Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T53524 | Target Info | |||
| Target Name | Platelet-derived growth factor receptor alpha (PDGFRA) | ||||
| Synonyms |
RHEPDGFRA; Platelet-derived growth factor receptor 2; Platelet-derived growth factor alpha receptor; PDGFR2; PDGFR-alpha; PDGFR-2; PDGF-R-alpha; CD140a antigen; CD140a; CD140 antigen-like family member A; Alpha-type platelet-derived growth factor receptor; Alpha platelet-derived growth factor receptor
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| Target Type | Successful Target | ||||
| Gene Name | PDGFRA | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 40 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4238023
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463459
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-[4-(3-Methyl-6-oxo-2,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-4-yl)phenyl]-3-(3-methylphenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4063976; BDBM50238287
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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
|
[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 |
4-(3-((4-Hydroxy-3-oxobenzofuran-2(3H)-ylidene)methyl)-1-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-N-(2-hydroxyethyl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1092754; SCHEMBL4385411; BDBM50314344
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| Activity |
IC50 = 50000 nM
|
[5] | |||
| Compound Name |
6-[2-[2-(Dimethylamino)ethylamino]ethylamino]-2-hexadecylbenzo[de]isoquinoline-1,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2407635; BDBM50437557
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
Chembl4246600
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463456
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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 ~ 50000 nM
|
[7] | |||
| Compound Name |
1-(2-Fluoro-5-methylphenyl)-3-[4-(3-methyl-6-oxo-2,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4076032; BDBM50238282
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Chembl4250883
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463461
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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 ~ 50000 nM
|
[8] | |||
| Compound Name |
Chembl4245985
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463455
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-Cyclohexyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4096138; BDBM50238284
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-(1,3-Benzodioxol-5-ylmethyl)-4-pyrido[2,3]thieno[2,4-d]pyrimidin-4-ylpiperazine-1-carbothioamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2390788; CHEMBL3966621
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| Activity |
IC50 ~ 50000 nM
|
[9] | |||
| Compound Name |
1-Benzyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4093186; BDBM50238292
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|
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
1-Ethyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4096971; BDBM50238291
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|
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
3-[[2-(2-Fluorophenyl)pyridin-4-yl]amino]-4-[[(1R)-1-phenylethyl]amino]cyclobut-3-ene-1,2-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL468125; 3-{[2-(2-Fluorophenyl)pyridin-4-yl]amino}-4-{[(1R)-1-phenylethyl]amino}cyclobut-3-ene-1,2-dione; SCHEMBL4371574; BDBM50259601
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| Activity |
IC50 ~ 50000 nM
|
[10] | |||
| Compound Name |
1-[4-(3-Methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]-3-propylurea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4069773; BDBM50238306
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Chembl4247042
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50463458
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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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|
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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 |
Chembl4248043
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463451
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4239846
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463450
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(6,7-Dimethoxy-9H-pyrimido[4,5-b]indol-4-yl)-N-[4-(pyrimidin-2-ylsulfamoyl)phenyl]piperazine-1-carbothioamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL456689; SCHEMBL1882426; BDBM50270611
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|
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| Activity |
IC50 ~ 50000 nM
|
[9] | |||
| Compound Name |
4-(6,7-Dimethoxyquinazolin-4-yl)-N-[4-(pyrimidin-2-ylsulfamoyl)phenyl]piperazine-1-carbothioamide
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2388315; CHEMBL3926830
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|
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| Activity |
IC50 ~ 50000 nM
|
[9] | |||
| Compound Name |
Chembl4242803
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463464
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4243810
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463460
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-Pyrido[2,3]thieno[2,4-d]pyrimidin-4-yl-N-[4-(pyrimidin-2-ylsulfamoyl)phenyl]piperazine-1-carbothioamide
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2392393; CHEMBL3924103
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| Activity |
IC50 ~ 50000 nM
|
[9] | |||
| Compound Name |
Chembl4250240
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463452
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4244068
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Investigative | Compound Info | ||
| Synonyms |
BDBM50463453
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
6-[2-[2-(Dimethylamino)ethylamino]ethylamino]-2-ethylbenzo[de]isoquinoline-1,3-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2407517; BDBM50437562
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
6-[2-[2-(Dimethylamino)ethylamino]ethylamino]-2-methylbenzo[de]isoquinoline-1,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2407516; BDBM50437563
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
2-Butyl-6-[2-[2-(dimethylamino)ethylamino]ethylamino]benzo[de]isoquinoline-1,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2407518; BDBM50437561
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
6-[2-[2-(Dimethylamino)ethylamino]ethylamino]-2-octylbenzo[de]isoquinoline-1,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL598852; BDBM50437559
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
1-(2,2-Diethoxyethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3799221; SCHEMBL18250089; BDBM50184774
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| Activity |
IC50 ~ 100000 nM
|
[11] | |||
| Compound Name |
5-[4-Amino-1-(2,2-dimethoxyethyl)pyrazolo[3,4-d]pyrimidin-3-yl]-1,3-benzoxazol-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3800138
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| Activity |
IC50 ~ 100000 nM
|
[11] | |||
| Compound Name |
5-[4-Amino-1-(1,3-dioxolan-2-ylmethyl)pyrazolo[3,4-d]pyrimidin-3-yl]-1,3-benzoxazol-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3797590
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| Activity |
IC50 ~ 100000 nM
|
[11] | |||
| 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 |
5-[4-Amino-1-(2,2-diethoxyethyl)pyrazolo[3,4-d]pyrimidin-3-yl]-1,3-benzoxazol-2-amine
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Investigative | Compound Info | ||
| Synonyms |
eCF309; eCF-309; eCF 309; GTPL9571; CHEMBL3800481; SCHEMBL22773819; BDBM200300; cid_122163152; AKOS030211008; ZINC585672921; compound 12 [Fraser et al., 2016]; J3.595.265I
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| Activity |
IC50 ~ 100000 nM
|
[11] | |||
| Compound Name |
6-[2-[2-(Dimethylamino)ethylamino]ethylamino]-2-hexylbenzo[de]isoquinoline-1,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2407519; BDBM50437560
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of novel Syk/PDGFR-alpha/c-Kit inhibitors as multi-targeting drugs to treat rheumatoid arthritis. Bioorg Med Chem. 2018 Aug 15;26(15):4375-4381. | ||||
| REF 2 | Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRalpha) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). J Med Chem. 2017 Jun 22;60(12):5099-5119. | ||||
| 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 | Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Bioorg Med Chem Lett. 2010 Apr 1;20(7):2321-5. | ||||
| REF 6 | Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs). Eur J Med Chem. 2013 Jul;65:477-86. | ||||
| 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 | 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 9 | US patent application no. 7326712B2, Substituted tricyclic compounds as protein kinase inhibitors | ||||
| REF 10 | Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem. 2009 May 1;17(9):3342-51. | ||||
| REF 11 | eCF309: a potent, selective and cell-permeable mTOR inhibitor. Medchemcomm. 2016;7:471-7. | ||||
| 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. | ||||
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