Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T84133 | Target Info | |||
| Target Name | Phosphodiesterase 10A (PDE10) | ||||
| Synonyms |
cAMP and cAMPinhibited cGMP 3',5'cyclic phosphodiesterase 10A; cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
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| Target Type | Clinical trial Target | ||||
| Gene Name | PDE10A | ||||
| Biochemical Class | Phosphoric diester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 24 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
US9388139, 12
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Patented | Compound Info | ||
| Synonyms |
SCHEMBL12493454; CHEMBL3899621; BDBM236643; US9388139, 12
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
BC11-28
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Patented | Compound Info | ||
| Synonyms |
BDBM86641; 7-(4-fluorophenyl)-N-(2-methylphenyl)-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine; AC1MM8WN; Oprea1_524381; CHEMBL2132713; SCHEMBL14998917; BDBM60812; HMS1911I05; ZINC2713985; STK859438; AKOS002104616; MCULE-7713625102; BC11-28; NCGC00138975-01; ST50069829; EU-0095146; US9173884, BC11-28; SR-01000567887; SR-01000567887-1; K405-0344; 7-(4-fluorophenyl)-N-(2-methylphenyl)-5-phenylpyrrolo[2,3-d]pyrimidin-4-amine; [7-(4-fluorophenyl)-5-phenylpyrrolo[3,2-e]pyrimidin-4-yl](2-methylphenyl)amine
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(2S)-2-[[1-(2-Chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N-(4-methoxyphenyl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3360413; BDBM50034649
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
6-(3,4-Dimethoxyphenyl)-3-(2-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine
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Investigative | Compound Info | ||
| Synonyms |
triazolothiadiazine, 21; MLS000040393; BMCL181297 Compound 5A; CHEMBL251785; cid_662965; SCHEMBL1773326; REGID_for_CID_662965; BDBM30027; HMS2427C11; ZINC4312962; STK877959; AKOS002046530; CCG-193287; MCULE-2949109211; NCGC00071837-02; NCGC00071837-03; NCGC00071837-05; SMR000043645; ST081704; SR-01000612138; SR-01000612138-3; BRD-K77507773-001-10-1
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
2-[[1-(2-Chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N-(4-methoxyphenyl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2178115; SCHEMBL16981747; BDBM50398649
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
1-(3-((1-(Quinolin-2-yl)azetidin-3-yl)oxy)pyrazin-2-yl)piperidin-4-ol
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2631007; CHEMBL3356654; BDBM98875; US8497265, 201; 1-[3-(1-quinolin-2-ylazetidin-3-yl)oxypyrazin-2-yl]piperidin-4-ol
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| Activity |
IC50 = 54000 nM
|
[6] | |||
| Compound Name |
Methyl 4-(3-((1-(quinolin-2-yl)azetidin-3-yl)oxy)pyrazin-2-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2630828; CHEMBL3356682; BDBM99031; US8497265, 671; methyl 4-[3-(1-quinolin-2-ylazetidin-3-yl)oxypyrazin-2-yl]piperidine-1-carboxylate
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| Activity |
IC50 = 64000 nM
|
[6] | |||
| Compound Name |
2-[3-[3-(2-Methylpyridin-3-yl)pyrazin-2-yl]oxyazetidin-1-yl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2631163; CHEMBL3356674; BDBM98983; US8497265, 439
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| Activity |
IC50 = 98000 nM
|
[6] | |||
| Compound Name |
N-(4-Methoxybenzyl)-3-(cyclopentyloxy)-4-(difluoromethoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3628685; BDBM50129817
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
N-(2-Chlorophenyl)-3-cyclopentyloxy-4-(difluoromethoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3883753; BDBM50208310
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
Chembl4206423
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Investigative | Compound Info | ||
| Synonyms |
BDBM50455384
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
Chembl4215772
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Investigative | Compound Info | ||
| Synonyms |
BDBM50455383
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
3-(Cyclopropylmethoxy)-4-(difluoromethoxy)-N-pyridin-3-ylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3884224; BDBM50208315
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-(Butylthio)-3-phenyl-6,7-dihydrothieno[3,2-d]pyrimidin-4(3H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3955950; SCHEMBL16200699; BDBM86643; ZINC2719706; AKOS024584760; MCULE-1273250191; BC11-38-1; EU-0022193; SR-01000120181; SR-01000120181-1; F0579-0062
