BDBM264212 (2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-yl)amino] pyrimidin-4- yl}-1H-indol-7-yl)-2-(4- methylpiperazin-1- yl)propanamide::US10167276, Example 32::US10654835, Example 32::US11247983, Example 32::US20230416237, Example AZD4205::US9714236, 32

SMILES COc1nn(C)cc1Nc1nccc(n1)-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(C)CC3)cccc12

InChI Key

Data  22 IC50

  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 22 hits for monomerid = 264212   

TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  73nMpH: 7.3Assay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Csir-Indian Institute Of Integrative Medicine

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  73nMAssay Description:Inhibition of JAK 1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >3.00E+4nMpH: 7.3Assay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  73nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Dizal (Jiangsu) Pharmaceutical

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >1.47E+4nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3 [811-1124](Homo sapiens (Human))
Dizal (Jiangsu) Pharmaceutical

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >3.00E+4nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  73nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, PV4774, Carlsbad, Calif.), JAK2 (amino acid...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2 [831-1132](Homo sapiens (Human))
Dizal (Jiangsu) Pharmaceutical

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >1.47E+4nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, PV4774, Carlsbad, Calif.), JAK2 (amino acid...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >3.00E+4nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, PV4774, Carlsbad, Calif.), JAK2 (amino acid...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >1.50E+4nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 pep...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  2.80E+3nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 4B1(Homo sapiens)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of human Cytochrome P450More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Csir-Indian Institute Of Integrative Medicine

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  70nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged JAK1 (866 to 1154 residues) expressed in insect cells using FITC-labeled C6-KKHTDDGYMPMSPGVA-NH...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Csir-Indian Institute Of Integrative Medicine

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  130nMAssay Description:Inhibition of JAK1 in human NCI-H1975 cells assessed as decrease in STAT3 phosphorylation measured after 1 hr by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  73nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2 [831-1132](Homo sapiens (Human))
Dizal (Jiangsu) Pharmaceutical

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >1.47E+4nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >3.00E+4nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Csir-Indian Institute Of Integrative Medicine

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  56nMAssay Description:The inhibitory activity (IC50) of the amide compound for JAK1 and JAK2 under 1 mM ATP was measured by a mobility shift assay method. JAK1 was purchas...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50:  4.02E+3nMAssay Description:The inhibitory activity (IC50) of the amide compound for JAK1 and JAK2 under 1 mM ATP was measured by a mobility shift assay method. JAK1 was purchas...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2 [831-1132](Homo sapiens (Human))
Dizal (Jiangsu) Pharmaceutical

US Patent
LigandPNGBDBM264212((2R)-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-y...)
Affinity DataIC50: >1.47E+4nMpH: 7.3Assay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
In DepthDetails US Patent