Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T28713 | Target Info | |||
Target Name | Serine/threonine-protein kinase Chk2 (RAD53) | ||||
Synonyms |
hCds1; Hucds1; Checkpoint kinase 2; Cds1 homolog; Cds1; CHK2 checkpoint homolog; CHK2
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Target Type | Clinical trial Target | ||||
Gene Name | CHEK2 | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Poor Binders of This Target (in total, 63 binders) | Download | Top | |||
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Compound Name |
2-[(Z)-[6-(4-Fluorophenyl)-2-methylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910605; NSC-747107
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Activity |
IC50 ~ 50000 nM
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[1] | |||
Compound Name |
2-[9-(4-Amino-3-methoxyphenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepin-3-yl]-2-methyl-N-(4-morpholin-4-ylphenyl)propanamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL389745; BDBM50218709
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Activity |
IC50 ~ 50000 nM
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[2] | |||
Compound Name |
3-(4'-Hydroxybiphenyl-4-Yl)-N-(4-Hydroxycyclohexyl)-1,4-Dihydroindeno[1,2-C]pyrazole-6-Carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL438485; SCHEMBL4809259; SCHEMBL4809267; BDBM91830; BDBM50204694; ZINC100469705; ZINC253994709; Q27456666
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Activity |
IC50 ~ 50000 nM
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[3] | |||
Compound Name |
Pyrazolo pyridine, 11
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Investigative | Compound Info | ||
Synonyms |
CHEMBL560056; SCHEMBL4803059; BDBM33212
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Activity |
IC50 = 50000 nM
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[4] | |||
Compound Name |
2-[(Z)-[2-Fluoro-6-(4-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910607; NSC-748105
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Activity |
IC50 = 56500 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(2,4-Dichloro-5-nitrophenyl)-2-ethylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910758
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Activity |
IC50 = 59000 nM
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[1] | |||
Compound Name |
2-[(E)-[2-Methyl-6-(3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-722871; CHEMBL1910750; NSC722871
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Activity |
IC50 = 59000 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(4-Chloro-3-nitrophenyl)-2-methylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-720136; CHEMBL1910631; NSC720136
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Activity |
IC50 = 64800 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(2,5-Dichlorothiophen-3-yl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-732181; CHEMBL1910757; NSC732181
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Activity |
IC50 = 65000 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(4-Aminophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910628; NSC-709139
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Activity |
IC50 = 67500 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(3-Nitrophenyl)-2-propylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-723551; CHEMBL1910747; NSC723551
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Activity |
IC50 = 69500 nM
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[1] | |||
Compound Name |
2-[(Z)-[6-(4-Fluoro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910602; NSC-747112
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Activity |
IC50 = 77500 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(4-Chloro-3-nitrophenyl)-2-methylimidazo[2,1-b][1,3,4]thiadiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-734178; CHEMBL1910759; NSC734178
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Activity |
IC50 = 78000 nM
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[1] | |||
Compound Name |
2-[(E)-[2-Chloro-6-(4-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-720135; CHEMBL1910625; NSC720135
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Activity |
IC50 = 78750 nM
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[1] | |||
Compound Name |
2-[(E)-[2-(4-Chloro-3-nitrophenyl)imidazo[1,2-a]pyridin-3-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-734179; CHEMBL1910627; NSC734179
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Activity |
IC50 = 79000 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(4-Chloro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-709138; CHEMBL1910629; NSC709138
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Activity |
IC50 = 81000 nM
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[1] | |||
Compound Name |
2-[(E)-[2-Methyl-6-(4-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-720137; CHEMBL1910626; NSC720137
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Activity |
IC50 = 83000 nM
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[1] | |||
Compound Name |
5-[(8-Chloroisoquinolin-3-yl)amino]-3-[(2R)-1-(dimethylamino)propan-2-yl]oxypyrazine-2-carbonitrile
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Investigative | Compound Info | ||
Synonyms |
SCHEMBL1396948; CHEMBL1928704; HMS3741A21; SAR020106;SAR 020106
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Activity |
IC50 = 84000 nM
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[4] | |||