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-(Propylthio)-3-(p-tolyl)-6,7-dihydrothieno[3,2-d]pyrimidin-4(3H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3950652; SCHEMBL16200731; BDBM86645; ZINC2459466; AKOS024584842; MCULE-6274932978; BC11-38-3; EU-0088907; SR-01000120189; SR-01000120189-1; F0579-0160
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
3-Phenyl-[1,3,5]triazino[2,1-b][1,3]benzothiazole-2,4-dione
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM86640; Maybridge4_000373; Oprea1_392751; CHEMBL3974407; SCHEMBL14998934; BDBM60808; HMS1522A21; ZINC134330; CCG-51916; BC11-19; MCULE-1137806289; IDI1_030955; NCGC00177650-01; US9173884, BC11-19; SR-01000641186-1; BRD-K04557143-001-01-6
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
3-Cyclopentyloxy-4-(difluoromethoxy)-N-pyridin-3-ylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3885161; BDBM50208311
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
N-(2-Chlorophenyl)-3(cyclopropylmethoxy)-4-(difluoromethoxy)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3884788; BDBM50208314
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-[3-[3-(4-Methylpiperidin-1-yl)pyrazin-2-yl]oxyazetidin-1-yl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2630911; CHEMBL3356659; BDBM98878; US8497265, 204
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| Activity |
IC50 = 103000 nM
|
[6] | |||
| Compound Name |
2-[3-[3-(4-Methylphenyl)pyrazin-2-yl]oxyazetidin-1-yl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2630951; CHEMBL3356666; BDBM98966; US8497265, 422
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|
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| Activity |
IC50 = 107000 nM
|
[6] | |||
| Compound Name |
2-[3-(3-Pyrimidin-5-ylpyrazin-2-yl)oxyazetidin-1-yl]quinoline
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2631020; CHEMBL3356673; BDBM99003; ZINC96168837; US8497265, 459
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| Activity |
IC50 = 125000 nM
|
[6] | |||
| Compound Name |
2-[3-[3-[4-(Methoxymethyl)piperidin-1-yl]pyrazin-2-yl]oxyazetidin-1-yl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2630899; CHEMBL3356657; BDBM98895; US8497265, 221
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|
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| Activity |
IC50 = 147000 nM
|
[6] | |||
| Compound Name |
2-[3-[3-(1-Methylsulfonylpiperidin-4-yl)pyrazin-2-yl]oxyazetidin-1-yl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2631032; CHEMBL3356683; BDBM99032; US8497265, 672
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| Activity |
IC50 = 166000 nM
|
[6] | |||
| Compound Name |
Click to Show/Hide
|
Compound Info | |||
| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 33 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-Amino-4-chlorobenzothiazole
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Investigative | Compound Info | ||
| Synonyms |
4-Chloro-1,3-benzothiazol-2-amine; 4-chlorobenzo[d]thiazol-2-amine; 2-Benzothiazolamine, 4-chloro-; 4-Chlorobenzothiazol-2-ylamine; 4-Chloro-2-benzothiazolamine; Benzothiazole, 2-amino-4-chloro-; MFCD00005791; 4-Chloro-benzothiazol-2-ylamine; 4-Chloro-2-aminobenzothiazole; 2-Amino-4-chloro benzothiazole; CHEMBL1413383; 2-Amino-4-chlorobenzothiazole, 97%; 4-chlorobenzothiazole-2-ylamine; SMR000323910; EINECS 243-439-5; BRN 0136784; zlchem 166; PubChem21701; ACMC-1BSB6; DSSTox_CID_4470; DSSTox_RID_77413; DSSTox_GSID_24470; 2-Amino-4-chlorobenzothiazol; 4-Chlorobenzothiazol-2-amine; 4-27-00-04859 (Beilstein Handbook Reference); KSC495E6T; MLS000678672; MLS002152865; BIDD:GT0429; SCHEMBL103727; 2-amino-4-chloro-benzothiazole; DTXSID0024470; CTK3J5269; EBD2308; ZLB0155; HMS1655D11; HMS2736G18; ACT07689; BCP28042; KS-00000LB8; ZINC8615114; Tox21_200087; ANW-23863; BBL008104; BDBM50335099; GEO-00099; SBB000250; STK133071; AKOS000298479; 4-chloranyl-1,3-benzothiazol-2-amine; AC-6245; CS-W019581; FS-1334; MCULE-4764480034; VT10047; 4-Chloro-1,3-benzothiazol-2-amine #; NCGC00091638-01; NCGC00091638-02; NCGC00257641-01; AK-26844; BR-26844; SC-50738; ST079158; SY030942; DB-027746; AM20060539; BB 0245424; FT-0611104; FT-0611105; A18406; S-2904; A814103; W-110508; Q27452897; Z57607000; F1911-0008
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| Activity |
Ki = 210000 nM
