Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T47107 | Target Info | |||
| Target Name | Protein kinase C gamma (PRKCG) | ||||
| Synonyms |
PRKCG; PKCG; PKC-gamma
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| Target Type | Successful Target | ||||
| Gene Name | PRKCG | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
L-751250
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Preclinical | Compound Info | ||
| Synonyms |
Purvalanol B; 212844-54-7; PURVALANOL; Purvalanol B(NG-95); (R)-2-chloro-4-((2-((1-hydroxy-3-methylbutan-2-yl)amino)-9-isopropyl-9H-purin-6-yl)amino)benzoic acid; (2R)-2-[[6-[(3-CHLORO-4-CARBOXYPHENYL)AMINO]-9-(1-METHYLETHYL)-9H-PURIN-2-YL]AMINO]-3-METHYL-1-BUTANOL; CHEMBL23254; CHEBI:49840; NG 95; NG-95; C20H25ClN6O3; 2-chloro-4-[[2-[[(2R)-1-hydroxy-3-methylbutan-2-yl]amino]-9-propan-2-ylpurin-6-yl]amino]benzoic acid; J-502183; PVB
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
A-432411
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Investigative | Compound Info | ||
| Synonyms |
43A; (3Z)-6-(4-HYDROXY-3-METHOXYPHENYL)-3-(1H-PYRROL-2-YLMETHYLENE)-1,3-DIHYDRO-2H-INDOL-2-ONE; 2ayp; indolinone analog 13; A-432411; CHEMBL202930; SCHEMBL6674605; BDBM14649; DB07078; 29690-EP2311842A2; 29690-EP2289868A1; 29690-EP2289894A2; (3Z)-6-(4-hydroxy-3-methoxyphenyl)-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-2-one; (3Z)-6-(4-hydroxy-3-methoxyphenyl)-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihydro-1H-indol-2-one
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| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
aloisine A
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Investigative | Compound Info | ||
| Synonyms |
ALOISINE A; 4-(7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenol; 496864-16-5; RP107; 6-PHENYL[5H]PYRROLO[2,3-B]PYRAZINE; CHEMBL75680; 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine; RP-107; ALH; 4-{7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl}phenol; 1ung; SCHEMBL80147; BDBM7377; GTPL5924; AC1NS169; 4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol; CHEBI:93641; CTK8D4068; DTXSID30416115; HMS3229A14; RM-39; BCP26893; ZINC2540737; ACT06534; IN1539; HSCI1_000219; MFCD04973541; AKOS005145972; CCG-206814; DB07364; RTC-063070; AJ-39131
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[[(3R,4S)-3-[(4-hydroxybenzoyl)amino]azepan-4-yl]-methylcarbamoyl]benzoyl]-3-hydroxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2310935; BDBM50450311
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| Activity |
IC50 ~ 50000 nM
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[4] | |||
| Compound Name |
5-(Methoxymethyl)-4-[2,3,4-trihydroxy-6-(methoxymethyl)phenyl]benzene-1,2,3-triol
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Investigative | Compound Info | ||
| Synonyms |
hbdde; CHEMBL59451; Hhbpdde; [1,1'-Biphenyl]-2,2',3,3',4,4'-hexol,6,6'-bis(methoxymethyl)-; CHEMBL437222; CHEMBL537897; BiomolKI_000067; BiomolKI2_000071; BMK1-G7; BSPBio_001115; KBioGR_000455; KBioSS_000455; SCHEMBL1272421; CTK4C8370; KBio2_000455; KBio2_003023; KBio2_005591; KBio3_000849; KBio3_000850; DTXSID20935042; Bio2_000388; Bio2_000868; HMS1362G17; HMS1792G17; HMS1990G17; HMS3403G17; ZINC3800021; BDBM50043774; BDBM50375658; BDBM50375660; CCG-100671; IDI1_002143; NCGC00163390-01; NCGC00163390-02; NCGC00163390-03; NCGC00163390-04; HBDDE - CAS 154675-18-0; J-009130; BRD-K56064827-001-03-9; BRD-K56064827-001-04-7; Q27166474; 6,6''-Bis-methoxymethyl-biphenyl-2,3,4,2'',3'',4''-hexaol; 6,6'-Bis(methoxymethyl)[1,1'-biphenyl]-2,2',3,3',4,4'-hexol
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| Activity |
IC50 = 50000 nM
|
[5] | |||
| Compound Name |
2-[9-(4-Amino-3-methoxyphenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepin-3-yl]-N-(4-morpholin-4-ylphenyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL395080; BDBM50218700
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| Activity |
IC50 ~ 50000 nM
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[6] | |||
| Compound Name |
(3Z)-6-(4-Hydroxy-3-methoxyphenyl)-3-(1H-imidazol-2-ylmethylidene)-2,3-dihydro-1H-indol-2-one
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Investigative | Compound Info | ||
| Synonyms |
indolinone analog 29; CHEMBL199299; BDBM14665
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| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
