against the JH2 domain were determined by the following protocol for a KINOMEscan assay (Dis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2020
Entry Details
Go to US Patent

TargetNon-receptor tyrosine-protein kinase TYK2 [556-888](Human)
Nimbus Lakshimi

US Patent
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd: <0.200nMAssay Description:Binding constants for compounds of the present invention against the JH2 domain were determined by the following protocol for a KINOMEscan assay (Dis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2020
Entry Details
Go to US Patent

TargetNon-receptor tyrosine-protein kinase TYK2 [556-888](Human)
Nimbus Lakshimi

US Patent
LigandPNGBDBM424454(US10508120, Compound I-1183 | US10508120, Compound...)
Affinity DataKd:  0.600nMAssay Description:Binding constants for compounds of the present invention against the JH2 domain were determined by the following protocol for a KINOMEscan assay (Dis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/29/2020
Entry Details
Go to US Patent