Compound Name |
2-[(E)-[6-(4-Chloro-3-nitrophenyl)-3-methylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-720138; CHEMBL1910756; NSC720138
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Activity |
IC50 = 84400 nM
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[1] | |||
Compound Name |
4-(2-(Methylamino)-5-(thiophen-3-yl)pyridin-3-yl)benzamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL602232; BDBM50309216
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Activity |
IC50 = 85000 nM
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[5] | |||
Compound Name |
2-[(Z)-[2-Bromo-6-(4-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910608; NSC-748103
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Activity |
IC50 = 88500 nM
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[1] | |||
Compound Name |
2-[(E)-[2-Chloro-6-(4-fluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910373; NSC-747109
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Activity |
IC50 = 90000 nM
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[1] | |||
Compound Name |
2-[(E)-[2-Chloro-6-(4-chloro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-722868; CHEMBL1910634; NSC722868
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Activity |
IC50 = 90000 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(4-Chloro-3-nitrophenyl)-2-propylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-723549; CHEMBL1910744; NSC723549
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Activity |
IC50 = 90500 nM
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[1] | |||
Compound Name |
2-[(E)-[2-Chloro-6-(4-cyanophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910375; NSC-748104
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Activity |
IC50 = 93500 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(2,5-Dimethoxy-4-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-725093; CHEMBL1910630; NSC725093
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Activity |
IC50 = 96000 nM
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[1] | |||
Compound Name |
N-[(E)-[6-(4-Chloro-3-nitrophenyl)-2-methylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]-4,5-dihydro-1H-imidazol-2-amine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910753; NSC-730327
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(E)-[2-(2,5-Dimethoxy-4-nitrophenyl)imidazo[2,1-b][1,3]benzothiazol-1-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910614; NSC-745255
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(E)-[2-(2,5-Dichlorothiophen-3-yl)imidazo[2,1-b][1,3]benzothiazol-1-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910616; NSC-745256
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(4-Nitrophenyl)-2-propylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-723552; CHEMBL1910754; NSC723552
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(2,4-Dichloro-5-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-720142; CHEMBL1910635; NSC722864; NSC720142; NSC-722864
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
(R)-2-(4-(3-(Dimethylamino)pyrrolidin-1-yl)quinazolin-2-yl)-6-fluorophenol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1650095; BDBM50335644
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Activity |
IC50 ~ 100000 nM
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[6] | |||
Compound Name |
2-[(E)-[6-(2,4-Dichloro-5-nitrophenyl)-2,3-dimethylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-722877; CHEMBL1910760; NSC722877
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(E)-[2-(4-Chloro-3-nitrophenyl)imidazo[2,1-b][1,3]benzothiazol-1-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-732182; CHEMBL1910745; NSC732182
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(Z)-[6-(4-Fluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910597; NSC-747111
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
(R)-5-(8-Chloroisoquinolin-3-Ylamino)-3-(1-(Dimethylamino)propan-2-Yloxy)pyrazine-2-Carbonitrile
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Investigative | Compound Info | ||
Synonyms |
SAR-020106; SAR020106; CHEMBL1928705; SCHEMBL1396946; SYN1189; BCP29578; EX-A2810; BDBM50359807; s7740; ZINC68207132; CCG-268435; NCGC00387035-01; AC-29017; AS-16323; Q27467786; SAR020106; SAR 020106; SAR20106; SAR20106; SAR 20106
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Activity |
IC50 ~ 100000 nM
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[4] | |||
Compound Name |
2-[(E)-(2-Chloro-6-phenylimidazo[2,1-b][1,3]thiazol-5-yl)methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910372; NSC-747418
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(Z)-[6-(2-Fluoro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910603; NSC-747421
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-Amino-1-[(E)-[6-(4-chloro-3-nitrophenyl)-2-methylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910751; NSC-730326
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
N-[(E)-[2-(2,5-Dichlorothiophen-3-yl)imidazo[2,1-b][1,3]benzothiazol-1-yl]methylideneamino]-4,5-dihydro-1H-imidazol-2-amine;hydrobromide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910617; NSC-745851
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(E)-[2-Chloro-6-(2,5-dichlorothiophen-3-yl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910371; NSC-745252
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(4-Nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-709136; CHEMBL1910633; NSC709136
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Activity |
