Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T59190 | Target Info | |||
| Target Name | Protein kinase C zeta (PRKCZ) | ||||
| Synonyms |
Protein kinase C zeta type; PKC2; NPKC-zeta
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| Target Type | Patented-recorded Target | ||||
| Gene Name | PRKCZ | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 55 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Dasatinib
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|
Approved | Compound Info | ||
| Synonyms |
Sprycel (TN); BMS 354825; BMS-354825; BMS-354825, Sprycel, BMS354825, Dasatinib; BMS354825; Dasatinib (USAN); Dasatinib [USAN]; Dasatinib anhydrous; Dasatinib, BMS 354825; Dasatinibum; Sprycel; Spyrcel
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
LY333531
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Phase 2 | Compound Info | ||
| Synonyms |
Ruboxistaurin; 169939-94-0; LY-333531; Ruboxistaurin [INN]; LY 333531; UNII-721809WQCP; 721809WQCP; K00587a; 13-((Dimethylamino)methyl)-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo(e,k)pyrrolo(3,4-h)(1,4,13)oxadiazacyclohexadecene-1,3(2H)-dione; CHEMBL432130; (9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-di(metheno)dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione; Br-WR99210
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| 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
|
[3] | |||
| 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
|
[4] | |||
| Compound Name |
N-(7-Methoxyquinolin-6-yl)thieno[3,2-d]pyrimidine-7-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL357756; CHEMBL3822972; BDBM206104; DB-085143; US9255110, 17
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid (1R,2R)-2-(4-hydroxy-benzoylamino)-4-methylcarbamoyl-cyclopentyl ester
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL312067; BDBM50055665
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
2-(2,6-Dihydroxy-4-{[(1S,2R)-2-(4-hydroxy-benzoylamino)-cyclopentylmethyl]-carbamoyl}-benzoyl)-3-hydroxy-benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL293500; BDBM50285092
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|
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[[3-[(4-hydroxybenzoyl)amino]-1-azabicyclo[3.2.2]nonan-4-yl]oxycarbonyl]benzoyl]-3-hydroxybenzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL306884; SCHEMBL8303095
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| 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
|
[7] | |||
| Compound Name |
[6-Chloro-4-methyl-3-[[3-(methylsulfamoylamino)phenyl]methyl]-2-oxochromen-7-yl] N,N-dimethylcarbamate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3086065; SCHEMBL959662; BDBM50443366
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| Activity |
IC50 ~ 50000 nM
|
[9] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[[(1R,2R)-2-[(4-hydroxybenzoyl)amino]cyclopentyl]methoxycarbonyl]benzoyl]-3-hydroxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL60455; BDBM50285090
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[[9-[(4-hydroxybenzoyl)amino]-8-tricyclo[5.2.1.02,6]decanyl]oxycarbonyl]benzoyl]-3-hydroxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL72480; SCHEMBL8304368
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|
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| Compound Name |
5-(3,4-Dimethoxyphenyl)-4-(1H-indol-5-ylamino)pyridine-3-carbonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL492251; BMCL192461 Compound 1a; SCHEMBL2984333; BDBM25558; 4-arylamino-3-pyridinecarbonitrile, 4p; 5-(3,4-dimethoxyphenyl)-4-(1H-indol-5-ylamino)nicotinonitrile
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| Activity |
IC50 ~ 50000 nM
|
[10] | |||
| Compound Name |
(R)-2-{2,6-Dihydroxy-4-[3-(4-hydroxy-benzoylamino)-azepan-4-ylcarbamoyl]-benzoyl}-3-hydroxy-benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL59687; BDBM50285089
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[[3-[(4-hydroxybenzoyl)amino]-1,7,7-trimethyl-2-bicyclo[2.2.1]heptanyl]oxycarbonyl]benzoyl]-3-hydroxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL306170
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[[3-[(4-hydroxybenzoyl)amino]-2-bicyclo[2.2.1]heptanyl]oxycarbonyl]benzoyl]-3-hydroxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL305667; SCHEMBL8304244
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|
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid 2-(4-hydroxy-benzoylamino)-8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL306883; SCHEMBL8303183; BDBM50055675
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid (2R,3R)-3-(4-hydroxy-benzoylamino)-1,7,7-trimethyl-bicyclo[2.2.1]hept-2-yl ester
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL309078; BDBM50055667
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|
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
