Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T17687 | Target Info | |||
| Target Name | Fibroblast growth factor receptor (FGFR) | ||||
| Synonyms |
FGF receptor
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| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 14 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
PD158780 Analog 5h
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Investigative | Compound Info | ||
| Synonyms |
4-N-(3-bromophenyl)-6-N-[2-(dimethylamino)ethyl]pyrido[3,4-d]pyrimidine-4,6-diamine; BDBM3704; CHEMBL162034; 4-[(3-Bromophenyl)amino]-6-[[2-(dimethylamino)-ethyl]amino]pyrido[3,4-d]pyrimidine
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
PD158780 Analog 5k
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Investigative | Compound Info | ||
| Synonyms |
BDBM3707; CHEMBL433520; 4-[(3-Bromophenyl)amino]-6-[[3-(diethylamino)-2-hydroxypropyl]amino]pyrido[3,4-d]pyrimidine; 4-N-(3-bromophenyl)-6-N-[3-(diethylamino)-2-hydroxypropyl]pyrido[3,4-d]pyrimidine-4,6-diamine
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
6-(2,6-Dichlorophenyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL50977; BDBM50064347; 6-(2,6-dichlorophenyl)-8-methylpyrido[2,3-d]pyrimidin-7-one; 6-(2,6-Dichloro-phenyl)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one; 6-(2,6-Dichlorophenyl)-8-methylpyrido[2,3-d]pyrimidine-7(8H)-one
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
7-((4-Methylpiperazin-1-yl)methyl)-3-(thiophen-3-yl)-1,4-dihydroindeno[1,2-c]pyrazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL213743; BDBM50188266
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-[4-[(3-Chloro-4-fluorophenyl)amino]pyrido[3,4-d]pyrimidin-6-yl]-5-(4-methyl-1-piperazinyl)-2-pentynamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL203599; BDBM50182697; N-[4-(3-chloro-4-fluoroanilino)pyrido[3,4-d]pyrimidin-6-yl]-5-(4-methylpiperazin-1-yl)pent-2-ynamide
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
N-(3-Bromophenyl)-1H-imidazo[4,5-g]quinazolin-8-amine
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Investigative | Compound Info | ||
| Synonyms |
bpiq-ii; CHEMBL66031; Imidazoquinazoline deriv. 8; Anilinopyrimidine deriv. 7a; BDBM3570; SCHEMBL13898313; CTK0E4714; 8-[(3-Bromophenyl)amino]-1H-imidazo[4,5-g]-quinazoline; DTXSID20274367; ZINC3815028; HSCI1_000062; SC-91510; BRD-K35473459-001-01-7; N-(3-bromophenyl)-1H-imidazo[4,5-g]quinazolin-8-am; 8-[(3-Bromophenyl)amino]-1H-imidazo[4,5-g]quinazoline; 1H-Imidazo[4,5-g]quinazolin-8-amine, N-(3-bromophenyl)-
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
6-(2,6-Dichlorophenyl)-2-(dimethylamino)-8-methylpyrido[2,3-d]pyrimidin-7-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL299347; 2-aminopyrido[2,3-d]pyrimidin-7(8H)-one 28; BDBM3061; SCHEMBL5761783; 2-(Dimethylamino)-6-(2,6-dichlorophenyl)-8-methylpyrido[2,3-d]pyrimidine-7(8H)-one; 6-(2,6-dichlorophenyl)-2-(dimethylamino)-8-methyl-7H,8H-pyrido[2,3-d]pyrimidin-7-one; 6-(2,6-Dichlorophenyl)-2-dimethylamino-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
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| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
2-Aminopyrido[2,3-d]pyrimidin-7(8H)-one 19
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL51573; BDBM3052; SCHEMBL5763098; 2,8-Dimethyl-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidine-7(8H)-one; 6-(2,6-dichlorophenyl)-2,8-dimethyl-7H,8H-pyrido[2,3-d]pyrimidin-7-one
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
3-[[5-Cyano-6-(cyclopentylamino)pyrimidin-4-yl]amino]-4-methyl-N-(1,2-oxazol-3-yl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
3-{[5-cyano-6-(cyclopentylamino)pyrimidin-4-yl]amino}-4-methyl-N-(1,2-oxazol-3-yl)benzamide; CHEMBL383172; 5-Cyanopyrimidine Derivative 3b; SCHEMBL16576397; BDBM16326; 3-{[5-cyano-6-(cyclopentylamino)pyrimidin-4-yl]amino}-N-isoxazol-3-yl-4-methylbenzamide
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| Activity |
IC50 ~ 50000 nM
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[6] | |||
| Compound Name |
PD158780 Analog 5n
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Investigative | Compound Info | ||
| Synonyms |
BDBM3710; CHEMBL162622; PD-0165557; 4-[(3-Bromophenyl)amino]-6-[[2-(4-morpholino)ethyl]amino]pyrido[3,4-d]pyrimidine; 4-N-(3-bromophenyl)-6-N-[2-(morpholin-4-yl)ethyl]pyrido[3,4-d]pyrimidine-4,6-diamine
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Canertinib dihydrochloride
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Investigative | Compound Info | ||
| Synonyms |
Canertinib HCl; Canertinib (dihydrochloride); CI-1033; CI 1033; Canertinib 2HCl; UNII-ICJ93X8X90; PD183805; PD 183805; Canertinib dihydrochloride [USAN]; PD-0183805; ICJ93X8X90; MFCD09954112; 289499-45-2 (HCl); CI-1033 dihydrochloride;PD-183805 dihydrochloride; CHEMBL545315; Canertinib dihydrochloride (USAN); C24H25ClFN5O3.2ClH; Canertinib HCl; Canertinib.2HCL; Canertinib(dihydrochloride); cc-446; Canertinib dihydrochloride salt; SCHEMBL2052123; AOB6735; DTXSID80183143; HMS3295E05; BCP01902; KS-00000FV0; 3516AH; CI-103; HY-10367A; AKOS015924656; AC-2414; CS-0263; AK326128; AS-75065; SC-23744; SN-26606; A3276; AM20090674; FT-0724289; PD-0183805-002B; CI-1033, >=98% (HPLC); A19399; D03350; W-5427; Q-101362; Q-200787; Q27280663
