Target Poor or Non Binder(s) Information

Target General Information

Target ID

T60631

Target Info

Target Name

Proto-oncogene c-Ret (RET)

Synonyms

RET51; RET receptor tyrosine kinase; RET mutant Y791F; RET mutant V804M; RET mutant V804L; RET mutant S891A; RET mutant M918T; RET mutant G691S; Proto-oncogene tyrosine-protein kinase receptor Ret; PTC; Cadherin family member 12; CDHR16; CDHF12; C-ret

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Target Type

Successful Target

Gene Name

RET

Biochemical Class

Kinase

UniProt ID

P07949

Poor Binders of This Target (in total, 40 binders)

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Compound Name

Flavonoid derivative 4

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Patented

Compound Info

Synonyms

PMID26394986-Compound-48

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Activity

IC50 = 78100 nM

[1]

Compound Name

Chembl4237913

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Investigative

Compound Info

Synonyms

Maybridge4_001303; Oprea1_002513; HMS1524L05; BDBM50462225; CCG-43114; MCULE-1847675099; IDI1_031885; SR-01000633061-1; BRD-A52235082-001-01-5

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Activity

IC50 = 54000 nM

[1]

Compound Name

N-[(1R,2R,4R)-2-Bicyclo[2.2.1]heptanyl]-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL1807517; BDBM50349134

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Activity

IC50 = 55000 nM

[2]

Compound Name

4-Methoxy-N-[3-[[[1-(2-phenylethyl)pyrazolo[3,4-d]pyrimidin-4-yl]amino]methyl]phenyl]benzenesulfonamide

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Investigative

Compound Info

Synonyms

CHEMBL3128224; BDBM50448814

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Activity

IC50 = 57200 nM

[3]

Compound Name

1-Phenyl-N-[3-[[[1-(2-phenylethyl)pyrazolo[3,4-d]pyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide

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Investigative

Compound Info

Synonyms

CHEMBL3128226; BDBM50448813

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Activity

IC50 = 58600 nM

[3]

Compound Name

(E)-5-Amino-3-(4-methoxybenzylidene)indolin-2-one

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Investigative

Compound Info

Synonyms

CHEMBL608424; SCHEMBL21879083; BDBM50307135

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Activity

IC50 = 63000 nM

[4]

Compound Name

2-(((2-Aminophenyl)thio)methyl)quinazolin-4(3H)-one

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Investigative

Compound Info

Synonyms

CHEMBL4239930; Maybridge3_001034; Oprea1_252892; HMS1433O22; ZINC138179; BDBM50462220; CCG-40813; AKOS009318065; MCULE-8016017684; IDI1_012421; SR-01000022288; SR-01000022288-1; SR-01000022288-2; F2551-0038

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Activity

IC50 = 63800 nM

[1]

Compound Name

(E)-5-Amino-3-(5-bromo-furan-2-ylmethylene)-1,3-dihydro-indol-2-one

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Investigative

Compound Info

Synonyms

CHEMBL597176; BDBM50307133

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Activity

IC50 = 66000 nM

[4]

Compound Name

(3Z)-5-Methyl-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihydro-1H-indol-2-one

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Investigative

Compound Info

Synonyms

Indolinone based inhibitor, 1b; CHEMBL233373; SCHEMBL5727973; BDBM17017

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Activity

IC50 = 66000 nM

[4]

Compound Name

6-(4-Fluorophenyl)-4-(4-methylbenzyl)-3(2H)-pyridazinone

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Investigative

Compound Info

Synonyms

CHEMBL1488812; Cyto4B8; Oprea1_657781; MLS000850208; HMS2800L15; BDBM50462224; ZINC13657766; CCG-240306; MCULE-9171940002; SMR000456226

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Activity

IC50 = 66200 nM

[1]

Compound Name

N-(3-Chlorophenyl)-2-(4-imidazo[1,2-a]pyridin-6-ylphenyl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL3329394; BDBM50027466

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Activity

IC50 = 67800 nM

[5]

Compound Name

7-Ethoxy-5-hydroxy-2-phenyl-4H-chromen-4-one

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Investigative

Compound Info

Synonyms

5-Hydroxy-7-ethoxyflavone; CHEMBL172517; Maybridge3_003263; Oprea1_149189; Oprea1_185817; ZINC43094; HMS1440E07; BDBM50462230; EiM07-29928; STK089925; AKOS000574439; CCG-250449; MCULE-1005925021; IDI1_014650; NCGC00276704-01; AB01277137-01; SR-01000402579; SR-01000402579-1

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Activity

IC50 = 68400 nM

[1]

Compound Name

(E)-5-Nitro-3-(5-thiophen-3-yl-furan-2-ylmethylene)-1,3-dihydro-indol-2-one

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Investigative

Compound Info

Synonyms

CHEMBL603491; BDBM50307138

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Activity

IC50 = 78000 nM

[4]

