Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T24823 | Target Info | |||
| Target Name | Lysine-specific histone demethylase 1B (KDM1B) | ||||
| Synonyms |
Lysine-specific histone demethylase 2; LSD2; Flavin-containing amine oxidase domain-containing protein 1; C6orf193; AOF1
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| Target Type | Patented-recorded Target | ||||
| Gene Name | KDM1B | ||||
| Biochemical Class | CH-NH(2) donor oxidoreductase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 16 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Tranylcypromine
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Approved | Compound Info | ||
| Synonyms |
GJZ; Jatrosom; Parnate; Parnitene; Tranilcipromina; Transamine; Tranylcyprominum; Allphar Brand of Tranylcypromine Sulfate; Esparma Brand of Tranylcypromine Sulfate; GlaxoSmithKline Brand of Tranylcypromine Sulfate; Goldshield Brand of Tranylcypromine Sulfate; Link Brand of Tranylcypromine Sulfate; Racemic Tranylcypromine; SmithKline Brand of Tranylcypromine Sulfate; SKF 385; Trans 2 Phenylcyclopropylamine; D-Tranylcypromine; Dl-Tranylcypromine; Jatrosom (TN); L-Tranylcypromine; Parmodalin (TN); Parnate (TN); Parstelin (TN); SKF Trans-385; Sicoton (TN); Sulfate, Tranylcypromine; Tranilcipromina [INN-Spanish]; Transamine (TN); Transapin (TN); Tranylcypromine (INN); Tranylcypromine [INN:BAN]; Tranylcyprominum [INN-Latin]; Tylciprine (TN); Trans-2-Phenylcyclopropylamine; Trans-DL-2-Phenylcyclopropylamine; Trans-(-)-2-Phenylcyclopropanamine; Cyclopropanamine, 2-phenyl-, (1R-trans)-(9CI); (+)-(R)-Tranylcypromine; (+)-Tranylcypromine; (+)-trans-2-Phenylcyclopropylamine; (-)-Tranylcypromine; (1R)-2-phenylcyclopropan-1-amine; (1R,2R)-2-phenylcyclopropan-1-amine; (1R,2S)-2-phenylcyclopropan-1-amine; (1R,2S)-2-phenylcyclopropanamine; (1S)-2-phenylcyclopropan-1-amine; (1S,2R)-2-phenylcyclopropan-1-amine; (1S,2S)-2-phenylcyclopropan-1-amine; (2S)-2-phenylcyclopropan-1-amine; 2-Phenylcyclopropanamine; 2-phenylcyclopropan-1-amine
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
Chembl4299285
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Investigative | Compound Info | ||
| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Chembl4299338
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Investigative | Compound Info | ||
| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[4-[(1S,2R)-2-Aminocyclopropyl]phenyl]-4-(furan-3-yl)benzamide;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780391; BDBM50155763
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| Activity |
IC50 = 51000 nM
|
[3] | |||
| Compound Name |
N-[4-[(1S,2R)-2-Aminocyclopropyl]phenyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3546846; CHEMBL3416427; SCHEMBL12813993; BDBM50078896; BDBM50155579
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| Activity |
IC50 = 58300 nM
|
[3] | |||
| Compound Name |
N-[(2S)-1-(Benzylamino)-1-oxo-6-[(2-phenylcyclopropyl)amino]hexan-2-yl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622371; SCHEMBL15764504; BDBM50121213
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| Activity |
IC50 = 60000 nM
|
[4] | |||
| Compound Name |
N-[4-[(1S,2R)-2-Aminocyclopropyl]phenyl]-4-morpholin-4-ylbenzamide;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781329; SCHEMBL17287366; BDBM50155765
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| Activity |
IC50 = 74700 nM
|
[3] | |||
| Compound Name |
Chembl4162448
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4166129; BDBM50278412; BDBM50278460
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