IC50 ~ 100000 nM
|
[1] | |||
Compound Name |
(4-(2-Amino-5-phenylpyridin-3-yl)phenyl)methanol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL589501; BDBM50309214
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Activity |
IC50 ~ 100000 nM
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[5] | |||
Compound Name |
4-(2-Amino-5-(benzo[b]thiophen-3-yl)pyridin-3-yl)benzamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL590817; BDBM50309215
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Activity |
IC50 ~ 100000 nM
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[5] | |||
Compound Name |
2-[(E)-[6-(2,4-Dichloro-5-nitrophenyl)-2-propylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-723550; CHEMBL1910636; NSC723550
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Activity |
IC50 ~ 100000 nM
|
[1] | |||
Compound Name |
2-[(E)-[6-(3-Nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910752; NSC-722875
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Activity |
IC50 ~ 100000 nM
|
[1] | |||
Compound Name |
2-[(Z)-[6-(4-Bromo-3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1909651; NSC-747420
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Activity |
IC50 ~ 100000 nM
|
[1] | |||
Compound Name |
4-(2-Amino-5-phenylpyridin-3-yl)-N-(2-hydroxyethyl)benzamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL590792; BDBM50309213
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Activity |
IC50 ~ 100000 nM
|
[5] | |||
Compound Name |
2-[(E)-[2-(2,5-Dimethoxy-4-nitrophenyl)imidazo[1,2-a]pyridin-3-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910623; NSC-745849
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Activity |
IC50 ~ 100000 nM
|
[1] | |||
Compound Name |
5-(Isoquinolin-3-ylamino)pyrazine-2-carbonitrile
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1928696; SCHEMBL12983898; BDBM50359815; ZINC73198997
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Activity |
IC50 ~ 100000 nM
|
[4] | |||
Compound Name |
2-[(Z)-[6-[3-(Trifluoromethyl)phenyl]imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910604; NSC-747417
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Activity |
IC50 ~ 100000 nM
|
[1] | |||
Compound Name |
2-[(Z)-[6-(2,4,5-Trifluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910601; NSC-747419
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Activity |
IC50 ~ 100000 nM
|
[1] | |||
Compound Name |
N-Benzyl-N-methyl-4-(phenylsulfamoyl)benzamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3355482; BDBM50043416; ZINC17334508; AKOS008571954; Z31474376
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Activity |
IC50 ~ 100000 nM
|
[7] | |||
Compound Name |
5-[(8-Chloroisoquinolin-3-yl)amino]pyrazine-2-carbonitrile
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1928698; SCHEMBL12983749; BDBM50359813
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Activity |
IC50 ~ 100000 nM
|
[4] | |||
Compound Name |
2-[(E)-[2-Chloro-6-(3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910637; NSC-722874
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Activity |
IC50 ~ 100000 nM
|
[1] | |||
Compound Name |
3-(2-Amino-5-(thiophen-3-yl)pyridin-3-yl)benzamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL590774; BDBM50309212
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Activity |
IC50 ~ 100000 nM
|
[5] | |||
Compound Name |
2-[(Z)-[6-(2,6-Difluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910599; NSC-747413
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(E)-[6-(2,4-Dichloro-5-nitrophenyl)-2-methylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-722870; CHEMBL1910632; NSC722870
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(Z)-[6-(2-Fluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910598; NSC-747415
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Activity |
IC50 ~ 100000 nM
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[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
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[8] | |||
Compound Name |
2-[(E)-[6-(2,5-Dichlorothiophen-3-yl)-2-methylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-732180; CHEMBL1910755; NSC732180
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
2-[(Z)-[6-(3,4-Difluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1910600; NSC-747414
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
1,3-Bis[(E)-[2-chloro-6-(2,5-dimethoxy-4-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
NSC-734184; CHEMBL1910746; NSC734184
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Click to Show/Hide the Information of All Poor Binders |
References | Top | ||||
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REF 1 | Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. Eur J Med Chem. 2011 Sep;46(9):4311-23. | ||||
REF 2 | Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors. J Med Chem. 2007 Aug 23;50(17):4162-76. | ||||
REF 3 | Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem. 2007 Apr 1;15(7):2759-67. | ||||
REF 4 | Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem. 2011 Dec 22;54(24):8328-42. | ||||
REF 5 | Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2. Bioorg Med Chem. 2010 Jan 15;18(2):707-18. | ||||
REF 6 | Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J Med Chem. 2011 Jan 27;54(2):580-90. | ||||
REF 7 | Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. ACS Med Chem Lett. 2014 Aug 7;6(1):53-7 | ||||
REF 8 | 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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