Compound Name

3,3-Dimethyl-5-oxo-5-[(3-phenyl-1H-pyrazol-5-yl)amino]pentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL1704021; Maybridge3_002761; Oprea1_838653; MLS000850403; HMS1438N11; HMS2811J09; ZINC155679; BDBM50462226; CCG-49781; MCULE-6349782201; IDI1_014148; SMR000456421; SR-01000639212-1

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Activity

IC50 = 82600 nM

[1]

Compound Name

N-(3-Bromophenyl)-2-(4-imidazo[1,2-a]pyridin-6-ylphenyl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL3329391; BDBM50027469

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Activity

IC50 ~ 100000 nM

[5]

Compound Name

3-(6-Fluoro-1H-benzimidazol-2-yl)-5-pyridin-3-yl-2H-pyrazolo[3,4-b]pyridine

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Investigative

Compound Info

Synonyms

CHEMBL1808239; SCHEMBL4036114; SCHEMBL13797841; BDBM50349167

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Activity

IC50 = 100000 nM

[2]

Compound Name

2-(5-Isoquinolin-4-yl-1H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzoimidazole-4-carboxylic acid

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Investigative

Compound Info

Synonyms

CHEMBL249501; SCHEMBL4033912; BDBM50214109; 2-(5-(isoquinolin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzo[d]imidazole-4-carboxylic acid; 2-(5-isoquinolin-4-yl-1,2-dihydropyrazolo[3,4-b]pyridin-3-ylidene)benzimidazole-4-carboxylic acid

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

N-Methyl(5-(3-(5-(trifluoromethoxy)-1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)methanamine

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Investigative

Compound Info

Synonyms

CHEMBL400906; SCHEMBL4034563; BDBM50214117

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

4-(3-(4-(Isopropoxymethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)isoquinoline

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Investigative

Compound Info

Synonyms

CHEMBL249094; SCHEMBL4038351; BDBM50214106

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

N-[2-(Dimethylamino)ethyl]-2-(5-isoquinolin-4-yl-2H-pyrazolo[3,4-b]pyridin-3-yl)-N-methyl-3H-benzimidazole-5-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL1807518; BDBM50349135

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Activity

IC50 = 100000 nM

[2]

Compound Name

3-(4-(Dimethylamino)benzylidene)-1,3-dihydro-2H-indol-2-one

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Investigative

Compound Info

Synonyms

SU 4312; SU-4312; NSC86429; NSC 86429; CHEMBL328710; 3-[[4-(dimethylamino)phenyl]methylene]-1,3-dihydro-2H-indol-2-one; SU4312; SR-01000076222; BiomolKI_000054; BiomolKI2_000060; UPCMLD-DP118; cis-SU 4312; Lopac0_001121; BMK1-F6; BSPBio_000998; SCHEMBL1982207; UPCMLD-DP118:001; UPCMLD-DP118:002; BDBM17747; HMS1362B19; HMS1792B19; HMS1990B19; HMS3263B03; HMS3403B19; HMS3412D03; HMS3676D03; BCP20743; Tox21_501121; NSC-86429; STK946565; ZINC12339625; AKOS005640946; CCG-100658; LP01121; SDCCGSBI-0051089.P002; SU4312(NSC86429); IDI1_002094; NCGC00025170-02; NCGC00025170-03; NCGC00025170-04; NCGC00025170-05; NCGC00025170-06; NCGC00025170-07; NCGC00025170-08; NCGC00025170-09; NCGC00025170-10; NCGC00025170-11; NCGC00025170-12; NCGC00025170-14; NCGC00261806-01; B6746; EU-0101121; EC-000.2453; S 8567; (Z)-3-(4-(dimethylamino)benzylidene)indolin-2-one; SR-01000076222-1; SR-01000076222-3; BRD-K20287671-001-01-0; (3Z)-3-[(4-dimethylaminophenyl)methylene]indolin-2-one; DMBI; (Z)-3-(4-(dimethylamino)benzylidene)indolin-2-one; (3Z)-3-[[4-(dimethylamino)phenyl]methylidene]-1H-indol-2-one; (3Z)-3-[4-(dimethylamino)benzylidene]-1,3-dihydro-2H-indol-2-one; (3Z)-3-{[4-(dimethylamino)phenyl]methylidene}-2,3-dihydro-1H-indol-2-one; SU-4312; SU4312. DMBI; NSC 86429; NSC-86429; NSC86429

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Activity

IC50 ~ 100000 nM

[4]

Compound Name

3-(4-(Methoxymethyl)-1H-benzo[d]imidazol-2-yl)-5-(pyrimidin-5-yl)-1H-pyrazolo[3,4-b]pyridine

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Investigative

Compound Info

Synonyms

CHEMBL249302; SCHEMBL4039269; BDBM50214112

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

(2-(5-(Isoquinolin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzo[d]imidazol-4-yl)methanol

