Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T62460 | Target Info | |||
| Target Name | Janus kinase 1 (JAK-1) | ||||
| Synonyms |
Tyrosine-protein kinase JAK1; JAK1B; JAK1A
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| Target Type | Successful Target | ||||
| Gene Name | JAK1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 33 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Oxindole 94
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Investigative | Compound Info | ||
| Synonyms |
SB 202190; 152121-30-7; SB202190; SB-202190; FHPI; SB202190 (FHPI); UNII-PVX798P8GI; 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazole; CHEBI:79090; 4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole; PVX798P8GI; SB 202190, Immobilized; C20H14FN3O; Phenol, 4-[4-(4-fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-; 4-[4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl]phenol; 4-[5-(4-fluorophenyl)-4-(pyridin-4-yl)-1H-imidazol-2-yl]phenol
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-Chloro-N-(3-quinoxalin-2-ylphenyl)butanamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1463405; CHEMBL3645538; BDBM107121; US8592415, 5; 4-chloro-N-[3-(quinoxalin-2-yl)phenyl]butanamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
2-(Dimethylamino)-N-(3-quinoxalin-2-ylphenyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1463296; CHEMBL3645535; BDBM107118; US8592415, 2; N2,N2-dimethyl-N1-(3-quinoxalin-2-ylphenyl)glycinamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
3-Chloro-N-(3-quinoxalin-2-ylphenyl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1463291; CHEMBL3645548; BDBM107134; US8592415, 19; 3-chloro-N-[3-(quinoxalin-2-yl)phenyl]propanamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[3-(2-Quinoxalinyl)phenyl]methanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
N-[3-(quinoxalin-2-yl)phenyl]methanesulfonamide; N-(3-quinoxalin-2-ylphenyl)methanesulfonamide; MLS001165982; SCHEMBL1463425; CHEMBL1553519; KS-00001ZVU; BDBM107130; HMS2855A24; ZINC1399325; MFCD03617716; AKOS005099938; MCULE-3207290219; SMR000550249; US8592415, 15; 7T-0022
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-(3-Quinoxalin-2-ylphenyl)-2-(1,2,4-triazol-1-yl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1464125; CHEMBL3645539; BDBM107123; US8592415, 7; N-[3-(quinoxalin-2-yl)phenyl]-2-(1H-1,2,4-triazol-1-yl)acetamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[3-(2-Quinoxalinyl)phenyl]-2-furamide
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Investigative | Compound Info | ||
| Synonyms |
N-[3-(quinoxalin-2-yl)phenyl]furan-2-carboxamide; MLS000100130; regid4258715; N-(3-quinoxalin-2-ylphenyl)furan-2-carboxamide; SCHEMBL1462285; CHEMBL1572928; KS-00003DPA; BDBM107127; HMS2167I24; HMS3320K16; ZINC1399317; AKOS005099816; MCULE-1007454916; SMR000081936; US8592415, 12; 7T-0013
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
2-(4-Methylpiperazin-1-yl)-N-(3-quinoxalin-2-ylphenyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1464066; CHEMBL3645546; BDBM107132; US8592415, 17; 2-(4-methylpiperazin-1-yl)-N-[3-(quinoxalin-2-yl)phenyl]acetamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[4-(2-Quinoxalinyl)phenyl]cyclopropanecarboxamide
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Investigative | Compound Info | ||
| Synonyms |
N-[3-(quinoxalin-2-yl)phenyl]cyclopropanecarboxamide; N-(3-quinoxalin-2-ylphenyl)cyclopropanecarboxamide; SCHEMBL1463399; CHEMBL3645544; KS-00003DPB; BDBM107129; MFCD12910763; ZINC43796862; AKOS005099847; MCULE-7559936835; US8592415, 14; 7T-0015
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-Methyl-N'-[3-(2-quinoxalinyl)phenyl]thiourea
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Investigative | Compound Info | ||
| Synonyms |
1-methyl-3-(3-quinoxalin-2-ylphenyl)thiourea; MLS001165984; SMR000550248; 3-methyl-1-[3-(quinoxalin-2-yl)phenyl]thiourea; SCHEMBL1462401; CHEMBL1537091; REGID_for_CID_409246; BDBM67663; cid_1485416; KS-00001ZVR; REGID_for_CID_1485416; HMS2852P03; ZINC1399314; AKOS005099784; MCULE-4454820641; 1-methyl-3-[3-(2-quinoxalinyl)phenyl]thiourea; 1-methyl-3-[3-(quinoxalin-2-yl)phenyl]thiourea; 7T-0009
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[3-(2-Quinoxalinyl)phenyl]-2-thiophenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
n-[3-(quinoxalin-2-yl)phenyl]thiophene-2-sulfonamide; N-(3-quinoxalin-2-ylphenyl)thiophene-2-sulfonamide; SCHEMBL1462283; CHEMBL3645543; KS-00001ZVS; BDBM107128; ZINC1399318; AKOS005099846; MCULE-1175160761; US8592415, 13; 7T-0014
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
2-Morpholino-N-(3-(quinoxalin-2-yl)phenyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1463453; CHEMBL3645549; BDBM107135; US8592415, 20; 2-morpholin-4-yl-N-(3-quinoxalin-2-ylphenyl)acetamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Chembl4289149
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Investigative | Compound Info | ||
| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
2-Chloro-N-(3-quinoxalin-2-ylphenyl)propanamide
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1463360; CHEMBL3645550; BDBM107136; US8592415, 21; 2-chloro-N-(3-(quinoxalin-2-yl)phenyl)propanamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-(3-Quinoxalin-2-ylphenyl)propanamide