Modified Benzophenone Ring, Balanol Analog 20
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Investigative | Compound Info | ||
| Synonyms |
BDBM3220; CHEMBL294303
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|
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| Compound Name |
(18S)-18-[(Benzylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL328229; BDBM50052040
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|
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| Activity |
IC50 = 54000 nM
|
[2] | |||
| Compound Name |
(18S)-18-(Pyrrolidin-1-ylmethyl)-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL419866; BDBM50052038; 3,4-[[(S)-3-Oxa-4-(pyrrolizinomethyl)hexane-1,6-diyl]bis(1H-indole-1,3-diyl)]-3-pyrroline-2,5-dione
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| Activity |
IC50 = 55000 nM
|
[2] | |||
| Compound Name |
4-(6-Chloro-4-methyl-1H-benzimidazol-2-yl)-3-(4-chlorophenyl)butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1829833; SCHEMBL2303116; BDBM50353648
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| Activity |
IC50 = 55000 nM
|
[11] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid (1R,2R)-2-(4-hydroxy-benzoylamino)-4-(2,2,2-trifluoro-acetyl)-cyclopentyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL262980; BDBM50055679
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| Activity |
IC50 = 56000 nM
|
[6] | |||
| Compound Name |
US8889672, Apogee B
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3702555; SCHEMBL13837684; BDBM139492
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| Activity |
IC50 = 71000 nM
|
[12] | |||
| Compound Name |
6-(2,9-Diazaspiro[5.5]undecan-9-Yl)-9h-Purine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2420911; BDBM50439463; 9-(9H-purin-6-yl)-2,9-diazaspiro[5.5]undecane; Q27451706; 15I
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| Activity |
IC50 = 74000 nM
|
[13] | |||
| Compound Name |
3-[1-(1-Benzyl-piperidin-4-yl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-pyrrole-2,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL300549; BDBM50128284; 3-(1-(1-benzylpiperidin-4-yl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione; 3-(1-Methyl-1H-indole-3-yl)-4-[1-(1-benzylpiperidine-4-yl)-1H-indole-3-yl]-1H-pyrrole-2,5-dione
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| Activity |
IC50 ~ 100000 nM
|
[14] | |||
| Compound Name |
4-(4-Methyl-1H-indole-5-ylamino)-5-[5-(4-methylpiperazinomethyl)benzofuran-2-yl]pyridine-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL571581; SCHEMBL2984577; BDBM50302042
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| Activity |
IC50 ~ 100000 nM
|
[15] | |||
| Compound Name |
5-Vinyl-3-pyridinecarbonitrile, 14b
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL593883; SCHEMBL2933835; SCHEMBL2933837; BDBM35129
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| Activity |
IC50 ~ 100000 nM
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[16] | |||
| Compound Name |
5-Vinyl-3-pyridinecarbonitrile, 13b
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL603418; SCHEMBL2928579; SCHEMBL2928581; BDBM35126; 4-[(4-methyl-1H-indol-5-yl)amino]-5-[(E)-4-piperazin-1-ylbut-1-enyl]pyridine-3-carbonitrile
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| Activity |
IC50 ~ 100000 nM
|
[16] | |||
| Compound Name |
5-Vinyl-3-pyridinecarbonitrile, 19
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL606245; BDBM35137
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| Activity |
IC50 ~ 100000 nM
|
[16] | |||
| Compound Name |
4-(4-Methyl-1H-indol-5-ylamino)-5-(3-(4-methylpiperazin-1-ylsulfonyl)styryl)nicotinonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1080994; SCHEMBL2934634; BDBM50311953
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| Activity |
IC50 ~ 100000 nM
|
[17] | |||
| Compound Name |
5-Vinyl-3-pyridinecarbonitrile, 24
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL595048; SCHEMBL2928203; BDBM35142
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| Activity |
IC50 ~ 100000 nM
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[16] | |||
| Compound Name |
1-((5-(3-Ethynyl-2-((4-methyl-1H-inden-5-yl)methyl)phenyl)furan-2-yl)methyl)-4-methylpiperazine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL570865; BDBM50301686
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| Activity |
IC50 ~ 100000 nM
|
[18] | |||
| Compound Name |
3-(1-Methyl-1H-indole-3-yl)-4-[1-(1-benzylpyrrolidine-3-yl)-1H-indole-3-yl]-1H-pyrrole-2,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL291975; SCHEMBL6421778; BDBM50128283; 3-[1-(1-Benzyl-pyrrolidin-3-yl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-pyrrole-2,5-dione
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| Activity |
IC50 ~ 100000 nM
|
[14] | |||
| Compound Name |