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Investigative

Compound Info

Synonyms

CHEMBL248890; SCHEMBL4037729; BDBM50214102; [2-(5-isoquinolin-4-yl-1H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzoimidazol-4-yl]-methanol; [2-(5-isoquinolin-4-yl-1,2-dihydropyrazolo[3,4-b]pyridin-3-ylidene)benzimidazol-4-yl]methanol

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

N-(2-Fluorophenyl)-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL377048; SCHEMBL3779801; BDBM50191932; (2-Fluorophenyl)-[4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-pyrimidin-2-yl]-amine

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Activity

IC50 = 100000 nM

[2]

Compound Name

N-((2-(5-(Isoquinolin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzo[d]imidazol-4-yl)methyl)propan-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL401064; SCHEMBL4035762; BDBM50214098

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

5-[(1E)-{[3-(Dimethylamino)propoxy]imino}methyl]-6-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]pyrimidin-4-amine

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Investigative

Compound Info

Synonyms

oxime analog 24; CHEMBL220444; SCHEMBL12303469; BDBM12335

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Activity

IC50 = 100000 nM

[2]

Compound Name

(Z)-4-Methyl-3-(4-morpholinobenzylidene)indolin-2-one

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Investigative

Compound Info

Synonyms

CHEMBL90277; BDBM50065312; 4-Methyl-3-(4-morpholin-4-yl-benzylidene)-1,3-dihydro-indol-2-one; 4-Methyl-3-[1-(4-morpholin-4-yl-phenyl)-meth-(Z)-ylidene]-1,3-dihydro-indol-2-one

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Activity

IC50 = 100000 nM

[4]

Compound Name

4-(3-(4-(Methoxymethyl)-1H-benzo[d]imidazol-2-yl)-1-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)isoquinoline

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Investigative

Compound Info

Synonyms

CHEMBL251740; SCHEMBL4035835; BDBM50214101

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

(2,4-Dichlorophenyl)-[4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-pyrimidin-2-yl]-amine

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Investigative

Compound Info

Synonyms

CHEMBL1807520; SCHEMBL3774014; BDBM50349137; N-(2,4-dichlorophenyl)-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine

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Activity

IC50 = 100000 nM

[2]

Compound Name

2-(4-Imidazo[1,2-a]pyridin-6-ylphenyl)-N-(3-methylphenyl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL3329392; BDBM50027468

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Activity

IC50 ~ 100000 nM

[5]

Compound Name

3-(3-(4-(Methoxymethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)quinoline

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Investigative

Compound Info

Synonyms

CHEMBL249095; SCHEMBL4037124; BDBM50214103

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

N-(3-Fluorophenyl)-2-(4-imidazo[1,2-a]pyridin-6-ylphenyl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL3329393; BDBM50027467

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Activity

IC50 ~ 100000 nM

[5]

Compound Name

N-(Cyclohexylmethyl)-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL213207; Kinome_254; SCHEMBL3779871; BDBM50191930; Cyclohexylmethyl-[4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-pyrimidin-2-yl]-amine

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-[(1E)-(Methoxyimino)methyl]-6-[(2-methyl-1H-indol-5-yl)oxy]pyrimidin-4-amine

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Investigative

Compound Info

Synonyms

oxime analog 9; CHEMBL223486; SCHEMBL12303449; BDBM12320

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Activity

IC50 = 100000 nM

[2]

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

[7]

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

[7]

Compound Name

N-(4-Methoxycyclohexyl)-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL1807519; SCHEMBL13007978; BDBM50349136

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Activity

IC50 = 100000 nM

[2]

Compound Name

2-(5-Isoquinolin-4-yl-1H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzoimidazole-4-carboxylic acid methyl ester

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Investigative

Compound Info

Synonyms

CHEMBL399042; SCHEMBL4037517; BDBM50214104; methyl 2-(5-(isoquinolin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzo[d]imidazole-4-carboxylate

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Activity

IC50 ~ 100000 nM

[6]

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

[7]

Compound Name

3-(4-(Methoxymethyl)-1H-benzo[d]imidazol-2-yl)-5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridine

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Investigative

Compound Info

Synonyms

CHEMBL249096; SCHEMBL4035751; BDBM50214105

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Activity

IC50 ~ 100000 nM

[6]

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References

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REF 1

Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. Eur J Med Chem. 2018 Apr 25;150:491-505.

REF 2

Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4490-7.

REF 3

Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies. J Med Chem. 2014 Feb 27;57(4):1225-35.

REF 4

Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.

REF 5

Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation. Eur J Med Chem. 2014 Oct 30;86:714-23.

REF 6

Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4297-302.

REF 7

eCF309: a potent, selective and cell-permeable mTOR inhibitor. Medchemcomm. 2016;7:471-7.

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