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| Activity |
IC50 ~ 50000 nM
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[4] | |||
| Compound Name |
PD089828 analog 12
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL49658; BDBM4831; 1-{2-amino-6-[3,5-bis(trifluoromethyl)phenyl]pyrido[2,3-d]pyrimidin-7-yl}-3-tert-butylurea; N-[2-Amino-6-[3,5-bis(trifluoromethyl)phenyl]pyrido[2,3-d]pyrimidine-7-yl]-N'-tert-butylurea
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| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
9-Hydroxy-4-phenylpyrrolo[3,4-C]carbazole-1,3(2H,6H)-dione
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Investigative | Compound Info | ||
| Synonyms |
PD 407824; PD-407824; 9-HYDROXY-4-PHENYL-6H-PYRROLO[3,4-C]CARBAZOLE-1,3-DIONE; PD0407824; CHEMBL214253; PD407824; SCHEMBL6516584; CTK2C3047; DTXSID40402483; HMS3262B15; HMS3269N21; HMS3413B22; HMS3677B22; ZINC6475935; Tox21_500807; BDBM50192349; MFCD09753286; AKOS024457242; CCG-222111; DB04608; NCGC00167836-01; NCGC00167836-04; NCGC00261492-01; HY-18961; CS-0014679; FT-0673544; PD-407824, >=98% (HPLC); BRD-K82823804-001-01-7; Q27095347; 9-Hydroxy-4-phenyl-pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione; Pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione, 9-hydroxy-4-phenyl-
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| Compound Name |
4-(6,7-Dimethoxy-4-quinazolinyl)-N-(3,4-methylenedioxybenzyl)-1-piperazinethiocarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL102301; SCHEMBL2923651; KN734; BDBM50118826; KN-734; N-(1,3-benzodioxol-5-ylmethyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carbothioamide; 4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carbothioic acid (benzo[1,3]dioxol-5-ylmethyl)-amide
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| Activity |
IC50 = 160000 nM
|
[8] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(4-Cyanophenyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL106966; SCHEMBL2921461; BDBM50115297; 4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carboxylic acid (4-cyano-phenyl)-amide
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| Activity |
IC50 > 200000 nM
|
[9] | |||
| Compound Name |
4-(6,7-Dimethoxy-4-quinazolinyl)-N-(4-nitrophenyl)-1-piperazinecarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL99743; SCHEMBL842459; BDBM50115295; KN1022; 4-(6,7-dimethoxyquinazolin-4-yl)-N-(4-nitrophenyl)piperazine-1-carboxamide; 4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carboxylic acid (4-nitro-phenyl)-amide; 4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carboxylic acid (4-nitro-phenyl)-amide(KN1022)
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| Activity |
IC50 > 200000 nM
|
[9] | |||
| Compound Name |
N-Benzyl-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carbothioamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL319894; SCHEMBL2919724; BDBM50118831; N-Benzyl-4-(6,7-dimethoxyquinazoline-4-yl)piperazine-1-carbothioamide; 4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carbothioic acid benzylamide
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| Activity |
IC50 > 200000 nM
|
[8] | |||
| Compound Name |
N-(4-Bromophenyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL323336; SCHEMBL2918427; BDBM50115298; N-(4-bromophenyl)-4-(6,7-dimethoxy-4-quinazolinyl)-1-piperazinecarboxamide; 4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carboxylic acid (4-bromo-phenyl)-amide
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| Activity |
IC50 > 200000 nM
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[9] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors. J Med Chem. 1998 Feb 26;41(5):742-51. | ||||
| REF 2 | Development of a binding model to protein tyrosine kinases for substituted pyrido[2,3-d]pyrimidine inhibitors. J Med Chem. 1998 May 21;41(11):1752-63. | ||||
| REF 3 | Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4371-5. | ||||
| REF 4 | Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB... J Med Chem. 2006 Feb 23;49(4):1475-85. | ||||
| REF 5 | Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase acti... J Med Chem. 1996 Feb 16;39(4):918-28. | ||||
| REF 6 | 5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase. J Med Chem. 2005 Oct 6;48(20):6261-70. | ||||
| REF 7 | 4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modific... J Med Chem. 2006 Aug 10;49(16):4896-911. | ||||
| REF 8 | Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. J Med Chem. 2002 Sep 26;45(20):4513-23. | ||||
| REF 9 | Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives. J Med Chem. 2002 Jul 4;45(14):3057-66. | ||||
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