4-(4-Methyl-1H-indol-5-ylamino)-2-(3-oxo-3-(pyrrolidin-1-yl)prop-1-enyl)thieno[2,3-b]pyridine-5-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL477817; SCHEMBL5520662; SCHEMBL5520668; BDBM50263132
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| Activity |
IC50 ~ 100000 nM
|
[19] | |||
| Compound Name |
4-(4-Methyl-1H-indol-5-ylamino)-5-(4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl)nicotinonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL467069; SCHEMBL2983866; BDBM50258822
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| Activity |
IC50 ~ 100000 nM
|
[20] | |||
| Compound Name |
3-(1-Methyl-1H-indole-3-yl)-4-[1-[1-(tert-butoxycarbonyl)piperidine-4-yl]-1H-indole-3-yl]-1H-pyrrole-2,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL293805; BDBM50128289
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| Activity |
IC50 ~ 100000 nM
|
[14] | |||
| Compound Name |
4-(4-Methyl-1H-indol-5-ylamino)-5-(3-(2-(4-methylpiperazin-1-yl)ethoxy)styryl)nicotinonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL567124; SCHEMBL2934756; BDBM50302507
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| Activity |
IC50 ~ 100000 nM
|
[21] | |||
| Compound Name |
6-Methyl-4-(4-methyl-1H-indol-5-ylamino)-5-(3-(4-methylpiperazin-1-ylsulfonyl)styryl)nicotinonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1080995; SCHEMBL2934911; BDBM50311954
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| Activity |
IC50 ~ 100000 nM
|
[17] | |||
| Compound Name |
Purvalanol A
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Investigative | Compound Info | ||
| Synonyms |
2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine; 6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine; CHEMBL23327; UNII-YP483E75C4; NG-60; NG 60; YP483E75C4; MFCD02179211; (2R)-2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]-3-methylbutan-1-ol; C19H25ClN6O; Tocris-1580; Purvalanol A(NG 60); Lopac-P-4484; MLS006010846; SCHEMBL1217069; BCBcMAP01_000180; BDBM27216; AOB6163; DTXSID30175553; EX-A648; 2,6,9-Trisubstitute purine, 1; 2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropyl-purine; HMS3268E19; HMS3412L07; HMS3676L07; ZINC582575; BCP06309; 3983AH; HY-18299A; s7793; AKOS022185058; CCG-101285; CS-4001; DB04751; SMP1_000251; NCGC00015814-01; NCGC00025219-01; NCGC00025219-02; NCGC00025219-04; NCGC00025219-10; Purvalanol A, >=98% (HPLC), powder; Purvalanol A - CAS 212844-53-6; SMR004701771; J-013971; BRD-K50836978-001-01-7; Q27464217; (2R)-2-[[6-(3-chloroanilino)-9-isopropyl-purin-2-yl]amino]-3-methyl-butan-1-ol; 6-(3-CHLOROANILINO)-2(1R)-ISOPROPYL-2-HYDROXYETHYLAMINO-9-ISOPROPYLPURINE
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
5-Vinyl-3-pyridinecarbonitrile, 13a
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL593619; SCHEMBL2927188; SCHEMBL2927191; BDBM35125; 4-[(4-methyl-1H-indol-5-yl)amino]-5-[(E)-3-piperazin-1-ylprop-1-enyl]pyridine-3-carbonitrile
Click to Show/Hide
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| Activity |
IC50 ~ 100000 nM
|
[16] | |||
| Compound Name |
(E)-4-(4-Methyl-1H-indol-5-ylamino)-5-(2-(6-((4-methylpiperazin-1-yl)methyl)pyridin-2-yl)vinyl)nicotinonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1084411; SCHEMBL2928701; BDBM50313569
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| Activity |
IC50 ~ 100000 nM
|
[22] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[(3R,4R)-3-[(4-hydroxybenzoyl)amino]thiepan-4-yl]oxycarbonylbenzoyl]-3-hydroxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL67788; BDBM50285234
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| Activity |
IC50 = 121000 nM
|
[23] | |||
| Compound Name |
3-Hydroxy-2-[2,6-dihydroxy-4-[[[[3beta-[(4-hydroxybenzoyl)amino]hexahydrothiepin]-4alpha-yl]oxy]carbonyl]benzoyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL76537; SCHEMBL9393090; BDBM50055674
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| Activity |
IC50 = 121000 nM
|
[6] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid (1R,2R)-4-acetyl-2-(4-hydroxy-benzoylamino)-cyclopentyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL441802; BDBM50055673
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| Activity |
IC50 ~ 150000 nM
|
[6] | |||
| Compound Name |
Balanol analog 3
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL67442; BDBM3151
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| Activity |
IC50 ~ 150000 nM
|
[24] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid (1R,2R)-2-(4-hydroxy-benzoylamino)-4-methanesulfonyl-cyclopentyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL306623; BDBM50055678
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| Activity |
IC50 ~ 150000 nM
|
[6] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[(3S,4R)-3-[(4-hydroxybenzoyl)amino]-1,1-dioxothiepan-4-yl]oxycarbonylbenzoyl]-3-hydroxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL305718; SCHEMBL9393845; BDBM50055680
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| Activity |