|
[10] | |||
| Compound Name |
2-(4-Methyl-1,3-thiazol-2-yl)pyridine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3745823; 4-methyl-2-pyridin-2-yl-1,3-thiazole; 4-methyl-2-(pyridin-2-yl)thiazole; SCHEMBL6840490; 2-(4'-Pyridyl)-4-methyl-thiazol; BDBM50500499; STK657869; ZINC19620728; AKOS005588587; MCULE-4280534817; NE59885
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| Activity |
IC50 = 324000 nM
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[11] | |||
| Compound Name |
N,N-Dimethyl-1-[3-(1-quinolin-2-ylazetidin-3-yl)oxypyrazin-2-yl]piperidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2631164; CHEMBL3356660; BDBM98920; US8497265, 246
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| Activity |
IC50 = 343000 nM
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[6] | |||
| Compound Name |
2-[3-(3-Pyridin-2-ylpyrazin-2-yl)oxyazetidin-1-yl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2630961; CHEMBL3356670; BDBM98961; US8497265, 416
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| Activity |
IC50 = 350000 nM
|
[6] | |||
| Compound Name |
5-(Furan-2-yl)-3-methyl-1H-pyrazole
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Investigative | Compound Info | ||
| Synonyms |
5-(2-Furyl)-3-methyl-1H-pyrazole; 3-(furan-2-yl)-5-methyl-1H-pyrazole; CHEMBL3746647; 5-Furan-2-yl-3-methyl-1H-pyrazole; EC-000.1665; SCHEMBL2736625; 3-furan-2-yl-5-methylpyrazole; ZINC79612; BBL005755; BDBM50500498; MFCD00462226; STK325840; 3-(2-Furyl)-5-methyl-1H-pyrazole; AKOS000588821; MCULE-1677776889; NCGC00323308-01; H3300; AB01318866-02
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| Activity |
IC50 = 851000 nM
|
[11] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(quinoxalin-2-yloxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
PQ-10; UNII-63643I762J; (R)-6,7-dimethoxy-4-(3-(quinoxalin-2-yloxy)pyrrolidin-1-yl)quinazoline; 63643I762J; PubChem16363; CHEMBL219445; SCHEMBL2451079; BDBM14768; ZINC14956507; Quinazoline, 6,7-dimethoxy-4-((3R)-3-(2-quinoxalinyloxy)-1-pyrrolidinyl)-; DB08391; 6,7-DIMETHOXY-4-[(3R)-3-(2-QUINOXALINYLOXY)-1-PYRROLIDINYL]QUINAZOLINE; PQ-10, >=98% (HPLC); 6,7-Dimethoxy-4-pyrrolidylquinazoline 29; 691D212; Q27097603; (R)-6,7-dimethoxy-4-[3-(quinoxalin-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 3981071.71 nM
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[12] | |||
| Compound Name |
2-[4-Fluoro-3-[7-methyl-12-(trifluoromethyl)-2,4,5,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-3-yl]phenyl]propan-2-ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3693367; SCHEMBL15471893; BDBM171961; US9085584, 103c
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| Activity |
IC50 = 7980000 nM
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[13] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(quinolin-6-yloxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL263641; BDBM14764; 6,7-Dimethoxy-4-pyrrolidylquinazoline 25; (R)-6,7-dimethoxy-4-[3-(quinolin-6-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 11748975.55 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(quinolin-7-yloxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL409613; BDBM14766; 6,7-Dimethoxy-4-pyrrolidylquinazoline 27; (R)-6,7-dimethoxy-4-[3-(quinolin-7-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 11748975.55 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3r)-3-(2-Naphthyloxy)pyrrolidin-1-Yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
6,7-dimethoxy-4-[(3R)-3-(naphthalen-2-yloxy)pyrrolidin-1-yl]quinazoline; CHEMBL410834; SCHEMBL21067602; BDBM14760; DB08389; 6,7-Dimethoxy-4-pyrrolidylquinazoline 21; Q27097601; (R)-6,7-dimethoxy-4-[3-(naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 11748975.55 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-[(7-methoxynaphthalen-2-yl)oxy]pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL218955; BDBM14763; 6,7-Dimethoxy-4-pyrrolidylquinazoline 24; (R)-6,7-dimethoxy-4-[3-(7-methoxy-naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 16982436.52 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-[(6-methoxynaphthalen-2-yl)oxy]pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL261711; BDBM14762; 6,7-Dimethoxy-4-pyrrolidylquinazoline 23; (R)-6,7-dimethoxy-4-[3-(6-methoxy-naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 17782794.1 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-[(2-methylquinolin-6-yl)oxy]pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL409651; BDBM14765; 6,7-Dimethoxy-4-pyrrolidylquinazoline 26; (R)-6,7-dimethoxy-4-[3-(2-methyl-quinolin-6-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 17782794.1 nM
