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PubMed code 17114291

Compile data set for download or QSAR
Found 10 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Methionine Aminopeptidase Type 1 (MetAP1)


(Homo sapiens (human))
BDBM17847
PNG
(CHEMBL327579 | pyridine-2-carboxylic acid inhibito...)
Show SMILES CC(C)(C)OC(=O)Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C14H16N4O3S/c1-14(2,3)21-13(20)17-9-5-4-6-15-10(9)11(19)18-12-16-7-8-22-12/h4-8H,1-3H3,(H,17,20)(H,16,18,19)
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Article
PubMed
n/an/a 1.50E+3n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Methionine Aminopeptidase Type 1 (MetAP1)


(Homo sapiens (human))
BDBM17849
PNG
(3-(2,2-dimethylpropanamido)-N-(1,3-thiazol-2-yl)py...)
Show SMILES CC(C)(C)C(=O)Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C14H16N4O2S/c1-14(2,3)12(20)17-9-5-4-6-15-10(9)11(19)18-13-16-7-8-21-13/h4-8H,1-3H3,(H,17,20)(H,16,18,19)
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Article
PubMed
n/an/a 2.90E+3n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Methionine Aminopeptidase Type 1 (MetAP1)


(Homo sapiens (human))
BDBM17850
PNG
(3-(3-phenylpropanamido)-N-(1,3-thiazol-2-yl)pyridi...)
Show SMILES O=C(CCc1ccccc1)Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C18H16N4O2S/c23-15(9-8-13-5-2-1-3-6-13)21-14-7-4-10-19-16(14)17(24)22-18-20-11-12-25-18/h1-7,10-12H,8-9H2,(H,21,23)(H,20,22,24)
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PubMed
n/an/a 3.50E+3n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
Methionine Aminopeptidase Type 1 (MetAP1)


(Homo sapiens (human))
BDBM17851
PNG
(3-[(E)-(2-methylpropylidene)amino]-N-(1,3-thiazol-...)
Show SMILES CC(C)C=Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C13H14N4OS/c1-9(2)8-16-10-4-3-5-14-11(10)12(18)17-13-15-6-7-19-13/h3-9H,1-2H3,(H,15,17,18)
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PubMed
n/an/a 6.40E+3n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (human))
BDBM17847
PNG
(CHEMBL327579 | pyridine-2-carboxylic acid inhibito...)
Show SMILES CC(C)(C)OC(=O)Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C14H16N4O3S/c1-14(2,3)21-13(20)17-9-5-4-6-15-10(9)11(19)18-12-16-7-8-22-12/h4-8H,1-3H3,(H,17,20)(H,16,18,19)
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Article
PubMed
n/an/a>3.00E+5n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (human))
BDBM17852
PNG
(3-octanamido-N-(1,3-thiazol-2-yl)pyridine-2-carbox...)
Show SMILES CCCCCCCC(=O)Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C17H22N4O2S/c1-2-3-4-5-6-9-14(22)20-13-8-7-10-18-15(13)16(23)21-17-19-11-12-24-17/h7-8,10-12H,2-6,9H2,1H3,(H,20,22)(H,19,21,23)
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PubMed
n/an/a>5.00E+5n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (human))
BDBM17849
PNG
(3-(2,2-dimethylpropanamido)-N-(1,3-thiazol-2-yl)py...)
Show SMILES CC(C)(C)C(=O)Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C14H16N4O2S/c1-14(2,3)12(20)17-9-5-4-6-15-10(9)11(19)18-13-16-7-8-21-13/h4-8H,1-3H3,(H,17,20)(H,16,18,19)
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PubMed
n/an/a>5.00E+5n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
Methionine Aminopeptidase Type 1 (MetAP1)


(Homo sapiens (human))
BDBM17852
PNG
(3-octanamido-N-(1,3-thiazol-2-yl)pyridine-2-carbox...)
Show SMILES CCCCCCCC(=O)Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C17H22N4O2S/c1-2-3-4-5-6-9-14(22)20-13-8-7-10-18-15(13)16(23)21-17-19-11-12-24-17/h7-8,10-12H,2-6,9H2,1H3,(H,20,22)(H,19,21,23)
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PubMed
n/an/a>5.00E+5n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (human))
BDBM17850
PNG
(3-(3-phenylpropanamido)-N-(1,3-thiazol-2-yl)pyridi...)
Show SMILES O=C(CCc1ccccc1)Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C18H16N4O2S/c23-15(9-8-13-5-2-1-3-6-13)21-14-7-4-10-19-16(14)17(24)22-18-20-11-12-25-18/h1-7,10-12H,8-9H2,(H,21,23)(H,20,22,24)
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PubMed
n/an/a>5.00E+5n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (human))
BDBM17851
PNG
(3-[(E)-(2-methylpropylidene)amino]-N-(1,3-thiazol-...)
Show SMILES CC(C)C=Nc1cccnc1C(=O)Nc1nccs1
Show InChI InChI=1S/C13H14N4OS/c1-9(2)8-16-10-4-3-5-14-11(10)12(18)17-13-15-6-7-19-13/h3-9H,1-2H3,(H,15,17,18)
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PubMed
n/an/a>1.00E+6n/an/an/an/a7.522



Johns Hopkins University



Assay Description
The MetAP reaction with Co2+ as a cofactor is coupled to a prolyl aminopeptidase (ProAP) using Met-Pro-p-nitroanilide as substrate. MetAP-catalyzed c...


Proc Natl Acad Sci U S A 103: 18148-53 (2006)


Article DOI: 10.1073/pnas.0608389103
BindingDB Entry DOI: 10.7270/Q2RB72VK
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%