Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T73482 | Target Info | |||
| Target Name | Orexin receptor type 1 (HCRTR1) | ||||
| Synonyms |
Ox1r; Ox1-R; Ox-1-R; Orexin-1 receptor; Hypocretin receptor type 1; HFGAN72 receptor; 7-transmembrane G-protein coupledneuropeptide receptor
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| Target Type | Clinical trial Target | ||||
| Gene Name | HCRTR1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 2 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
5-[3,5-Bis(trifluoromethyl)phenyl]-N-[(3,4-dimethoxyphenyl)methyl]-2-pyridin-3-ylpyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3099896; BDBM50444608
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| Activity |
Ki = 65000 nM
|
[1] | |||
| Compound Name |
(4S)-4-Amino-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL262404; BDBM50219318
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| Activity |
Ki = 66069.34 nM
|
[2] | |||
| Non Binders of This Target (in total, 12 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
G-N-H-A-A-G-I-L-T-L
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL430345; BDBM50140015
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
S-G-N-H-A-A-G-I-L-T-M
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL214619; BDBM50139980
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
N-H-A-A-G-I-L-T-L
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL280472; BDBM50139967
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
R-S-G-P-P-G-L-Q-G-R-L-Q-R-L-L-Q
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL409188; BDBM50139991
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
(3S)-4-[[(2R)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-Amino-1-[[(2S)-6-amino-1-[[(2S,3R)-1-[[(2R)-1-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-[[(2S)-1-[(2S)-4-methyl-2-[[(2S)-1-[(2S)-5-oxopyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-4-oxobutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2370375
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
L-L-H-G-A-G-N-H-A-A-G-I-L-T-L
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL439167; BDBM50139987
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
A-G-N-H-A-A-G-I-L-T-L
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL384047; BDBM50140007
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
H-A-A-G-I-L-T-L
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL429205; BDBM50140000
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| Activity |
EC50 > 1000000 nM
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[3] | |||
| Compound Name |
R-S-G-P-P-G-L-Q-G-R-L-Q-R
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL412250; BDBM50140027
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
(3S)-4-[[(2R)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-Amino-1-[[(2S)-6-amino-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-[[(2S)-1-[(2S)-4-methyl-2-[[(2S)-1-[(2S)-5-oxopyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-4-oxobutanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2370351
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
R-S-G-P-P-G-L-Q-G-R
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL386724; BDBM50139963
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Compound Name |
L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL384249; BDBM50139978
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| Activity |
EC50 > 1000000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs). Bioorg Med Chem Lett. 2013 Dec 15;23(24):6620-4. | ||||
| REF 2 | Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor. Bioorg Med Chem Lett. 2001 Mar 12;11(5):737-40. | ||||
| REF 3 | Structure-activity studies of orexin a and orexin B at the human orexin 1 and orexin 2 receptors led to orexin 2 receptor selective and orexin 1 receptor preferring ligands. J Med Chem. 2004 Feb 26;47(5):1153-60. | ||||
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