Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T99727 | Target Info | |||
| Target Name | Hyperpolarization cyclic nucleotide-gated channel (HCN) | ||||
| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 19 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
MEL57A
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1253475; MEL57A; GTPL6260; SCHEMBL16410080; BDBM50326990; 3-[(Z)-4-[[(Z)-4-(7, 8-dimethoxy-2-oxo-1H-3-benzazepin-3-yl)but-2-enyl]-[(2R)-2-(3, 4-dimethoxyphenyl)propyl]amino]but-2-enyl]-7, 8-dimethoxy-1H-3-benzazepin-2-one
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
EC50 = 103780 nM
|
[1] | ||
| Compound Name |
2-Methoxy-N-[(2-piperidin-1-yl-1,3-dihydroinden-2-yl)methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823675; BDBM50419061
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 = 50118.72 nM
|
[2] | ||
| Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 199526.23 nM
|
[2] | |||
| Compound Name |
2-Methoxy-N-[(1-morpholin-4-ylcyclohexyl)methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1332972; HMS1853M19; BDBM50419072; STL202395; ZINC19902148; AKOS002244663; MCULE-3926575372; NCGC00118793-01; D335-0521; 2-methoxy-N-{[1-(morpholin-4-yl)cyclohexyl]methyl}benzamide
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 = 50118.72 nM
|
[2] | ||
| Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 ~ 199526.23 nM
|
[2] | |||
| Compound Name |
3-Methoxy-N-[[2-(4-methylpiperazin-1-yl)-1,3-dihydroinden-2-yl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823669; BDBM50419057
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 = 63095.73 nM
|
[2] | ||
| Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 199526.23 nM
|
[2] | |||
| Compound Name |
2-Methyl-N-[[1-(4-methylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823678; BDBM50419063
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 = 63095.73 nM
|
[2] | ||
| Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 199526.23 nM
|
[2] | |||
| Compound Name |
3-[(Z)-4-[[(Z)-4-(7,8-Dimethoxy-2-oxo-1H-3-benzazepin-3-yl)but-2-enyl]-[2-(3,4-dimethoxyphenyl)ethyl]amino]but-2-enyl]-7,8-dimethoxy-1H-3-benzazepin-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1253477; BDBM50326985
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
EC50 = 70670 nM
|
[1] | ||
| Compound Name |
2-Ethyl-N-[[1-(4-propan-2-ylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823877; BDBM50419082
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 = 79432.82 nM
|
[2] | ||
| Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 ~ 199526.23 nM
|
[2] | |||
| Compound Name |
2-Ethoxy-N-[[1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823884; BDBM50419073
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 = 100000 nM
|
[2] | ||
| Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 ~ 199526.23 nM
|
[2] | |||
| Compound Name |
4-Methoxy-N-[[2-(4-methylpiperazin-1-yl)-1,3-dihydroinden-2-yl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823670; BDBM50419058
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 = 100000 nM
|
[2] | ||
| Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 199526.23 nM
|
[2] | |||
| Compound Name |
6-[({1-[2-(7-Methoxy-2-oxoquinoxalin-1(2H)-yl)ethyl]piperidin-4-yl}amino)methyl]-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2165063; SCHEMBL708423; BDBM50395399
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
6H-Pyrimido[5,4-b][1,4]oxazin-7(8H)-one, 2-[[[trans-4-[(1R)-1-amino-2-(7-fluoro-2-oxo-1(2H)-quinoxalinyl)ethyl]cyclohexyl]amino]methyl]-
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3355573; SCHEMBL1375934; SCHEMBL1375938; BDBM50023589; SB19220
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 100000 nM
|
[3] | ||
| Compound Name |
Auglurant
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|
Investigative | Compound Info | ||
| Synonyms |
VU0424238; N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide; CHEMBL2386850; UNII-GRN8X62ZW2; GRN8X62ZW2; SCHEMBL12499337; VU238; EX-A2936; BDBM50257064; MFCD28386341; VU 238; 2-PyridinecarboxaMide, N-(5-fluoro-2-pyridinyl)-6-Methyl-4-(5-pyriMidinyloxy)-; HY-16617; CS-0009173; VU 0424238; YU-0424238; J3.655.475D; 2-PyridinecarboxaMide,N-(5-fluoro-2-pyridinyl)-6-Methyl-4-(5-pyriMidinyloxy)-; N-(5-Fluoro-2-pyridinyl)-6-methyl-4-(5-pyrimidinyloxy)-2-pyridinecarboxamide; N-(5-fluoropyridin-2-yl)-6-methyl-4-pyrimidin-5-yloxypyridine-2-carboxamide
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 100000 nM
|
[4] | ||
| Hyperpolarization cyclic nucleotide-gated channel 2 |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
3-[(Z)-4-[[(Z)-4-(7,8-Dimethoxy-2-oxo-1H-3-benzazepin-3-yl)but-2-enyl]-[(2S)-2-(3,4-dimethoxyphenyl)propyl]amino]but-2-enyl]-7,8-dimethoxy-1H-3-benzazepin-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1253476; BDBM50326986
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
EC50 = 135730 nM
|
[1] | ||
| Compound Name |
2-Chloro-N-[[2-(4-methylpiperazin-1-yl)-1,3-dihydroinden-2-yl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823671; BDBM50419086
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|
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| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 = 158489.32 nM
|
[2] | ||
| Compound Name |
2-Fluoro-N-[[2-(4-methylpiperazin-1-yl)-1,3-dihydroinden-2-yl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823673; BDBM50419079
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|
||||
| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 199526.23 nM
|
[2] | ||
| Compound Name |
2-Chloro-N-[[1-(4-methylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823679; BDBM50419081; MCULE-4962371646
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|
||||
| Activity | Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 ~ 199526.23 nM
|
[2] | ||
| Compound Name |
2-Hydroxy-N-[[2-(4-methylpiperazin-1-yl)-1,3-dihydroinden-2-yl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823672; BDBM50419059
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|
||||
| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 199526.23 nM
|
[2] | ||
| Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 ~ 199526.23 nM
|
[2] | |||
| Compound Name |
N-[[2-(4-Methylpiperazin-1-yl)-1,3-dihydroinden-2-yl]methyl]-2-(trifluoromethoxy)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823668; BDBM50419056
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|
||||
| Activity | Hyperpolarization cyclic nucleotide-gated channel 4 |
IC50 ~ 199526.23 nM
|
[2] | ||
| Compound Name |
2-Methoxy-N-[2-(4-methylpiperazin-1-yl)ethyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823890; SCHEMBL15825898; BDBM50419077; ZINC22830029; AKOS004075417
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|
||||
| Activity | Hyperpolarization cyclic nucleotide-gated channel 1 |
IC50 ~ 199526.23 nM
|
[2] | ||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers. J Med Chem. 2010 Sep 23;53(18):6773-7. | ||||
| REF 2 | Discovery of a novel series of selective HCN1 blockers. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5197-201. | ||||
| REF 3 | Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa. Bioorg Med Chem. 2014 Oct 1;22(19):5392-409. | ||||
| REF 4 | Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem. 2017 Jun 22;60(12):5072-5085. | ||||
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