Tyrosine-protein kinase receptor RET Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Cabozantinib	IC50	10.1 [1]
	3-(2-Phenylethynyl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	56.5 [1]
	3-(5-Cyclopropyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	4.0 [1]
	N-(5-Tert-butyl-1,2-oxazol-3-yl)-2-(4-imidazo[1,2-a]pyridin-6-ylphenyl)acetamide	IC50	250.0 [1]
	Vandetanib	IC50	49.0 [1], 97.0 [2], 100.0 [3], 102.0 [4], 950.0 [5]
	2-[4-(4-Ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[3-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-5-yl]acetamide	IC50	0.4 [1], 3.4 [2], 100.0 [3]
	RET Kinase inhibitor 1	IC50	0.4 [1], 11.1 [2], 100.0 [3]
	Staurosporine	IC50	0.46 [1], 1.69 [2], 4.6 [3], 4.7 [4]
	Sunitinib	IC50	1.0 [1], 220.0 [2], 224.0 [3], 1300.0 [4]
	Ponatinib	IC50	0.3 [1], 0.9 [2], 25.8 [3], 33.9 [4]
	JH-VIII-157-02	IC50	3.0 [1], 12.0 [2], 13.0 [3]
	1-Propan-2-yl-3-(5-propan-2-yl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine	IC50	41.0 [1], 355.0 [2]
	3-(1,2-Oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	213.0 [1], 903.0 [2]
	3-(5-Cyclopropyl-1,2-oxazol-3-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-amine	IC50	52.0 [1], 354.0 [2]
	N-(5-Tert-butyl-1,2-oxazol-3-yl)-2-(3-imidazo[1,2-b]pyridazin-6-yloxyphenyl)acetamide	IC50	750.0 [1], 2500.0 [2]
	N-[(R)-Cyclopropyl(pyridin-2-yl)methyl]-3-[4-[(1S,5S)-3-hydroxy-8-azabicyclo[3.2.1]octan-8-yl]phenyl]-1H-indazole-5-carboxamide	IC50	250.0 [1], 280.0 [2], 2800.0 [3]
	8-[1-[3-(Dimethylamino)propyl]pyrazol-4-yl]-9-ethyl-6,6-dimethyl-11-oxo-5H-benzo[b]carbazole-3-carbonitrile	IC50	2.0 [1], 9.0 [2], 23.0 [3]
	2-[4-(5-Ethoxy-6-oxo-1H-pyridin-3-yl)-2,3-difluorophenyl]-N-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]acetamide	IC50	100.0 [1]
	N-(3,4-Dichlorophenyl)-2-[4-(5-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide	IC50	100.0 [1], 500.0 [2]
	Sorafenib	IC50	6.0 [1], 9.0 [2]
	Dasatinib	IC50	433.0 [1], 2100.0 [2]
	Ibrutinib	IC50	5.2 [1], 37.0 [2]
	Alectinib	IC50	4.8 [1], 39.8 [2]
	Ceritinib	IC50	400.0 [1], 2304.0 [2]
	Motesanib	IC50	66.0 [1], 90.0 [2]
	Nvp-aew541	IC50	3300.0 [1]
	Mivavotinib	IC50	8.4 [1], 19.0 [2]
	Tafetinib	IC50	1.3 [1], 5.0 [2]
	6,6-Dimethyl-8-[1-(oxan-4-ylmethyl)piperidin-4-yl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile	IC50	1.6 [1], 10.4 [2]
	6-(4-Fluorophenyl)-4-(4-methylbenzyl)-3(2H)-pyridazinone	IC50	6160.0 [1], 66200.0 [2]
	cis-3-[4-Amino-7-(3-azetidin-1-ylmethyl-cyclobutyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-phenol	IC50	8.0 [1]
	7-[3-(Azetidin-1-ylmethyl)cyclobutyl]-5-[3-[[(2S)-oxolan-2-yl]methoxy]phenyl]pyrrolo[2,3-d]pyrimidin-4-amine	IC50	4400.0 [1]
	3-[(6,7-Dimethoxyquinazolin-4-yl)amino]-4-fluoro-2-methylphenol	IC50	44.0 [1]
	4-(3-(5-Morpholino-1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)isoquinoline	IC50	1000.0 [1]
	N-[[5-[3-(6-Fluoro-1H-benzimidazol-2-yl)-2H-pyrazolo[3,4-b]pyridin-5-yl]pyridin-3-yl]methyl]ethanamine	IC50	110.0 [1]
	N-[[5-[3-(5,6-Difluoro-1H-benzimidazol-2-yl)-2H-pyrazolo[3,4-b]pyridin-5-yl]pyridin-3-yl]methyl]ethanamine	IC50	39.0 [1], 390.0 [2]
