Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T31406 | Target Info | |||
| Target Name | Hematopoietic cell kinase (HCK) | ||||
| Synonyms |
p61Hck; p59Hck; p59-HCK/p60-HCK; Tyrosine-protein kinase HCK; Hemopoietic cell kinase
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| Target Type | Patented-recorded Target | ||||
| Gene Name | HCK | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 26 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
ABT-869
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Phase 3 | Compound Info | ||
| Synonyms |
Linifanib; ABT 869; S1003_Selleck; AL-39324; RG-3635; ABT869, Linifanib, AL-39324, RG3635; N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N1-(2-fluoro-5-methylphenyl)urea; N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
N-(4-(4-Amino-7-(3-(4-phenylpiperazin-1-yl)prop-1-enyl)thieno[3,2-c]pyridin-3-yl)-2-methoxyphenyl)-1-methyl-1H-indole-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL233540; SCHEMBL3527755; SCHEMBL3527761; BDBM50202756
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
1-(4-Amino-3-(3-methoxy-4-(1-methyl-1H-indole-2-carboxamido)phenyl)thieno[3,2-c]pyridin-7-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL413486; SCHEMBL3527270; BDBM50202752
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Methyl 4-(6-(4-(methoxycarbonylamino)phenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
WYE-354; WYE 354; pyrazolo pyrimidine, 19; cc-506; MLS006011008; SCHEMBL300431; CHEMBL561708; GTPL9361; WYE354; BDBM35587; DTXSID00657912; C24H29N7O5; HMS3654N09; BCP02898; ZINC43013490; CCG-264882; CS-0183; SB19260; NCGC00242484-01; NCGC00242484-02; NCGC00242484-09; AC-28454; AS-55957; HY-12034; SMR004702806; BCP0726000260; DB-059456; FT-0675866; S1266; SW219671-1; X7422; W-5702; J-001552; J-514253; BRD-K77008974-001-01-6; Q27166532; mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5
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| Activity |
IC50 ~ 50000 nM
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[3] | |||
| Compound Name |
Methyl 4-(6-(4-aminophenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1095626; SCHEMBL3984085; BDBM50316252; methyl 4-[6-(4-aminophenyl)-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
Methyl 2-oxo-2-[[3-[5-(3-phenoxyprop-1-ynyl)thiophen-3-yl]-1,4-dihydroindeno[1,2-c]pyrazol-5-yl]amino]acetate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL246166; BDBM50209148
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| Activity |
IC50 ~ 50000 nM
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[5] | |||
| Compound Name |
2-((4-Amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one
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Investigative | Compound Info | ||
| Synonyms |
PIK-294; PIK294; PIK 294; C28H23N7O2; cc-610; MLS006010993; SCHEMBL1952680; CHEMBL1241767; BDBM36411; AOB6611; DTXSID20648004; SYN1098; HMS3244E13; HMS3244E14; HMS3244F13; HMS3655P12; BCP01970; EX-A2568; s2227; ZINC62260316; AKOS026750411; CCG-269607; CS-3528; CID24905149; NCGC00346614-01; NCGC00346614-02; NCGC00346614-07; AC-32796; AK176035; AS-16244; HY-10303; QC-11467; SMR004702793; PIK-294, >=98% (HPLC); FT-0699808; SW220212-1; X7436; Z-3176; J-505227
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
cis-N-(4-(4-Amino-7-(3-(diethylamino)prop-1-enyl)thieno[3,2-c]pyridin-3-yl)-2-methoxyphenyl)-1-methyl-1H-indole-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL391247; SCHEMBL3532539; BDBM50202750
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-(4-(4-Amino-7-(1-methylpiperazine-4-carbonyl)thieno[3,2-c]pyridin-3-yl)-2-methoxyphenyl)-1-methyl-1H-indole-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL232335; BDBM50202749
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
3-[4-(3-Amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-1-(3-chlorophenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
Aminobenzoisoxazole, 51; SCHEMBL420822; CHEMBL269884; BDBM21105; 1-[4-(3-amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-3-(3-chlorophenyl)urea
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
N-(4-(4,7-Diaminothieno[3,2-c]pyridin-3-yl)-2-methoxyphenyl)-1-methyl-1H-indole-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL233965; N-[4-(4,7-diaminothieno[3,2-c]pyridin-3-yl)-2-methoxyphenyl]-1-methyl-1H-indole-2-carboxamide; SCHEMBL3527019; BDBM50202743; N-[4-(4,7-diaminothieno[3,2-c]pyridin-3-yl)-2-methoxyphenyl]-1-methylindole-2-carboxamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
2-(2-Methoxy-ethoxy)-N-{3-[5-(3-phenoxy-prop-1-ynyl)-thiophen-3-yl]-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl}-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL245968; BDBM50209144
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| Activity |
IC50 ~ 50000 nM
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[5] | |||
| Compound Name |
2-(4-Methyl-piperazin-1-yl)-N-{3-[5-(3-phenoxy-prop-1-ynyl)-thiophen-3-yl]-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl}-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL245377; SCHEMBL4820003; BDBM50209158
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
Tert-Butyl 4-(6-(4-aminophenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1095627; SCHEMBL3991434; BDBM50316253
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| 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 ~ 50000 nM
|
[7] | |||
| Compound Name |
7-((1H-1,2,4-Triazol-1-yl)methyl)-3-(5-(3-(2-methoxyethoxy)-prop-1-ynyl)thiophen-3-yl)-1,4-dihydroindeno[1,2-c]pyrazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL223971; SCHEMBL17004664; BDBM50210271