N-(3-(Methoxymethyl)phenyl)-4-methyl-4H-thieno[3,2-b]pyrrole-5-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4066708; N-[3-(methoxymethyl)phenyl]-4-methyl-4H-thieno[3,2-b]pyrrole-5-carboxamide; SCHEMBL17554399; BDBM50236360; STK942407; ZINC40786272; AKOS005671469; MCULE-5738884822; N-[3-(methoxymethyl)phenyl]-4-methylthieno[3,2-b]pyrrole-5-carboxamide
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Chembl4166776
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Investigative | Compound Info | ||
| Synonyms |
BDBM50278410
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(1S,2R)-2-Phenylcyclopropan-1-amine;(1R,2S)-2-phenylcyclopropan-1-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3989843
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Chembl4174280
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Investigative | Compound Info | ||
| Synonyms |
BDBM50278409
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Iadademstat
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Investigative | Compound Info | ||
| Synonyms |
ORY-1001; ORY-1001 free base; CHEMBL3781751; UNII-54T74394F8; 1431304-21-0 (free base); 54T74394F8; N-[(1R,2S)-2-Phenylcyclopropyl]-1,4-cyclohexanediamine; 4-N-[(1R,2S)-2-phenylcyclopropyl]cyclohexane-1,4-diamine; Iadademstat [INN]; GTPL8390; CHEMBL3906257; SCHEMBL14880401; SCHEMBL14880402; SCHEMBL14880654; BDBM254603; BDBM50155773; ZINC94088493; NCGC00480828-02; NCGC00480828-04; B5882; US9469597, 4; trans-N1-((1R,2S)-2-Phenylcyclopropyl)-1,4-cyclohexanediamine; 1,4-Cyclohexanediamine, N1-((1R,2S)-2-phenylcyclopropyl)-, trans-
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-Methyl-N-[3-[[4-(1-methylpiperidin-4-yl)oxyphenoxy]methyl]phenyl]thieno[3,2-b]pyrrole-5-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4090002; SCHEMBL17554378; BDBM50236365
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Chembl4160042
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Investigative | Compound Info | ||
| Synonyms |
BDBM50278439
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-Methyl-N-[3-[(4-piperidin-4-yloxyphenoxy)methyl]phenyl]thieno[3,2-b]pyrrole-5-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4083038; SCHEMBL17554390; BDBM50236366
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-[(2S)-1-(Benzylamino)-1-oxo-6-[(2-phenylcyclopropyl)amino]hexan-2-yl]-4-phenylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3765529; SCHEMBL15764564; BDBM50140043
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| Activity |
IC50 = 230000 nM
|
[4] | |||
| Compound Name |
N-[(2S)-1-[(4-Chlorophenyl)methylamino]-1-oxo-6-[(2-phenylcyclopropyl)amino]hexan-2-yl]-4-phenylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3764353; SCHEMBL17537314; BDBM50140044
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| Activity |
IC50 = 250000 nM
|
[4] | |||
| Compound Name |
N-[(2S)-1-Oxo-6-[(2-phenylcyclopropyl)amino]-1-[[3-(trifluoromethyl)phenyl]methylamino]hexan-2-yl]-4-phenylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3764836; NCD-41; SCHEMBL15764503; BDBM50140045; J3.514.195B
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| Activity |
IC50 > 540000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Tying up tranylcypromine: Novel selective histone lysine specific demethylase 1 (LSD1) inhibitors. Eur J Med Chem. 2017 Dec 1;141:101-112. | ||||
| REF 2 | Identification of SNAIL1 Peptide-Based Irreversible Lysine-Specific Demethylase 1-Selective Inactivators. J Med Chem. 2016 Feb 25;59(4):1531-44. | ||||
| REF 3 | Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent. J Med Chem. 2016 Feb 25;59(4):1501-17. | ||||
| REF 4 | Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1193-5. | ||||
| REF 5 | Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration. J Med Chem. 2017 Mar 9;60(5):1673-1692. | ||||
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