	N-Ethyl-N-[[2-(5-isoquinolin-4-yl-2H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzimidazol-4-yl]methyl]ethanamine	IC50	1000.0 [1]
	2-(5-Isoquinolin-4-yl-2H-pyrazolo[3,4-b]pyridin-3-yl)-N-propan-2-yl-1H-benzimidazole-4-carboxamide	IC50	410.0 [1]
	N,N-Diethyl-2-(5-isoquinolin-4-yl-2H-pyrazolo[3,4-b]pyridin-3-yl)-1H-benzimidazole-4-carboxamide	IC50	1230.0 [1]
	4-[3-[6-(4-Methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-2H-pyrazolo[3,4-b]pyridin-5-yl]isoquinoline	IC50	1000.0 [1]
	3-(4-(Methoxymethyl)-1H-benzo[d]imidazol-2-yl)-5-(pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridine	IC50	1100.0 [1]
	N-[[5-[3-[6-(4-Methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-2H-pyrazolo[3,4-b]pyridin-5-yl]pyridin-3-yl]methyl]ethanamine	IC50	140.0 [1]
	1-[5-[3-[4-(Methoxymethyl)-1H-benzimidazol-2-yl]-2H-pyrazolo[3,4-b]pyridin-5-yl]pyridin-3-yl]-N,N-dimethylmethanamine	IC50	3230.0 [1]
	1-[4-[(E)-(5,6-Dimethoxy-2-oxo-1H-indol-3-ylidene)methyl]phenyl]-3-(4-hydroxyphenyl)urea	IC50	50.0 [1]
	1-(2,2-Diethoxyethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine	IC50	598.0 [1]
	3-(5-Cyclopropyl-1,2-oxazol-3-yl)-1-heptylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	96.0 [1], 927.0 [2]
	1-[4-Amino-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropan-2-ol	IC50	68.0 [1], 217.0 [2]
	1-Cyclohexyl-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine	IC50	2.0 [1], 14.0 [2]
	3-(5-Cyclopentyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	241.0 [1], 1570.0 [2]
	3-(5-Benzyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	241.0 [1], 1990.0 [2]
	1-Benzyl-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine	IC50	74.0 [1], 557.0 [2]
	3-(5-Phenyl-4,5-dihydro-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	583.0 [1], 5680.0 [2]
	1-Propan-2-yl-3-(5-pyridin-2-yl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine	IC50	910.0 [1], 5880.0 [2]
	3-(5-Tert-butyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	210.0 [1], 2100.0 [2]
	3-(5-Cyclopropyl-1,2-oxazol-3-yl)-1-methylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	27.0 [1], 182.0 [2]
	3-(5-Cyclopropyl-1,2-oxazol-3-yl)-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine	IC50	5.0 [1], 41.0 [2]
	3-(5-Ethyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine	IC50	41.0 [1], 531.0 [2]
	5-Amino-3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazole-4-carboxamide	IC50	44.0 [1], 252.0 [2]
	(NE)-N-[(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)methylidene]hydroxylamine	IC50	3680.0 [1], 4900.0 [2]
	5-Amino-1-propan-2-yl-3-(5-thiophen-3-yl-1,2-oxazol-3-yl)pyrazole-4-carboxamide	IC50	162.0 [1], 2902.0 [2]
	4-Fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol	IC50	0.2 [1], 315.7 [2]
	5-Amino-1-propan-2-yl-3-(5-thiophen-2-yl-1,2-oxazol-3-yl)pyrazole-4-carboxamide	IC50	78.0 [1], 1218.0 [2]
	N-[3-[(Dimethylamino)methyl]-2-fluoro-5-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide	IC50	2.8 [1], 70.2 [2]
	N-[4-[(Dimethylamino)methyl]-3-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide	IC50	0.8 [1], 20.7 [2]