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| Compound Name |
3-[4-(3-Amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-1-[3-(trifluoromethyl)phenyl]urea
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Investigative | Compound Info | ||
| Synonyms |
Aminobenzoisoxazole, 50; SCHEMBL425740; CHEMBL430090; BDBM21104; 1-[4-(3-amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-3-[3-(trifluoromethyl)phenyl]urea
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
3-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)benzonitrile
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2434145; CHEMBL1241679; 3-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)benzonitrile
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| Activity |
IC50 = 50000 nM
|
[6] | |||
| Compound Name |
N-(4-(4-Amino-7-(3-hydroxypropyl)thieno[3,2-c]pyridin-3-yl)-2-methoxyphenyl)-1-methyl-1H-indole-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL391044; SCHEMBL3608291; BDBM50202755
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
3-[2-(3-Phenoxy-1-propynyl)-4-thienyl]-6-[(4-methyl-1-piperazinyl)methyl]-1,4-dihydroindeno[1,2-c]pyrazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL390156; SCHEMBL4813916; BDBM50210272
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| Compound Name |
4-Amino-3-(3-methoxy-4-(1-methyl-1H-indole-2-carboxamido)phenyl)thieno[3,2-c]pyridine-7-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL392904; SCHEMBL3526665; BDBM50202747
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Ethyl 3-oxo-3-[[3-[5-(3-phenoxyprop-1-ynyl)thiophen-3-yl]-1,4-dihydroindeno[1,2-c]pyrazol-5-yl]amino]propanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL395427; BDBM50209156
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
3-[4-(3-Amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-1-(2-fluoro-5-methylphenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
Aminobenzoisoxazole, 49; SCHEMBL419044; CHEMBL270084; BDBM21103; 1-[4-(3-amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-Methyl-3-(quinolin-6-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1242756
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| Activity |
IC50 = 100000 nM
|
[6] | |||
| Compound Name |
1-Isopropyl-3-(isoquinolin-6-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1242207
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| Activity |
IC50 = 100000 nM
|
[6] | |||
| Compound Name |
3-(H-Imidazo[1,2-a]pyridin-7-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1242665
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| Activity |
IC50 = 100000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-Aminoquinoline
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Investigative | Compound Info | ||
| Synonyms |
quinolin-2-amine; 2-Quinolinamine; Aminoquinoline; Quinolinamine; Quinoline, 2-amino-; quinolin-2-ylamine; 2-amino-quinoline; Fragment 19; UNII-GR9M8HW75Z; GR9M8HW75Z; CHEMBL61236; 2-quinolylamine; CCRIS 1677; EINECS 209-458-8; NSC 57739; NSC 58387; BRN 0113163; quinolimine; amino-quinoline; a-Aminoquinoline; 2-Quinolinylamine; 2-?Quinolinamine; quinoline-2-amine; 2-Aminoquinoline 1; PubChem5818; 2-Quinolinamine, 9CI; 2-Aminoquinoline, 97%; ACMC-1AH5U; 2-1H-QUINOLINIMINE; SCHEMBL38775; 5-22-10-00220 (Beilstein Handbook Reference); KSC223A9P; 2-imino-1,2-dihydroquinoline; SCHEMBL1146984; DTXSID2060381; BDBM14322; CTK1C3097; CTK4C1715; KS-00000FQW; HMS1719H05; ACT03947; BCP30417; NSC57739; NSC58387; ANW-32862; BBL100884; MFCD00038079; NSC-57739; NSC-58387; SBB051994; STL554678; ZINC19074717; AKOS000279069; CS-W007524; MCULE-9057285409; PS-4207; VQ10090; 2-Aminoquinoline pound>>2-Quinolinamine; NCGC00188269-01; AC-13271; AK-26798; BR-26798; SC-05494; DB-005975; fragment 2 (J. med. chem.,50,1116); A0417; AM20061864; FT-0632430; ST50409632; EN300-10204; S-1912; 22860-EP2286812A1; 22860-EP2295421A1; 22860-EP2308848A1; 22860-EP2315502A1; 22860-EP2371810A1; 22860-EP2371812A1; 580A223; A831703; AC-907/25014242; Q209310; J-400243; Z56347237
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| Activity |
EC50 > 1000000 nM
|
[9] | |||
| Compound Name |
1-[2-(Furan-2-yl)pyrrolidin-1-yl]prop-2-en-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3617729; BDBM50119571
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| Activity |
Ki > 1250000 nM
|
[10] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases. J Med Chem. 2008 Mar 13;51(5):1231-41. | ||||
| REF 2 | Discovery of thienopyridines as Src-family selective Lck inhibitors. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1167-71. | ||||
| REF 3 | ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines. J Med Chem. 2009 Aug 27;52(16):5013-6. | ||||
| REF 4 | Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent. J Med Chem. 2009 Dec 24;52(24):8010-24. | ||||
| REF 5 | Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3136-40. | ||||
| REF 6 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. | ||||
| REF 7 | 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 8 | 1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel. J Med Chem. 2007 May 3;50(9):2011-29. | ||||
| REF 9 | Identification and specificity studies of small-molecule ligands for SH3 protein domains. J Med Chem. 2004 Oct 21;47(22):5405-17. | ||||
| REF 10 | Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration. ACS Med Chem Lett. 2015 Jul 13;6(8):898-901. | ||||
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