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[12] | |||
| Compound Name |
4-[(3R)-3-(Isoquinolin-3-yloxy)pyrrolidin-1-yl]-6,7-dimethoxyquinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL220185; BDBM14767; 6,7-Dimethoxy-4-pyrrolidylquinazoline 28; (R)-4-[3-(isoquinolin-3-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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| Activity |
Ki = 18620871.37 nM
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[12] | |||
| Compound Name |
(R)-4-[3-(5-Chloro-pyrimidin-2-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL385754; BDBM14756; 6,7-Dimethoxy-4-pyrrolidylquinazoline 17; 4-[(3R)-3-[(5-chloropyrimidin-2-yl)oxy]pyrrolidin-1-yl]-6,7-dimethoxyquinazoline
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| Activity |
Ki = 43651583.22 nM
|
[12] | |||
| Compound Name |
4-[(3R)-3-(4-Ethoxyphenoxy)pyrrolidin-1-yl]-6,7-dimethoxyquinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL375200; BDBM14748; 6,7-Dimethoxy-4-pyrrolidylquinazoline 11; (R)-4-[3-(4-ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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| Activity |
Ki = 53703179.64 nM
|
[12] | |||
| Compound Name |
4-{[(3R)-1-(6,7-Dimethoxyquinazolin-4-yl)pyrrolidin-3-yl]oxy}benzonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL441704; BDBM14745; 6,7-Dimethoxy-4-pyrrolidylquinazoline 8; (R)-4-[1-(6,7-dimethoxy-quinazolin-4-yl)-pyrrolidin-3-yloxy]-benzonitrile
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| Activity |
Ki = 54954087.39 nM
|
[12] | |||
| Compound Name |
4-[(3R)-3-(3,4-Dimethoxyphenoxy)pyrrolidin-1-yl]-6,7-dimethoxyquinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL409862; BDBM14753; 6,7-Dimethoxy-4-pyrrolidylquinazoline 16; (R)-4-[3-(3,4-dimethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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| Activity |
Ki = 66069344.8 nM
|
[12] | |||
| Compound Name |
(R)-4-[3-(Indan-5-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL408977; BDBM14752; 6,7-Dimethoxy-4-pyrrolidylquinazoline 15; 4-[(3R)-3-(2,3-dihydro-1H-inden-5-yloxy)pyrrolidin-1-yl]-6,7-dimethoxyquinazoline
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| Activity |
Ki = 67608297.54 nM
|
[12] | |||
| Compound Name |
4-[(3R)-3-(3-Ethoxyphenoxy)pyrrolidin-1-yl]-6,7-dimethoxyquinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL219451; BDBM14751; 6,7-Dimethoxy-4-pyrrolidylquinazoline 14; (R)-4-[3-(3-ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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| Activity |
Ki = 93325430.08 nM
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[12] | |||
| Compound Name |
4-[(3R)-3-(4-Tert-butylphenoxy)pyrrolidin-1-yl]-6,7-dimethoxyquinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL387167; BDBM14747; 6,7-Dimethoxy-4-pyrrolidylquinazoline 10; (R)-4-[3-(4-tert-butyl-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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| Activity |
Ki = 100000000 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(pyridin-4-yloxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL259295; BDBM14759; 6,7-Dimethoxy-4-pyrrolidylquinazoline 20; (R)-6,7-dimethoxy-4-[3-(pyridin-4-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 109647819.6 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(pyridin-2-yloxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL260006; BDBM14757; 6,7-Dimethoxy-4-pyrrolidylquinazoline 18; (R)-6,7-dimethoxy-4-[3-(pyridin-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 120226443.5 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(pyridin-3-yloxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL374993; BDBM14758; 6,7-Dimethoxy-4-pyrrolidylquinazoline 19; (R)-6,7-dimethoxy-4-[3-(pyridin-3-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 125892541.2 nM
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[12] | |||
| Compound Name |
2-{[(3R)-1-(6,7-Dimethoxyquinazolin-4-yl)pyrrolidin-3-yl]oxy}benzonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL409484; BDBM14744; 6,7-Dimethoxy-4-pyrrolidylquinazoline 7; (R)-2-[1-(6,7-dimethoxy-quinazolin-4-yl)-pyrrolidin-3-yloxy]-benzonitrile
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| Activity |
