Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T50594 | Target Info | |||
| Target Name | Serine/threonine-protein kinase pim-1 (PIM1) | ||||
| Synonyms |
Pim-1 proto-oncogene, serine/threonine kinase; PIM
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| Target Type | Clinical trial Target | ||||
| Gene Name | PIM1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 45 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
PINOCEMBRIN
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|
Phase 2 | Compound Info | ||
| Synonyms |
Pinocembrin; 480-39-7; (+)-Pinocembrin; (2S)-pinocembrin; Dihydrochrysin; UNII-8T7C8CH791; NSC 43318; NSC 279005; NSC 661207; 4H-1-Benzopyran-4-one, 2,3-dihydro-5,7-dihydroxy-2-phenyl-, (2S)-; (S)-5,7-dihydroxyflavanone; (S)-5,7-dihydroxy-2-phenylchroman-4-one; CHEMBL399910; CHEBI:28157; (2s)-5,7-dihydroxy-2-phenyl-2,3-dihydro-4h-chromen-4-one; (S)-2,3-Dihydro-5,7-dihydroxy-2-phenyl-4H-1-benzopyran-4-one; 8T7C8CH791; Pinocembrin (6CI); 4H-1-Benzopyran-4-one, 2,3-dihydro-5,7-dihydroxy-2-phenyl-, (-)-
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| Activity |
IC50 = 107000 nM
|
[1] | |||
| Compound Name |
NSC-73306
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Investigative | Compound Info | ||
| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-(1H-Indol-3-yl)-1H-imidazo[4,5-c]pyridin-2-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL575945; SCHEMBL1990207; BDBM50393115
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| Activity |
IC50 = 50000 nM
|
[3] | |||
| Compound Name |
N-[4-[[3-[3-(Dimethylamino)phenyl]pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]-4-methylbenzenesulfonamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3355540; SCHEMBL178324; BDBM50043698
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| Activity |
IC50 = 52000 nM
|
[4] | |||
| Compound Name |
1,4,5,8,9,10-Anthracenehexol
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|
Investigative | Compound Info | ||
| Synonyms |
1,4,5,8,9,10-Hexahydroxyanthracene; CHEMBL3810033; 1,4,5,8,9,10-Anthracenehexol (8CI)(9CI); 1,4,5,8,9,10-Anthrahexol; NSC 31336; NSC31336; anthracene-1,4,5,8,9,10-hexol; 1,5,8,9,10-Anthrahexol; CTK1A6087; DTXSID40178035; 1,5,8,9,10-Hexahydroxyanthracene; BDBM50174538; NSC-31336; ZINC100516554; DS-008384
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| Activity |
IC50 = 57100 nM
|
[5] | |||
| Compound Name |
(5E)-1-Benzyl-5-[(4-bromophenyl)methylidene]imidazolidine-2,4-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL522916; BDBM26652; 5-Arylidene-3-benzylhydantoin, 29c-1
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| Activity |
IC50 = 58000 nM
|
[6] | |||
| Compound Name |
3-(2-Fluorobenzyl)-1,3-thiazolidine-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
BAS 07786895; CHEMBL506711; ZINC4498572; STL370236; AKOS000348948; MCULE-7964484038; CS-0118417; SR-01000322937; SR-01000322937-1
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| Activity |
IC50 = 63000 nM
|
[6] | |||
| Compound Name |
(5E)-1-Benzyl-5-[(4-chlorophenyl)methylidene]imidazolidine-2,4-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL496588; SCHEMBL2542527
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| Activity |
IC50 = 69000 nM
|
[6] | |||
| Compound Name |
(5E)-1-Benzyl-5-[(4-ethoxyphenyl)methylidene]imidazolidine-2,4-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL496971
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| Activity |
IC50 = 73000 nM
|
[6] | |||
| Compound Name |
(5E)-1-Benzyl-5-[(4-methoxyphenyl)methylidene]imidazolidine-2,4-dione;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL526284
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| Activity |
IC50 = 75000 nM
|
[6] | |||
| Compound Name |
(5E)-1-Benzyl-5-[(2-methoxyphenyl)methylidene]imidazolidine-2,4-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL496973
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| Activity |
IC50 = 78000 nM
|
[6] | |||
| Compound Name |
(5E)-1-Benzyl-5-[[4-(dimethylamino)phenyl]methylidene]imidazolidine-2,4-dione
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|
Investigative | Compound Info | ||
| Synonyms |
(5E)-1-benzyl-5-{[4-(dimethylamino)phenyl]methylidene}imidazolidine-2,4-dione; CHEMBL496972; SCHEMBL2545538; BDBM26653; 5-Arylidene-3-benzylhydantoin, 30c
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| Activity |
IC50 = 78000 nM
|
[6] | |||
| Compound Name |
N-(3-Methoxyphenyl)-3-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-8-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3782023
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
(8S,16S)-3,16-Dihydroxy-9,10-seco-1,3,5(10)-cholestatrien-9-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL456294; Calicoferol I; USFQLAVWHQCNDG-AYEIPMSGSA-; BDBM50358248; LMST03020180
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
