Epidermal growth factor receptor erbB1 Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Gefitinib	IC50	20.0 [1]
	Gefitinib	Ki	0.4 [1]
	Erlotinib	IC50	30.0 [1]
	Erlotinib	Ki	0.1 [1], 45.0 [2]
	Osimertinib	IC50	3.9 [1]
	Osimertinib	Ki	1.5 [1], 1.6 [2], 3.5 [3], 14.0 [4]
	Lapatinib	IC50	12.0 [1]
	N-(3-Bromophenyl)-6,7-dimethoxyquinazolin-4-amine	IC50	30.0 [1]
	N-(3-Bromophenyl)-6,7-dimethoxyquinazolin-4-amine	Ki	0.01 [1]
	Rociletinib	IC50	20.0 [1]
	Rociletinib	Ki	1.7 [1], 1.8 [2], 21.0 [3], 74.0 [4], 303.0 [5]
	WZ4002	IC50	10.0 [1]
	4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline	IC50	2.0 [1]
	Staurosporine	IC50	49.0 [1]
	Afatinib	IC50	1.0 [1]
	Canertinib	IC50	2.3 [1]
	Pelitinib	IC50	39.0 [1]
	N4-(3-Bromophenyl)quinazoline-4,6-diamine	IC50	44.0 [1]
	Vandetanib	IC50	200.0 [1]
	Sunitinib	IC50	172100.0 [1]
	Tyrphostin A46	IC50	10000.0 [1]
	Tyrphostin A46	Ki	3500.0 [1]
	4-(4-Fluorophenyl)-5-pyridin-4-yl-2-(2,4,6-trichlorophenyl)pyrazol-3-amine	IC50	113.0 [1]
	Neratinib	IC50	2.5 [1]
	N-(3-Chloro-4-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine	IC50	9.0 [1]
	Ibrutinib	IC50	5.6 [1]
	N4-(3-Chlorophenyl)quinazoline-4,6-diamine	IC50	200.0 [1]
	Tyrphostin B42	IC50	501.19 [1]
	N4-(3-Bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine	IC50	0.01 [1]
	Tykerb	IC50	11.0 [1]
	Semaxanib	IC50	100000.0 [1]
	N-(4-((3-Bromophenyl)amino)quinazolin-6-yl)but-2-ynamide	IC50	2.5 [1]
	Tyrphostin AG 538	IC50	5000.0 [1]
	4-[(3-Bromophenyl)amino]-6,7-diaminoquinazoline	IC50	0.12 [1]
	(E)-N-[4-(3-Bromoanilino)-3-cyanoquinolin-6-yl]-4-(dimethylamino)but-2-enamide	IC50	310.0 [1]
	N-(3-Bromophenyl)-1H-pyrazolo[4,3-g]quinazolin-5-amine	IC50	0.44 [1]
	N-[4-(3-Bromoanilino)-3-cyanoquinolin-6-yl]but-2-ynamide	IC50	940.0 [1]
	N-[4-(3-Bromo-phenylamino)-3-cyano-quinolin-6-yl]-acrylamide	IC50	590.0 [1]
	N-[3-[2-[4-(4-Acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]oxyphenyl]prop-2-enamide	IC50	7.0 [1], 67.0 [2], 132.0 [3], 200.0 [4], 1034.0 [5]
	Tyrphostin 47	IC50	1310.0 [1], 2400.0 [2], 3000.0 [3], 7000.0 [4]
	Tyrphostin 47	Ki	850.0 [1]
	Dacomitinib	IC50	6.0 [1]
	Tyrphostin AG 555	IC50	700.0 [1]
	Tyrphostin B48	IC50	1250.0 [1]
	Lavendustin c	IC50	30.0 [1], 150.0 [2], 2900.0 [3], 92000.0 [4]
	(2e)-N-{4-[(3-Bromophenyl)amino]quinazolin-6-Yl}-4-(Dimethylamino)but-2-Enamide	IC50	10.0 [1]
	7-Amino-4-[(3-bromophenyl)amino]pyrido[4,3-d]pyrimidine	IC50	10.0 [1]
	N-(3-Bromophenyl)-8H-pyrrolo[3,2-g]quinazolin-4-amine	IC50	0.44 [1]
	Afatinib Impurity C	IC50	0.5 [1]
	Dithiobis(1H-indoles) deriv. 4	IC50	3300.0 [1], 7400.0 [2], 7600.0 [3], 100000.0 [4]
	Dithiobis(1H-indoles) deriv. 4	Ki	19400.0 [1], 21200.0 [2]
	4-N-(3-Bromophenyl)pyrido[3,4-d]pyrimidine-4,6-diamine	IC50	0.13 [1]
	4-N-(3-Bromophenyl)-6-N,6-N-dimethylpyrido[3,4-d]pyrimidine-4,6-diamine	IC50	0.01 [1]
