BDBM50527406 CHEMBL4588333::US10981911, Example 45

SMILES Fc1ccc(CNC(=O)Cc2nc3cnc4[nH]ccc4c3n2[C@H]2CC[C@H](CC#N)CC2)cc1

InChI Key InChIKey=MMAFBZVPAFVVFX-UHFFFAOYSA-N

Data  9 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 9 hits for monomerid = 50527406   

TargetTyrosine-protein kinase JAK3(Human)
Janssen Research and Development

Curated by ChEMBL
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 174nMAssay Description:Inhibition of JAK3-JH1/JH2 domain (512 to 1124 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Janssen Research and Development

Curated by ChEMBL
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 0.490nMAssay Description:Inhibition of JAK1-JH1/JH2 domain (574 to 1154 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Janssen Research and Development

Curated by ChEMBL
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 28nMAssay Description:Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulati...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetJAK3/JAK1(Human)
Janssen Research and Development

Curated by ChEMBL
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 2.60nMAssay Description:Inhibition of JAK1/JAK3 in human PBMC assessed as reduction in IL2-induced STAT5 phosphorylation pre-incubated for 30 mins before IL2 stimulation for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Janssen Research and Development

Curated by ChEMBL
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 9.20nMAssay Description:Inhibition of JAK2-JH1/JH2 domain (532 to 1132 residues) (unknown origin) pre-incubated before NH2-KGGEEEEYFELVKK-CO2 substrate addition and measured...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1 [574-1154](Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 0.200nMAssay Description:11-point dosing series were made for each compound by serially diluting 1:3 or 1:4 in DMSO, with point 12 being a DMSO control. From the serial dilut...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2021
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2 [532-1132](Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 6.10nMAssay Description:11-point dosing series were made for each compound by serially diluting 1:3 or 1:4 in DMSO, with point 12 being a DMSO control. From the serial dilut...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2021
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK3 [512-1124](Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 183nMAssay Description:11-point dosing series were made for each compound by serially diluting 1:3 or 1:4 in DMSO, with point 12 being a DMSO control. From the serial dilut...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2021
Entry Details
Go to US Patent

TargetNon-receptor tyrosine-protein kinase TYK2 [580-1182,C936A,C1142A](Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50527406(CHEMBL4588333 | US10981911, Example 45)
Affinity DataIC50: 12.2nMAssay Description:11-point dosing series were made for each compound by serially diluting 1:3 or 1:4 in DMSO, with point 12 being a DMSO control. From the serial dilut...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2021
Entry Details
Go to US Patent