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Found 12 hits Enz. Inhib. hit(s) with Target = 'Lysine-specific histone demethylase 1A' and Ligand = 'BDBM283256'   
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
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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n/an/a<100n/an/an/an/an/a25



CELGENE QUANTICEL RESEARCH, INC.

US Patent


Assay Description
This assay determines the ability of a test compound to inhibit LSD1 demethylase activity. E. coli expressed full-length human LSD1 (Accession number...


US Patent US10023543 (2018)


BindingDB Entry DOI: 10.7270/Q2GQ70TM
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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Celgene Quanticel Research, Inc.

US Patent


Assay Description
This assay determines the ability of a test compound to inhibit LSD1 demethylase activity. E. coli expressed full-length human LSD1 (Accession number...


US Patent US9573930 (2017)


BindingDB Entry DOI: 10.7270/Q2H70HV3
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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Celgene Quanticel Research, Inc.

US Patent


Assay Description
The enzymatic assay of LSD1 activity is based on Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The inhibitory properties ...


US Patent US9776974 (2017)


BindingDB Entry DOI: 10.7270/Q2BZ686N
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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Celgene Quanticel Research, Inc.

US Patent


Assay Description
The enzymatic assay of LSD1 activity is based on Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The inhibitory properties ...


US Patent US9771329 (2017)


BindingDB Entry DOI: 10.7270/Q2NG4SR7
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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n/an/a<100n/an/an/an/an/an/a



Duquesne University



Assay Description
This assay determines the ability of a test compound to inhibit LSD-1 demethylase activity. E. coli expressed full-length human LSD-1 (Accession numb...


Bioorg Med Chem 17: 7324-36 (2009)


BindingDB Entry DOI: 10.7270/Q2W66P3N
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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n/an/a<100n/an/an/an/an/an/a


TBA

Assay Description
This assay determines the ability of a test compound to inhibit LSD1 demethylase activity. E. coli expressed full-length human LSD1 (Accession number...


Citation and Details

BindingDB Entry DOI: 10.7270/Q2TF01G7
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTICEL RESEARCH, INC.

US Patent


Assay Description
This assay determines the ability of a test compound to inhibit LSD1 demethylase activity. E. coli expressed full-length human LSD1 (Accession number...


US Patent US10207999 (2019)


BindingDB Entry DOI: 10.7270/Q2DJ5HRT
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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n/an/a<100n/an/an/an/an/an/a



Celgene Quanticel Research, Inc.

US Patent


Assay Description
This assay determines the ability of a test compound to inhibit LSD-1 demethylase activity. E. coli expressed full-length human LSD-1 (Accession numb...


US Patent US10543213 (2020)


BindingDB Entry DOI: 10.7270/Q2X63QBC
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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Celgene Quanticel Research, Inc.

US Patent


Assay Description
This assay determines the ability of a test compound to inhibit LSD-1 demethylase activity. E. coli expressed full-length human LSD-1 (Accession numb...


US Patent US10548896 (2020)


BindingDB Entry DOI: 10.7270/Q29889CV
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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CELGENE QUANTICEL RESEARCH, INC.

US Patent


Assay Description
This assay determines the ability of a test compound to inhibit LSD-1 demethylase activity. E. coli expressed full-length human LSD-1 (Accession numb...


US Patent US10849898 (2020)


BindingDB Entry DOI: 10.7270/Q2XS5ZGP
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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CELGENE QUANTICEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of LSD-1 activity is based on Tnne Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The inhibitory properties...


US Patent US10960005 (2021)


BindingDB Entry DOI: 10.7270/Q2CR5XFH
More data for this
Ligand-Target Pair
Lysine-specific histone demethylase 1A


(Homo sapiens (Human))
BDBM283256
PNG
(4-[2-(4-aminopiperidyl)-6- (4-cyanophenyl)-3-methy...)
Show SMILES Cn1c(nc(-c2ccc(cc2)C#N)c(-c2ccc(C(N)=O)c(F)c2)c1=O)N1CCC(N)CC1
Show InChI InChI=1S/C24H23FN6O2/c1-30-23(33)20(16-6-7-18(22(28)32)19(25)12-16)21(15-4-2-14(13-26)3-5-15)29-24(30)31-10-8-17(27)9-11-31/h2-7,12,17H,8-11,27H2,1H3,(H2,28,32)
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CELGENE QUANTICEL RESEARCH, INC.

US Patent


Assay Description
To analyze LSD1 inhibitor efficacy in cells, a CD11b flow cytometry assay was performed. LSD1 inhibition induces CD11b expression in THP-1 (AML) cell...


US Patent US10207999 (2019)


BindingDB Entry DOI: 10.7270/Q2DJ5HRT
More data for this
Ligand-Target Pair