BDBM50186460 CHEMBL209148::N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-2-methylphenylthio)thiazol-2-yl)-4-((3,3-dimethylbutan-2-ylamino)methyl)benzamide

SMILES Cc1cc(c(cc1Sc2cnc(s2)NC(=O)c3ccc(cc3)CN[C@@H](C)C(C)(C)C)C(=O)N4CCN(CC4)C(=O)C)OC

InChI Key InChIKey=ZHXNIYGJAOPMSO-UHFFFAOYSA-N

Data  1 KI  19 IC50  1 EC50

  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 45 hits for monomerid = 50186460   

TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 10nMAssay Description:Inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2023
Entry Details Article
PubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataKi:  16nMAssay Description:Inhibition of ITKMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/1/2013
Entry Details Article
PubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 19nMAssay Description:Inhibition of human Itk using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 19nMAssay Description:Inhibition of ItkMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 19nMAssay Description:Inhibition of ITK (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetTyrosine-protein kinase ITK/TSK(Mus musculus)TBA
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 72nMAssay Description:Inhibition of Itk in mouse EL4 cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by ELISA an...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetInterleukin-2(Human)
Peking University

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataEC50:  238nMAssay Description:Inhibition of IL-2 in human Jurkat T cells pretreated with compound for 16 hrs followed by anti-CD3 stimulation by ELISA analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 250nMAssay Description:Inhibition of Itk in human Jurkat T cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by ELI...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTyrosine-protein kinase ITK/TSK(Mus musculus)TBA
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 380nMAssay Description:Inhibition of Itk in mouse Splenocyte cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 390nMAssay Description:Inhibition of Itk in human PBMC cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by ELISA a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetInsulin receptor(Human)TBA
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of IR (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetInsulin receptor(Human)TBA
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of Insulin receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase Fyn(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of FynMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase Fyn(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of Fyn (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.31E+3nMAssay Description:Inhibition of Itk in human Jurkat T cells assessed as inhibition of Ca2+ mobilization incubated for 30 mins in presence of anti-CD3 antibody G19-4 by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 2.40E+3nMAssay Description:Inhibition of Lck (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 2.40E+3nMAssay Description:Inhibition of LCKMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 4.10E+3nMAssay Description:Inhibition of BtkMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 4.10E+3nMAssay Description:Inhibition of Btk (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTyrosine-protein kinase TXK(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.10E+4nMAssay Description:Inhibition of TxkMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase TXK(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.10E+4nMAssay Description:Inhibition of Txk (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTyrosine-protein kinase Tec(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.70E+4nMAssay Description:Inhibition of TecMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase Tec(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 1.70E+4nMAssay Description:Inhibition of Tec (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetO94806/P05129/P05771/P17252/P24723/P41743/Q02156/Q04759/Q05513/Q05655/Q15139(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 2.40E+4nMAssay Description:Inhibition of PKCMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 2.40E+4nMAssay Description:Inhibition of PKC (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of Itk in LPS induced human PBMC cells assessed as inhibition of TNF alpha productionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 2.90E+4nMAssay Description:Inhibition of Cdk2 (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 2.90E+4nMAssay Description:Inhibition of Cdk2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGlycogen synthase kinase-3 beta(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 3.60E+4nMAssay Description:Inhibition of GSK3-betaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGlycogen synthase kinase-3 beta(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 3.60E+4nMAssay Description:Inhibition of GSK-3beta (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation c...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of EGFR (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of Akt1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of ERK-1 (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation count...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of EGFRMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase ZAP-70(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of ZAP70More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of ERK1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of PKA (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of IKKbeta (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation cou...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of Bmx (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of Akt1 (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha/beta/gamma(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of PKAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of Syk (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of SykMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTyrosine-protein kinase ZAP-70(Human)
Bristol-Myers Squibb Pharmaceutical Research Institute

Curated by ChEMBL
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of ZAP-70 (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50186460(N-(5-(5-(1-acetylpiperazine-4-carbonyl)-4-methoxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of IKK-betaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed