Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T15068 | Target Info | |||
| Target Name | Focal adhesion kinase 1 (FAK) | ||||
| Synonyms |
pp125FAK; p125FAK; Protein-tyrosine kinase 2; Protein phosphatase 1 regulatory subunit 71; PPP1R71; Focal adhesion kinase-related nonkinase; FRNK; FAK1; FADK 1; FADK
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| Target Type | Clinical trial Target | ||||
| Gene Name | PTK2 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 33 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 |
JNJ-10198409
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Investigative | Compound Info | ||
| Synonyms |
JNJ-10198409; 627518-40-5; PDGFR Tyrosine Kinase Inhibitor IV; PDGF Receptor Tyrosine Kinase Inhibitor IV; CHEMBL120077; N-(3-fluorophenyl)-6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-amine; 3-Fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine; ZDNURMVOKAERHZ-UHFFFAOYSA-N; SCHEMBL3088170; GTPL6020; CTK8E8807; jnj10198409; DTXSID70430890; MolPort-009-019-131; HMS3650O03; HMS3229I11; ZINC13677843; BDBM50179207; AKOS030525202; RWJ 540973; CCG-206773; NCGC00343986-02; RT-014973; KB-274227; SR-01000946814
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| 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
|
[3] | |||
| Compound Name |
N-{5-[(3,4-Difluorophenyl)methyl]-1,3-thiazol-2-yl}-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3125863; BDBM50449315; ZINC12913829; AKOS034027971; MCULE-9320206927; Z278071350
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
3-[(E)-2-(4-Chlorophenyl)ethenyl]-N-[(2R)-2,3-dihydroxypropyl]-4-methoxybenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1949788; SCHEMBL12134179; BDBM50364832; CH-4932748
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| 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
|
[6] | |||
| Compound Name |
3-[(E)-2-(4-Chlorophenyl)ethenyl]-N-[(2S)-2,3-dihydroxypropyl]-4-methoxybenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1949789; SCHEMBL12134185; BDBM50364833; CH-4932750
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
3-(N-Methyl-1H-indol-3-yl)-4-(3,4,5-trimethoxyphenyl)-1,5-dihydro-2H-pyrrole-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL509435; SCHEMBL13961125; BDBM50243980; 4-(1-methylindol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-one
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| Activity |
IC50 = 50000 nM
|
[7] | |||
| Compound Name |
2-{[(5-{[(Oxolan-2-yl)methyl]amino}-1,3,4-thiadiazol-2-yl)sulfanyl]methyl}-6-phenyl-3H,4H-thieno[2,3-d]pyrimidin-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3125862; BDBM50449314; AKOS033393124; MCULE-1152611879; Z151832316
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
N-[2-[[4-Methyl-6-(3,4,5-trimethoxyanilino)-1,3,5-triazin-2-yl]amino]phenyl]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2409601; BDBM50438037
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| Activity |
IC50 = 50800 nM
|
[8] | |||
| Compound Name |
1,1-Dimethyl-3-[2-[[4-methyl-6-(3,4,5-trimethoxyanilino)-1,3,5-triazin-2-yl]amino]phenyl]urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2409603; BDBM50438035
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| Activity |
IC50 = 54300 nM
|
[8] | |||
| Compound Name |
N-[3-[[4-Chloro-6-(3,4,5-trimethoxyanilino)-1,3,5-triazin-2-yl]amino]phenyl]methanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2409597; BDBM50438041
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| Activity |
IC50 = 57800 nM
|
[8] | |||
| Compound Name |
4-(1-Methylbenzimidazol-2-yl)-N-(4-methylphenyl)pyrimidin-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2036726; BDBM50385172
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| Activity |
IC50 = 58000 nM
|
[9] | |||
| Compound Name |
N-[2-[[4-(Methylamino)-6-(3,4,5-trimethoxyanilino)-1,3,5-triazin-2-yl]amino]phenyl]methanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2409596; BDBM50438042
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| Activity |
IC50 = 65900 nM
|
[8] | |||
| Compound Name |
N-(4-Chlorophenyl)-4-(1-methylbenzimidazol-2-yl)pyrimidin-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2036727; BDBM50385173
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| Activity |
IC50 = 69000 nM
|
[9] | |||
| Compound Name |
1,3-Dimethyl-7-(1-methylbenzimidazol-2-yl)pyrido[2,3-d]pyrimidine-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2036871; BDBM50385180
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| Activity |
IC50 = 92000 nM
|
[9] | |||
| 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
|
[10] | |||
| Compound Name |
Calicoferol C
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL515982; BDBM50358249
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| Activity |
IC50 ~ 100000 nM
|
[10] | |||
| Compound Name |
Calicoferol B
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL464351; BDBM50358250
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| Activity |
IC50 ~ 100000 nM
|
[10] | |||
| Compound Name |
N-(4-Ethoxyphenyl)-4-(1-methylbenzimidazol-2-yl)pyrimidin-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2036867; BDBM50385176
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
5-(1H-Indol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1H-pyrazin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3358966
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| Activity |
IC50 ~ 100000 nM
|
[11] | |||
| Compound Name |
Norlichexanthone
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Investigative | Compound Info | ||
| Synonyms |