3-Phenyl-N-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-7-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780571
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
Calicoferol E
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL456936; (8S)-3-hydroxy-9,10-seco-1,3,5(10)-cholestatrien-9-one; BDBM50358246; LMST03020157
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
N-(3-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-7-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781159
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-[7-(3,4-Dimethoxyphenyl)-1,5-naphthyridin-2-yl]-3-ethylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318024; SCHEMBL1932174; BDBM50050850
Click to Show/Hide
|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
N-(4-Morpholin-4-ylphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780515
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
3-[1-(4-Chlorobenzyl)-1h-indol-3-yl]-n-(4-nitrophenyl)propanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1221633; BDBM50324796
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|
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| Activity |
IC50 ~ 100000 nM
|
[10] | |||
| Compound Name |
7-[[(1R,2S,4Ar,8aS)-1,2,4a,5-tetramethyl-2,3,4,7,8,8a-hexahydronaphthalen-1-yl]methyl]-5-methoxy-2-methyl-1,3-benzoxazol-6-ol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3109402; BDBM50446565
Click to Show/Hide
|
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| Activity |
IC50 ~ 100000 nM
|
[11] | |||
| Compound Name |
N-(4-Morpholin-4-ylphenyl)-2-phenylpyrido[3,4-b]pyrazin-7-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780543
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-Tert-butyl-3-[7-(3,4-dimethoxyphenyl)-1,5-naphthyridin-2-yl]urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318025; SCHEMBL1932951; BDBM50050849
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|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
N-(3-Ethynylphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780350
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-Ethyl-3-(2-phenylpyrido[3,4-b]pyrazin-5-yl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780985
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-(3-Methoxyphenyl)-3-(2-phenylpyrido[3,4-b]pyrazin-5-yl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780768
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-(3-Phenylpyrido[3,4-b]pyrazin-8-yl)-3-prop-2-enylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781906
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
N-Phenyl-3-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-8-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781538
Click to Show/Hide
|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
Calicoferol C
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL515982; BDBM50358249
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
Calicoferol B
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL464351; BDBM50358250
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
Astrogorgiadiol B
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|
Investigative | Compound Info | ||
| Synonyms |
ASTROGORGIADIOL; (8S,9R)-9,10-seco-1,3,5(10)-cholestatriene-3,9-diol; LMST03020242; CHEMBL517956; SCHEMBL4865385; BDBM50358247
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
N-(Pyridin-4-yl)-3-[1-(4-chlorobenzyl)indol-3-yl]-propanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL185140; SCHEMBL21585709; BDBM50324797; 3-(1-(4-chlorobenzyl)-1H-indol-3-yl)-N-(pyridin-4-yl)propanamide; 3-[1-(4-Chloro-benzyl)-1H-indol-3-yl]-N-pyridin-4-yl-propionamide
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|
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| Activity |
IC50 ~ 100000 nM
|
[10] | |||
| Compound Name |
N-(3-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781584
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
N-(2-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781543
Click to Show/Hide
|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
N-(3-Chloro-4-fluorophenyl)-3-phenylpyrido[3,4-b]pyrazin-8-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780151
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
Calicoferol A
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|
Investigative | Compound Info | ||
| Synonyms |
(22E)-(8S)-3-hydroxy-9,10-seco-1,3,5(10),22-cholestatetraen-9-one; LMST03020605; CHEMBL518060; BDBM50358244
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
N-(4-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781566
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-Tert-butyl-3-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318027; SCHEMBL1932932; BDBM50050847
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|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| 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
|
[12] | |||
| Compound Name |