3,13-Diazahexacyclo[14.8.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tetracosa-1(16),2(10),4(9),5,7,11(15),17(22),18,20,23-decaene-12,14-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL332575; Imide Analog 12; BDBM14187; 11H-Naphtho[2,1-a]carbazole-5,6-dicarbimide; 6H,14H-naphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5,7(5H,7H)-dione
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| Activity |
IC50 = 56500 nM
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[7] | |||
| Compound Name |
Hippolide A
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1782082; BDBM50345577; Q27136206
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| Activity |
IC50 = 61970 nM
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[8] | |||
| Compound Name |
Betulinic acid 3-O-benzoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL509553; BDBM50292432; 3beta-(Benzoyloxy)lupa-20(29)-ene-28-oic acid
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| Activity |
IC50 = 74000 nM
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[9] | |||
| Compound Name |
1-(Tert-Butyl)-3-(naphthalen-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
1-NAPHTHYL PP1; 1-NA-PP1; pp1 analog; 4-Amino-1-tert-butyl-3-(1'-naphthyl)pyrazolo[3,4-d]pyrimidine; 1-(1,1-dimethylethyl)-3-(1-naphthalenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; 1-tert-butyl-3-naphthalen-1-ylpyrazolo[3,4-d]pyrimidin-4-amine; CHEMBL264406; 1-tert-butyl-3-(naphthalen-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; C19H19N5; 1-tert-butyl-3-naphthalen-1-yl-1H-pyrazolo[3,4-d]pyrimidin-4-amine; 1-tert-butyl-3-naphthalen-1-yl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine; 1-Na PP1; 1-NaphthylPP1; NA-PP1; K00047; SCHEMBL173288; 1-NA-PP 1; CTK4E8691; 1-Naphthyl PP1(1-NA-PP1); DTXSID00274446; EX-A867; HMS3266C18; HMS3413H14; HMS3677H14; PP1-AG1872; BCP09108; ZINC2576349; 3272AH; 4-Amino-1-tert-butyl-3-(1'naphthyl)pyrazolo[3,4-d]pyrimidine; BDBM50229961; MFCD03425471; QC-203; s2642; AKOS024457409; ACN-046104; CS-1804; MB02817; KS-00001D85; NCGC00262627-06; AS-56537; HY-13941; AB0094864; PP1 Analog - CAS 221243-82-9; FT-0661645; A13232; InSolution PP1 Analog - CAS 221243-82-9; 425B471; W-201916; BRD-K29542628-001-01-3; Q27123369; 1-t-butyl-3-naphthalen-1-yl-1h-pyrazolo[3,4-d]pyrimidin-4-ylamine; 4-Amino-1-tert-butyl-3-(1''-naphthyl)pyrazolo[3,4-d]pyrimidine; 4-Amino-1-tert-butyl-3-(1?-naphthyl)pyrazolo[3,4-d]pyrimidine; 1-(tert-butyl)-3-(naphthalen-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine (4); 1H-pyrazolo[3,4-d]pyrimidin-4-amine, 1-(1,1-dimethylethyl)-3-(1-naphthalenyl)-; 1H-Pyrazolo[3,4-d]pyrimidin-4-amine,1-(1,1-dimethylethyl)-3-(1-naphthalenyl)-
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| Activity |
IC50 ~ 100000 nM
|
[10] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
4-Phenyl-[1]benzofuro[2,3-b]pyridine-3,6-diol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2163772; BDBM50395892
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| Activity |
Ki > 1000000 nM
|
[11] | |||
| Compound Name |
N-(4-Methoxybenzyl)benzofuro[2,3-b]pyridin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1290072; BDBM50331612
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| Activity |
Ki > 1000000 nM
|
[12] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8. | ||||
| REF 2 | Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors. Bioorg Med Chem Lett. 2006 Jan 15;16(2):421-6. | ||||
| REF 3 | Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46(2):222-36. | ||||
| REF 4 | Novel PKC inhibitory analogs of balanol with replacement of the ester functionality. Bioorg Med Chem Lett. 1995 Sep 7;5(17):2015-20. | ||||
| REF 5 | New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C. J Med Chem. 1994 Jan 7;37(1):195-200. | ||||
| REF 6 | 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 7 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. Bioorg Med Chem Lett. 2003 Nov 3;13(21):3835-9. | ||||
| REF 8 | Hippolides A-H, acyclic manoalide derivatives from the marine sponge Hippospongia lachne. J Nat Prod. 2011 May 27;74(5):1248-54. | ||||
| REF 9 | Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids. J Nat Prod. 1994 Feb;57(2):243-7. | ||||
| REF 10 | Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2... J Biol Chem. 2007 Nov 9;282(45):33052-63. | ||||
| REF 11 | Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6914-8. | ||||
| REF 12 | Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6915-9. | ||||
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