	N-[4-(2-Amino-2-methylpropyl)-3-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide	IC50	0.2 [1], 6.5 [2]
	2-[4-(4-Ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[4-(2-hydroxy-2-methylpropyl)-3-(trifluoromethyl)phenyl]acetamide	IC50	0.4 [1], 6.7 [2]
	N-[4-(1-Cyanoethyl)-3-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide	IC50	0.7 [1], 63.1 [2]
	N-[4-(2,2-Dimethyl-3-methylsulfonylpropyl)-3-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide	IC50	0.6 [1], 3.9 [2]
	5-(4-Chlorophenyl)-3-{[(4-chlorophenyl)sulfanyl]methyl}-1H-1,2,4-triazole	IC50	9380.0 [1], 10300.0 [2]
	Infigratinib phosphate	IC50	3352.0 [1], 10000.0 [2]
	4-Fluoro-N-[3-[[[1-(2-phenylethyl)pyrazolo[3,4-d]pyrimidin-4-yl]amino]methyl]phenyl]benzenesulfonamide	IC50	4830.0 [1], 5470.0 [2]
	1-(4-Fluorophenyl)-3-[3-[[[1-(2-phenylethyl)pyrazolo[3,4-d]pyrimidin-4-yl]amino]methyl]phenyl]urea	IC50	4800.0 [1], 7960.0 [2]
	4-Bromo-N-[3-[[[1-(2-phenylethyl)pyrazolo[3,4-d]pyrimidin-4-yl]amino]methyl]phenyl]benzamide	IC50	4260.0 [1], 9310.0 [2]
	2-[4-(4-Ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[4-(3-hydroxy-2,2-dimethylpropyl)-3-(trifluoromethyl)phenyl]acetamide	IC50	0.4 [1], 9.4 [2]
	2-[4-(4-Ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[3-(5-methyl-1,3,4-oxadiazol-2-yl)-5-(trifluoromethyl)phenyl]acetamide	IC50	0.4 [1], 29.5 [2]
	2-[4-(4-Ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[3-(trifluoromethyl)phenyl]acetamide	IC50	1.7 [1], 111.1 [2]
	6-Ethyl-5-[(4-hydroxy-4-methylcyclohexyl)amino]-3-[3-methyl-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]pyrazine-2-carboxamide	IC50	1.0 [1], 1.1 [2]
	Quercetin	IC50	78100.0 [1]
	Gefitinib	IC50	1700.0 [1]
	Amitriptyline	IC50	1000.0 [1]
	Staurosporine HCl	IC50	2.19 [1]
	Nortriptyline	IC50	5000.0 [1]
	Ellagic acid	IC50	40000.0 [1]
	Crizotinib	IC50	10000.0 [1]
	Sinequan	IC50	20000.0 [1]
	Semaxanib	IC50	170.0 [1]
	Cyclobenzaprine	IC50	300.0 [1]
	Lenvatinib	Ki	1.5 [1]
	Su6656	IC50	770.0 [1]
	Lofepramine	IC50	20000.0 [1]
	Doramapimod	IC50	30.0 [1]
	Sotrastaurin	IC50	10000.0 [1]
	Fedratinib	IC50	48.0 [1]
	Linifanib	IC50	1900.0 [1]
	Nvp-tae 684	IC50	1385.0 [1]
	(R)-6-(4-((4-Ethylpiperazin-1-yl)methyl)phenyl)-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine	IC50	740.0 [1]
	Danusertib	IC50	31.0 [1]
	Janex-1	IC50	720.0 [1]
	Entrectinib	IC50	393.0 [1]
	CID 53469448	IC50	1215.0 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

Items per page: 510All1 - 10 of 100 ⟨⟩

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References

This online tool may be cited as follows

MLA	"Quest Database™ Tyrosine-protein kinase receptor RET Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 10 May. 2024, https://www.aatbio.com/data-sets/tyrosine-protein-kinase-receptor-ret-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2024, May 10). Quest Database™ Tyrosine-protein kinase receptor RET Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tyrosine-protein-kinase-receptor-ret-inhibitors-ic50-ki.
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