IC50 ~ 150000 nM
|
[6] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[(3R,4R)-3-[(4-hydroxybenzoyl)amino]-1,1-dioxothiepan-4-yl]oxycarbonylbenzoyl]-3-hydroxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL303205; BDBM50285235
Click to Show/Hide
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| Activity |
IC50 ~ 150000 nM
|
[23] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[(3S,4R)-3-[(4-hydroxybenzoyl)amino]oxepan-4-yl]oxycarbonylbenzoyl]-3-hydroxybenzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL70078; BDBM50285233
Click to Show/Hide
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||||
| Activity |
IC50 ~ 150000 nM
|
[23] | |||
| Compound Name |
3-Hydroxy-2-[2,6-dihydroxy-4-[[[[3beta-[(4-hydroxybenzoyl)amino]hexahydrooxepin]-4alpha-yl]oxy]carbonyl]benzoyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL306373; BDBM50055669
Click to Show/Hide
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||||
| Activity |
IC50 ~ 150000 nM
|
[6] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid (1R,2S)-2-(4-hydroxy-benzoylamino)-cycloheptyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL302998; BDBM50285236
Click to Show/Hide
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||||
| Activity |
IC50 ~ 150000 nM
|
[23] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid (3S,4S)-3-(4-hydroxy-benzoylamino)-azepan-4-yl ester
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL77970; (+)-Balanol; BDBM50055671
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||||
| Activity |
IC50 ~ 150000 nM
|
[6] | |||
| Compound Name |
2-[2,6-Dihydroxy-4-[(1R,2R)-2-[(4-hydroxybenzoyl)amino]cycloheptyl]oxycarbonylbenzoyl]-3-hydroxybenzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL304549; BDBM3150; SCHEMBL9396305
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 150000 nM
|
[24] | |||
| Compound Name |
4-(2-Carboxy-6-hydroxy-benzoyl)-3,5-dihydroxy-benzoic acid (1R,2R)-2-(4-hydroxy-benzoylamino)-4-methoxycarbonyl-cyclopentyl ester
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL77399; BDBM50055683
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||||
| Activity |
IC50 ~ 150000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61. | ||||
| REF 2 | (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H... J Med Chem. 1996 Jul 5;39(14):2664-71. | ||||
| REF 3 | Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8. | ||||
| REF 4 | 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 5 | Identification of a selective inhibitor of transforming growth factor -activated kinase 1 by biosensor-based screening of focused libraries. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1031-1036. | ||||
| REF 6 | Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety. J Med Chem. 1997 Jan 17;40(2):226-35. | ||||
| REF 7 | Novel PKC inhibitory analogs of balanol with replacement of the ester functionality. Bioorg Med Chem Lett. 1995 Sep 7;5(17):2015-20. | ||||
| REF 8 | Synthesis and biological evaluation of conformationally constrained bicyclic and tricyclic balanol analogues as inhibitors of protein kinase C. Bioorg Med Chem Lett. 1995 Oct 5;5(19):2211-6. | ||||
| REF 9 | The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6223-7. | ||||
| REF 10 | Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors. J Med Chem. 2008 Oct 9;51(19):5958-63. | ||||
| REF 11 | 4-benzimidazolyl-3-phenylbutanoic acids as novel PIF-pocket-targeting allosteric inhibitors of protein kinase PKC. J Med Chem. 2011 Oct 13;54(19):6714-23. | ||||
| REF 12 | US patent application no. 8889672B2, Compounds, formulations, and methods of protein kinase C inhibition | ||||
| REF 13 | Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases. Bioorg Med Chem. 2013 Sep 15;21(18):5707-24. | ||||
| REF 14 | Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. Bioorg Med Chem Lett. 2003 Jun 2;13(11):1857-9. | ||||
| REF 15 | C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5799-802. | ||||
| REF 16 | 5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity. Bioorg Med Chem. 2009 Dec 1;17(23):7933-48. | ||||
| REF 17 | Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6575-7. | ||||
| REF 18 | C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5423-5. | ||||
| REF 19 | 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4420-3. | ||||
| REF 20 | Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3623-6. | ||||
| REF 21 | First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5829-32. | ||||
| REF 22 | Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1965-8. | ||||
| REF 23 | Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanol. Bioorg Med Chem Lett. 1995 Sep 21;5(18):2147-50. | ||||
| REF 24 | Ring size effect in the PKC inhibitory activities of perhydroazepine analogs of balanol. Bioorg Med Chem Lett. 1995 Sep 21;5(18):2151-4. | ||||
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