2-(4-Methoxyphenyl)-N-(4-morpholin-4-ylphenyl)pyrido[3,4-b]pyrazin-5-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780637
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
Rel-Astrogorgol F
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1922224; BDBM50358243
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
1-Tert-butyl-3-[7-(4-hydroxy-3-methoxyphenyl)-1,5-naphthyridin-2-yl]urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318026; SCHEMBL1933008; BDBM50050848
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
24-Exomethylenecalicoferol E
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1922225; BDBM50358245
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
Benzofuran-2-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
Coumarilic acid; 1-Benzofuran-2-carboxylic acid; Benzo[b]furan-2-carboxylic acid; 2-BENZOFURANCARBOXYLIC ACID; 2-Carboxybenzofuran; Coumarone-2-carboxylic acid; MFCD00005848; UNII-7Z6NMG947L; Benzo(b)furan-2-carboxylic acid; 2-Benzofuran carboxylic acid; CHEMBL84095; 7Z6NMG947L; NSC6165; Benzo[b]furan-2-carboxylic acid, 98%; NSC 6165; EINECS 207-818-9; benzofuran-2-carboxylicacid; BRN 0124204; AI3-03711; PubChem7019; Maybridge1_002455; ACMC-209kh6; 2-benzofuranecarboxylic acid; Cambridge id 5102130; benzofuran 2-carboxylic acid; 5-18-06-00419 (Beilstein Handbook Reference); KSC173I5H; DivK1c_001207; SCHEMBL155789; 1-benzofurane-2-carboxylic acid; DTXSID2060090; HMS548H13; ZINC53963; 1-Benzofuran-2-carboxylic acid #; 2,3-benzofuran-2-carboxylic acid; 4,5-benzofuran-2-carboxylic acid; ACN-S004172; ALBB-016356; KS-00000MZ3; NSC-6165; Benzofuran-2-carboxylic acid, 99%; ANW-30808; BBL018112; BDBM50345230; SBB000137; STK293001; AKOS000103488; AB00533; CS-W004676; MCULE-5646971945; SDCCGMLS-0065938.P001; SS-6002; CDS1_000167; NCGC00324555-01; AK-29301; BR-29301; SC-04821; ST021134; SY005603; DB-022566; AM20050579; BB 0244005; FT-0622682; A19599; L-1275; AB01319519-02; 496B413; AN-278/25047013; J-640024; J-800026; Q-101915; Q27269061; Z56839706; F3096-1740
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| Activity |
IC50 = 119000 nM
|
[13] | |||
| Compound Name |
5-(1-(4-Fluorobenzyl)-1H-1,2,3-triazol-4-yl)-1H-indazole
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1682352; SCHEMBL4297782; BDBM50337330; 5-[1-[(4-fluorophenyl)methyl]triazol-4-yl]-1H-indazole
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| Activity |
Ki = 165230 nM
|
[14] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
7-(2-Carboxyethylamino)-1-cyclopropyl-6-fluoro-8-nitro-4-oxoquinoline-3-carboxylic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4086292; BDBM50260554
Click to Show/Hide
|
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| Activity |
IC50 = 54871000 nM
|
[15] | |||
| Compound Name |
7-(2-Carboxyethylamino)-1-ethyl-6-fluoro-8-nitro-4-oxoquinoline-3-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4102686; BDBM50260547
Click to Show/Hide
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| Activity |
IC50 = 56511000 nM
|
[15] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Comparative molecular field analysis of flavonoid inhibitors of the PIM-1 kinase. Bioorg Med Chem. 2007 Oct 1;15(19):6463-73. | ||||
| REF 2 | Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. J Med Chem. 2009 May 28;52(10):3191-204. | ||||
| REF 3 | A one-pot synthesis and biological activity of ageladine A and analogues. J Med Chem. 2011 Apr 14;54(7):2492-503. | ||||
| REF 4 | Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors. ACS Med Chem Lett. 2014 Oct 22;6(1):63-7. | ||||
| REF 5 | Identification of quinones as novel PIM1 kinase inhibitors. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3187-3191. | ||||
| REF 6 | Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J Med Chem. 2009 Jan 8;52(1):74-86. | ||||
| REF 7 | Efficient synthesis of novel disubstituted pyrido[3,4-b]pyrazines for the design of protein kinase inhibitors. Medchemcomm. 2016;7:224-9. | ||||
| REF 8 | 9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp. Bioorg Med Chem. 2011 Nov 15;19(22):6873-80. | ||||
| REF 9 | Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3748-52. | ||||
| REF 10 | Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5203-6. | ||||
| REF 11 | Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia. J Nat Prod. 2014 Feb 28;77(2):218-26. | ||||
| REF 12 | N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK. Medchemcomm. 2018 Apr 12;9(6):963-968. | ||||
| REF 13 | The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors. Bioorg Med Chem Lett. 2011 May 15;21(10):3050-6. | ||||
| REF 14 | Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1476-9. | ||||
| REF 15 | Structure based drug design of Pim-1 kinase followed by pharmacophore guided synthesis of quinolone-based inhibitors. Bioorg Med Chem. 2017 Sep 1;25(17):4855-4875. | ||||
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