1,3,6-Trihydroxy-8-methyl-9H-xanthen-9-one; 9H-xanthen-9-one, 1,3,6-trihydroxy-8-methyl-; CHEMBL466154; 1,3,6-trihydroxy-8-methylxanthen-9-one; 1,3,6-trihydroxy-8-methyl-xanthen-9-one; 3,6,8-Trihydroxy-1-methylxanthone; Fusarindin; AC1NQYTV; Xanthen-9-one, 1,3,6-trihydroxy-8-methyl-; C10087; ACon0_000599; ACon1_001113; CTK4E4931; DTXSID20174777; 1,3,6-trihydroxy-8-methylxanthone; ZINC5765089; BDBM50350423; AKOS000365318; MCULE-8777096541; NCGC00169665-01; W2650; 1,3,6-Trihydroxy-8-methyl-9H-xanthen-9-one #; BRD-K97951054-001-01-6; Q27107546; NCGC00169665-03!1,3,6-trihydroxy-8-methylxanthen-9-one
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| Activity |
IC50 ~ 100000 nM
|
[12] | |||
| Compound Name |
N-(5-(6,7-Dimethoxyquinolin-4-yloxy)pyridin-2-yl)-4-(4-methylpiperazin-1-yl)-2-oxo-1-phenyl-1,2-dihydropyridine-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL570643; SCHEMBL197926; BDBM50301360
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| Activity |
IC50 ~ 125000 nM
|
[13] | |||
| Compound Name |
N-(5-(6,7-Dimethoxyquinolin-4-yloxy)pyridin-2-yl)-2-oxo-1-phenyl-5-(thiophen-2-yl)-1,2-dihydropyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL570380; SCHEMBL200905; BDBM50301364
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| Activity |
IC50 ~ 125000 nM
|
[13] | |||
| Compound Name |
N-(5-(6,7-Dimethoxyquinolin-4-yloxy)pyridin-2-yl)-4-(dimethylamino)-2-oxo-1-phenyl-1,2-dihydropyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL572237; SCHEMBL197710; BDBM50301357
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| Activity |
IC50 ~ 125000 nM
|
[13] | |||
| Compound Name |
N-(5-(6,7-Dimethoxyquinolin-4-yloxy)pyridin-2-yl)-2-oxo-1-phenyl-5-(pyridin-3-yl)-1,2-dihydropyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL570365; SCHEMBL198023; BDBM50301365
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| Activity |
IC50 ~ 125000 nM
|
[13] | |||
| Compound Name |
N-(5-(7-Methoxyquinolin-4-yloxy)pyridin-2-yl)-2-oxo-1-phenyl-5-(pyrazin-2-yl)-1,2-dihydropyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL570189; SCHEMBL200771; BDBM50301368; N-[5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]-2-oxo-1-phenyl-5-pyrazin-2-ylpyridine-3-carboxamide
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| Activity |
IC50 ~ 125000 nM
|
[13] | |||
| Compound Name |
4-(2-Methoxyethylamino)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-2-oxo-1-phenyl-1,2-dihydropyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL570955; SCHEMBL198807; BDBM50301362
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| Activity |
IC50 ~ 125000 nM
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[13] | |||
| Compound Name |
N-(5-(7-Methoxyquinolin-4-yloxy)pyridin-2-yl)-2-oxo-1-phenyl-5-(pyridin-3-yl)-1,2-dihydropyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL570381; SCHEMBL198261; BDBM50301367; N-[5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]-2-oxo-1-phenyl-5-pyridin-3-ylpyridine-3-carboxamide
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| Activity |
IC50 ~ 125000 nM
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[13] | |||
| Compound Name |
1-Benzyl-N-(5-(6,7-dimethoxyquinolin-4-yloxy)pyridin-2-yl)-4-(methylamino)-2-oxo-1,2-dihydropyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL570706; SCHEMBL199896; BDBM50301363
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| Activity |
IC50 ~ 125000 nM
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[13] | |||
| Compound Name |
N-[2-[[4-(Trifluoromethyl)-6-(3,4,5-trimethoxyanilino)-1,3,5-triazin-2-yl]amino]phenyl]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2409604; BDBM50438034
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| Activity |
IC50 = 125600 nM
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[8] | |||
| Compound Name |
3,5-Dihydro[1,2,4]triazino[3,4-C][1,4]benzoxazin-2(1h)-One
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1968515; (1,2,4)Triazino(3,4-c)(1,4)benzoxazin-2(1H)-one, 3,5-dihydro-; 3,5-Dihydro-(1,2,4)triazino(3,4-c)(1,4)benzoxazin-2(1H)-one; Kinome_3625; 3,5-dihydro-1H-[1,2,4]triazino[3,4-c][1,4]benzoxazin-2-one; SCHEMBL15798857; DTXSID60161121; BDBM50049435; ZINC19926414; Q27453440
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| Activity |
IC50 = 156000 nM
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[14] | |||
| 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 |
IC50 = 194000 nM
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[15] | |||
| 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 | (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad ant... J Med Chem. 2005 Dec 29;48(26):8163-73. | ||||
| REF 3 | 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 4 | Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1523-7. | ||||
| REF 5 | Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation. Bioorg Med Chem. 2012 Feb 15;20(4):1442-60. | ||||
| REF 6 | 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 7 | Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. J Med Chem. 2008 Jul 10;51(13):3814-24. | ||||
| REF 8 | Synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4552-6. | ||||
| REF 9 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. Eur J Med Chem. 2012 Jul;53:254-63. | ||||
| REF 10 | 9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp. Bioorg Med Chem. 2011 Nov 15;19(22):6873-80. | ||||
| REF 11 | Optimization of potent DFG-in inhibitors of platelet derived growth factor receptor (PDGF-R) guided by water thermodynamics. J Med Chem. 2015 Jan 8;58(1):170-82. | ||||
| REF 12 | Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp. Bioorg Med Chem. 2011 Aug 1;19(15):4644-51. | ||||
| REF 13 | Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4924-8. | ||||
| REF 14 | Discovery of selective and orally bioavailable protein kinase C (PKC) inhibitors from a fragment hit. J Med Chem. 2015 Jan 8;58(1):222-36. | ||||
| REF 15 | 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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