	Unii-5IE92SK9EB	IC50	7.0 [1], 13.0 [2], 140.0 [3], 5100.0 [4]
	Unii-5IE92SK9EB	Ki	1600.0 [1]
	N-[(3R,4R)-4-Fluoro-1-[6-[(1-methylpyrazol-4-yl)amino]-9-propan-2-ylpurin-2-yl]pyrrolidin-3-yl]prop-2-enamide	IC50	2.0 [1], 7.0 [2], 9.0 [3], 178.0 [4]
	N-[(3R,4R)-4-Fluoro-1-[6-[(1-methylpyrazol-4-yl)amino]-9-propan-2-ylpurin-2-yl]pyrrolidin-3-yl]prop-2-enamide	Ki	2.0 [1]
	N-[(3R,4R)-1-[6-[(1,3-Dimethylpyrazol-4-yl)amino]-9-propan-2-ylpurin-2-yl]-4-fluoropyrrolidin-3-yl]prop-2-enamide	IC50	4.0 [1], 16.0 [2], 26.0 [3], 1450.0 [4], 10000.0 [5]
	N-[(3R,4R)-1-[6-[(1,3-Dimethylpyrazol-4-yl)amino]-9-propan-2-ylpurin-2-yl]-4-fluoropyrrolidin-3-yl]prop-2-enamide	Ki	17.0 [1]
	1-[(3R)-3-[4-Amino-3-(1-methylindol-3-yl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one	IC50	3.0 [1]
	1-[(3R)-3-(4-Amino-3-naphthalen-1-ylpyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl]prop-2-en-1-one	IC50	2.0 [1]
	1-[(3R)-3-(4-Amino-3-naphthalen-2-ylpyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl]prop-2-en-1-one	IC50	1.0 [1]
	N-(4-(3-Bromoanilino)quinazolin-6-yl)-2-(perfluorophenoxy)-acetamide	IC50	49.8 [1]
	N-[2-[2-(Dimethylamino)ethyl-methylamino]-5-[[6-(3-fluoroanilino)-1H-indazol-3-yl]amino]-4-methoxyphenyl]prop-2-enamide	IC50	1.0 [1]
	N-[2-[2-(Dimethylamino)ethyl-methylamino]-5-[[6-(3-fluoroanilino)-1H-indazol-3-yl]amino]-4-methoxyphenyl]prop-2-enamide	Ki	3.9 [1], 5.1 [2], 7.4 [3]
	N-[2-[2-(Dimethylamino)ethyl-methylamino]-4-methoxy-5-[(5-naphthalen-2-yl-1H-indazol-3-yl)amino]phenyl]prop-2-enamide	IC50	1.1 [1], 2.2 [2], 8.1 [3]
	N-[2-[2-(Dimethylamino)ethyl-methylamino]-4-methoxy-5-[(5-naphthalen-2-yl-1H-indazol-3-yl)amino]phenyl]prop-2-enamide	Ki	28.0 [1], 105.0 [2], 147.0 [3]
	N-[2-[2-(Dimethylamino)ethyl-methylamino]-4-methoxy-5-[[6-(1-methylindol-3-yl)-1H-indazol-3-yl]amino]phenyl]prop-2-enamide	IC50	1.5 [1], 4.8 [2], 9.3 [3]
	N-[2-[2-(Dimethylamino)ethyl-methylamino]-4-methoxy-5-[[6-(1-methylindol-3-yl)-1H-indazol-3-yl]amino]phenyl]prop-2-enamide	Ki	57.0 [1], 149.0 [2], 236.0 [3]
	Genistein	IC50	1000.0 [1], 2600.0 [2], 25120.0 [3]
	Dasatinib	IC50	20.0 [1], 180.0 [2], 322.0 [3], 2870.0 [4]
	Crizotinib	IC50	1000.0 [1], 12500.0 [2], 1000000.0 [3]
	N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine	IC50	0.31 [1], 0.32 [2], 5.0 [3], 6.0 [4], 120.0 [5]
	Tyrphostin B56	IC50	1100.0 [1], 3000.0 [2], 5000.0 [3], 5011.87 [4]
	Cudc-101	IC50	2.4 [1], 17.6 [2]
	Poziotinib	IC50	1.3 [1], 2.2 [2], 3.2 [3], 4.2 [4], 4.4 [5]
	Tyrphostin AG 698	IC50	616.6 [1], 625.0 [2], 900.0 [3], 930.0 [4]
	N-(3-Bromophenyl)quinazolin-4-amine	IC50	27.0 [1], 27.54 [2]
	(E)-N-[4-(3-Bromoanilino)-3-cyanoquinolin-6-yl]but-2-enamide	IC50	1620.0 [1], 1621.81 [2], 1620317.04 [3]
	N-[4-(3-Bromoanilino)-3-cyanoquinolin-6-yl]-4-methoxybut-2-ynamide	IC50	954.99 [1], 960.0 [2], 960063.59 [3]