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|
Investigative | Compound Info | ||
| Synonyms |
MLS000537362; SCHEMBL1462316; CHEMBL1446198; BDBM107122; HMS1599D07; HMS2400O23; ZINC555918; AKOS003653098; MCULE-9745117709; N-[3-(2-quinoxalinyl)phenyl]propanamide; SMR000143800; N-[3-(quinoxalin-2-yl)phenyl]propionamide; ST45104659; US8592415, 6; SR-01000287574; SR-01000287574-1
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-(4-Methoxyphenyl)-N'-[3-(2-quinoxalinyl)phenyl]urea
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Investigative | Compound Info | ||
| Synonyms |
1-(4-methoxyphenyl)-3-[3-(quinoxalin-2-yl)phenyl]urea; 1-(4-methoxyphenyl)-3-(3-quinoxalin-2-ylphenyl)urea; SCHEMBL1463272; CHEMBL3645542; KS-00001ZVQ; BDBM107126; ZINC1399313; AKOS005099783; MCULE-4650809137; US8592415, 10; 7T-0007
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Disodium;2-[4-[4-(4-fluorophenyl)-1-methyl-5-pyridin-4-ylimidazol-2-yl]triazol-1-yl]ethyl-dioxido-oxo-lambda5-phosphane
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3120985
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Sodium;2-[4-[2-(4-fluorophenyl)-3-(2-methylsulfanylpyrimidin-4-yl)imidazo[1,2-a]pyrimidin-7-yl]triazol-1-yl]acetate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3314273
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[5-(4-Fluorophenyl)-3-methyl-2-(2H-triazol-4-yl)imidazol-4-yl]pyridine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3120960; BDBM50045572
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-(4-Fluorophenyl)-3-(2-methylsulfanylpyrimidin-4-yl)imidazo[1,2-a]pyrimidin-7-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3314271; SCHEMBL6217129; BDBM50045555
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2R,3R,4R,5S,6R)-3-[4-[4-(4-Fluorophenyl)-1-methyl-5-pyridin-4-ylimidazol-2-yl]triazol-1-yl]-6-(hydroxymethyl)oxane-2,4,5-triol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3314270; BDBM50045576
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[4-[4-(4-Fluorophenyl)-1-methyl-5-pyridin-4-ylimidazol-2-yl]triazol-1-yl]ethanol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3120963; BDBM50045575
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Disodium;2-[4-[2-(4-fluorophenyl)-3-(2-methylsulfanylpyrimidin-4-yl)imidazo[1,2-a]pyrimidin-7-yl]triazol-1-yl]ethyl-dioxido-oxo-lambda5-phosphane
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3314275
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[4-(4-Fluorophenyl)-5-(2-methylsulfanylpyrimidin-4-yl)-1H-imidazol-2-yl]phenol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3314285; BDBM50045570
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
7-Ethynyl-2-(4-fluorophenyl)-3-(2-methylsulfanylpyrimidin-4-yl)imidazo[1,2-a]pyrimidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3314272; BDBM50045556
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[2-(4-Ethynylphenyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-methylsulfanylpyrimidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3314286; BDBM50045571
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-(4-Fluorophenyl)-3-[2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl]imidazo[1,2-a]pyrimidin-7-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3120970; SCHEMBL13823117; BDBM50045580
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[5-(4-Fluorophenyl)-2-[1-[(3S,4S)-3-fluoropiperidin-4-yl]triazol-4-yl]-3-methylimidazol-4-yl]pyridine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3120986
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-[4-[4-(4-Fluorophenyl)-1-methyl-5-pyridin-4-ylimidazol-2-yl]triazol-1-yl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3120983; BDBM50045574
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[2-[1-(2-Diethoxyphosphorylethyl)triazol-4-yl]-5-(4-fluorophenyl)-3-methylimidazol-4-yl]pyridine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3120969; BDBM50045578
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
7-[1-(2-Diethoxyphosphorylethyl)triazol-4-yl]-2-(4-fluorophenyl)-3-(2-methylsulfanylpyrimidin-4-yl)imidazo[1,2-a]pyrimidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3314274; BDBM50045558
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4276946
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Investigative | Compound Info | ||
| Synonyms |
GTPL9965; compound 3a [Pipionne et al, 2018]; 1-[5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl]ethan-1-one
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
4-[4-[4-(4-Fluorophenyl)-1-methyl-5-pyridin-4-ylimidazol-2-yl]triazol-1-yl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3120995; BDBM50045573
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38alpha MAPK, CK1 and JAK2 kinase inhibitors. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3412-8. | ||||
| REF 2 | US patent application no. 8592415B2, Selective kinase inhibitors | ||||
| REF 3 | Identification of imidazo[1,2- b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling. Medchemcomm. 2016 Dec 15;8(4):700-712. | ||||
| REF 4 | N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK. Medchemcomm. 2018 Apr 12;9(6):963-968. | ||||
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