Ki = 128824955.2 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(3-phenylphenoxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL218855; BDBM14750; 6,7-Dimethoxy-4-pyrrolidylquinazoline 13; (R)-4-[3-(biphenyl-3-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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| Activity |
Ki = 134896288.3 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(2-propan-2-ylphenoxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL429686; BDBM50373149
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| Activity |
Ki = 169824365.3 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-[2-(trifluoromethoxy)phenoxy]pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL430071; BDBM50373150
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| Activity |
Ki = 181970085.9 nM
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[12] | |||
| Compound Name |
4-[(3R)-3-(2-Chlorophenoxy)pyrrolidin-1-yl]-6,7-dimethoxyquinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL408978; BDBM14743; 6,7-Dimethoxy-4-pyrrolidylquinazoline 6; (R)-4-[3-(2-chloro-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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| Activity |
Ki = 194984460 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(naphthalen-1-yloxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL263642; BDBM14761; 6,7-Dimethoxy-4-pyrrolidylquinazoline 22; (R)-6,7-dimethoxy-4-[3-(naphthalen-1-yloxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 208929613.1 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-(2-methoxyphenoxy)pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL427777; BDBM14741; 6,7-Dimethoxy-4-pyrrolidylquinazoline 4; (R)-6,7-dimethoxy-4-[3-(2-methoxy-phenoxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 239883291.9 nM
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[12] | |||
| Compound Name |
(R)-6,7-Dimethoxy-4-(3-o-tolyloxy-pyrrolidin-1-yl)-quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL262088; BDBM14740; 6,7-Dimethoxy-4-pyrrolidylquinazoline 3; 6,7-dimethoxy-4-[(3R)-3-(2-methylphenoxy)pyrrolidin-1-yl]quinazoline
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| Activity |
Ki = 323593656.9 nM
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[12] | |||
| Compound Name |
6,7-Dimethoxy-4-[(3R)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]quinazoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL428445; BDBM14739; 6,7-Dimethoxy-4-pyrrolidylquinazoline 2; (R)-6,7-dimethoxy-4-[3-(2-trifluoromethyl-phenoxy)-pyrrolidin-1-yl]-quinazoline
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| Activity |
Ki = 794328234.7 nM
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[12] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | US patent application no. 9388139B2, Derivatives of celeboxib, use thereof and preparation thereof | ||||
| REF 2 | US patent application no. 9173884B2, Inhibitors of phosphodiesterase 11 (PDE11) | ||||
| REF 3 | Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent. J Med Chem. 2014 Dec 26;57(24):10304-13. | ||||
| REF 4 | Identification of a potent new chemotype for the selective inhibition of PDE4. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. | ||||
| REF 5 | Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design. J Med Chem. 2012 Oct 11;55(19):8549-58. | ||||
| REF 6 | Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility. Bioorg Med Chem. 2014 Dec 1;22(23):6570-6585. | ||||
| REF 7 | Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships. Bioorg Med Chem. 2015 Nov 15;23(22):7332-9. | ||||
| REF 8 | Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings. Eur J Med Chem. 2016 Nov 29;124:372-379. | ||||
| REF 9 | Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors. Bioorg Med Chem Lett. 2018 Apr 15;28(7):1188-1193. | ||||
| REF 10 | Fragment-Based Drug Discovery of Phosphodiesterase Inhibitors. J Med Chem. 2018 Feb 22;61(4):1415-1424. | ||||
| REF 11 | Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors. Bioorg Med Chem Lett. 2016 Jan 1;26(1):197-202. | ||||
| REF 12 | CoMFA and HQSAR studies on 6,7-dimethoxy-4-pyrrolidylquinazoline derivatives as phosphodiesterase10A inhibitors. Bioorg Med Chem. 2008 Apr 1;16(7):3675-86. | ||||
| REF 13 | US patent application no. 9085584B2, Substituted pyrido[3,2-E][1,2,4]-triazolo[4,3-A]pyrazines for the treatment of central nervous system disorders | ||||
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