	N-[4-(3-Chloro-4-fluoro-phenylamino)-3-cyano-quinolin-6-yl]-2-morpholin-4-ylmethyl-acrylamide	IC50	2691.53 [1], 2700.0 [2], 2700225.29 [3]
	(E)-N-[4-(3-Chloro-4-fluoroanilino)-3-cyanoquinolin-6-yl]-4-morpholin-4-ylbut-2-enamide	IC50	2290.0 [1], 2290.87 [2], 2290340.22 [3]
	N-[4-(3-Bromoanilino)-3-cyanoquinolin-6-yl]-4-(2-methoxyethoxy)but-2-ynamide	IC50	930.0 [1], 933.25 [2], 930036.51 [3]
	N-[4-(3-Bromoanilino)-3-cyanoquinolin-6-yl]-4-thiomorpholin-4-ylbut-2-ynamide	IC50	549.54 [1], 550.0 [2], 550047.25 [3]
	(E)-N-[4-(3-Chloro-4-fluoroanilino)-3-cyanoquinolin-6-yl]-4-(dimethylamino)but-2-enamide	IC50	645.65 [1], 650.0 [2], 650129.69 [3]
	2-Hydroxy-5-[(2,5-dihydroxybenzyl)amino]benzoic acid methyl ester	IC50	600.0 [1], 1000.0 [2], 9000.0 [3], 24400.0 [4]
	4-N-(3-Bromophenyl)-7-N-methylpyrido[4,3-d]pyrimidine-4,7-diamine	IC50	0.13 [1], 16.0 [2]
	4-N-(3-Bromophenyl)-7-N,7-N-dimethylpyrido[4,3-d]pyrimidine-4,7-diamine	IC50	0.09 [1], 14.0 [2]
	4-N-(3-Bromophenyl)pyrido[3,2-d]pyrimidine-4,6-diamine	IC50	7.6 [1], 7.76 [2], 53.0 [3]
	4-N-(3-Bromophenyl)-6-N-methylpyrido[3,2-d]pyrimidine-4,6-diamine	IC50	3.1 [1], 3.16 [2], 20.0 [3]
	4-N-(3-Bromophenyl)-6-N,6-N-dimethylpyrido[3,2-d]pyrimidine-4,6-diamine	IC50	9.6 [1], 9.77 [2], 32.0 [3]
	Tyrphostin deriv. 25	IC50	560.0 [1], 600.0 [2], 5100.0 [3], 5128.61 [4], 20000.0 [5]
	Tyrphostin deriv. 28	IC50	880.0 [1], 900.0 [2], 7000.0 [3], 15000.0 [4], 15135.61 [5]
	Tyrphostin deriv. 29	IC50	1000.0 [1], 1300.0 [2], 14000.0 [3], 14125.38 [4], 15000.0 [5]
	Tyrphostin deriv. 33	IC50	2000.0 [1], 2300.0 [2], 10964.78 [3], 11000.0 [4], 20000.0 [5]
	2-Cyano-3-(4-hydroxy-3-methoxy-5-((phenylthio)methyl)phenyl)-2-propenamide	IC50	398.11 [1], 400.0 [2], 500.0 [3], 2900.0 [4], 12500.0 [5]
	6,7-Bis(3-morpholin-4-ylpropoxy)-N-[4-[(E)-prop-1-enyl]phenyl]quinazolin-4-amine	IC50	20.7 [1], 20.72 [2], 235.5 [3], 1000.0 [4], 2000.0 [5]
	Mavelertinib	IC50	3.0 [1], 5.0 [2], 12.0 [3], 307.0 [4]
	Mavelertinib	Ki	13.0 [1]
	N-[(3R,4R)-4-Fluoro-1-[6-[(3-methoxy-1-methylpyrazol-4-yl)amino]-9-propan-2-ylpurin-2-yl]pyrrolidin-3-yl]prop-2-enamide	IC50	1.0 [1], 2.0 [2], 5.0 [3], 160.0 [4]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

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References

This online tool may be cited as follows

MLA	"Quest Database™ Epidermal growth factor receptor erbB1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/epidermal-growth-factor-receptor-erbb1-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2025, February 21). Quest Database™ Epidermal growth factor receptor erbB1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/epidermal-growth-factor-receptor-erbb1-inhibitors-ic50-ki.
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