Protein Information

General Information of the Protein

Protein ID	PT01233
Protein Name	Receptor tyrosine-protein kinase erbB-2
Secondarily Protein Name	Metastatic lymph node gene 19 protein Proto-oncogene Neu Proto-oncogene c-ErbB-2 Tyrosine kinase-type cell surface receptor HER2 p185erbB2
Gene Name	ERBB2
Secondarily Gene Name	HER2 MLN19 NEU NGL
Sequence	MELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNLELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNGDPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLALTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQCAAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACPYNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSANIQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLPDLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTVPWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQECVEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARCPSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVGILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETELRKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAGVGSPYVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDVRLVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRFTHQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCWMIDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVDAEEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSEGAGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEYVNQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTPQGGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Kinase > Protein Kinase > TK protein kinase group > Tyrosine protein kinase EGFR family
Function	Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. This prevents the phosphorylation of APC and CLASP2, allowing its association with the cell membrane. In turn, membrane-bound APC allows the localization of MACF1 to the cell membrane, which is required for microtubule capture and stabilization. Show/Hide
Uniprot ID	Primary ID: P04626 Secondarily ID: B2RZG3 B4DHN3 Q14256 Q6LDV1 Q9UMK4 X5D2V5 Show/Hide
Ensembl ID	ENSG00000141736
HGNC ID	HGNC:3430
Subcellular Location	Cell membrane Cell projection Ruffle membrane

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000068 , A-549

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0236216 Compound Info	[3-oxo-3-[3-(pyridine-2-carbonylamino)anilino]propyl] 4-phenylpiperazine-1-carbodithioate Show/Hide	C26H27N5O2S2	1
1	IC50 = 54 nM Bioactivity Info	TI LI LO TS
CP0037987 Compound Info	N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine Show/Hide	C22H23N3O4	1
1	IC50 = 64 nM Bioactivity Info	TI LI LO TS
CP0348177 Compound Info	N-[3-(cyclohexylcarbamoylamino)phenyl]pyridine-2-carboxamide Show/Hide	C19H22N4O2	1
1	IC50 = 64 nM Bioactivity Info	TI LI LO TS
CP0343779 Compound Info	[2-oxo-2-[3-(pyridine-2-carbonylamino)anilino]ethyl] piperidine-1-carbodithioate Show/Hide	C20H22N4O2S2	1
1	IC50 = 104 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000077 , Ba/F3

Cell Line Info

Cell Line ID: CL000218 , BT-474

Cell Line Info

Cell Line ID: CL000083 , MCF-7

Cell Line Info

Cell Line ID: CL000919 , MCF-7 cl.24

Cell Line Info

Cell Line ID: CL000284 , MDA-MB-453

Cell Line Info

Cell Line ID: CL000216 , NCI-N87

Cell Line Info

Cell Line ID: CL000035 , NIH 3T3

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000261 , SK-BR-3

Cell Line Info

Cell Line ID: CL000084 , SK-OV-3

Cell Line Info

Cell Line ID: CL000203 , T24

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0569797 Compound Info	(Z)-N-[7-ethoxy-4-[3-methyl-4-([1,2,4]triazolo[4,3-c]pyrimidin-7-yloxy)anilino]quinazolin-6-yl]-2-fluoro-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide Show/Hide	C30H30FN9O3	4
1	IC50 = 0.16 nM
2	IC50 = 0.42 nM
3	IC50 = 0.43 nM
4	IC50 = 0.56 nM
CP0078880 Compound Info	4-Dimethylamino-but-2-enoic acid {4-[3-chloro-4-(pyridin-2-ylmethoxy)-phenylamino]-3-cyano-7-ethoxy-quinolin-6-yl}-amide Show/Hide	C30H29ClN6O3	9
1	IC50 = 1 nM
2	IC50 = 1.76 nM
3	IC50 = 4.4 nM
4	IC50 = 4.57 nM
5	IC50 = 6.09 nM
6	IC50 = 29.33 nM
7	IC50 = 59 nM
8	IC50 = 60 nM
9	Kd = 6 nM
CP0036696 Compound Info	(2R)-2-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]quinazolin-5-yl]oxy-N,N-dimethylpropanamide Show/Hide	C25H24ClN5O3	1
1	IC50 < 1 nM
CP0036701 Compound Info	(R)-N,N-dimethyl-2-(4-(3-methyl-4-(6-methylpyridin-3-yloxy)phenylamino)quinazolin-5-yloxy)propanamide Show/Hide	C26H27N5O3	1
1	IC50 < 1 nM
CP0053637 Compound Info	(S)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide Show/Hide	C24H25ClFN5O3	5
1	IC50 = 2 nM
2	IC50 = 12.5 nM
3	IC50 = 14 nM
4	IC50 = 17.3 nM
5	Kd = 5 nM
CP0077867 Compound Info	N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-(1-methylpiperidin-4-yl)oxyquinazolin-4-amine Show/Hide	C26H26ClN5O2	1
1	IC50 < 2 nM
CP0080978 Compound Info	N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-5-(1-methylpiperidin-4-yl)oxyquinazolin-4-amine Show/Hide	C27H26ClFN4O2	1
1	IC50 < 2 nM
CP0285486 Compound Info	(2R)-N-(2-hydroxyethyl)-N-methyl-2-[4-[3-methyl-4-(6-methylpyridin-3-yl)oxyanilino]quinazolin-5-yl]oxypropanamide Show/Hide	C27H29N5O4	1
1	IC50 = 2 nM
CP0318731 Compound Info	5-(Dimethyl-hydrazonomethyl)-N-[1-(3-fluoro-benzyl)-1H-indazol-5-yl]-pyrimidine-4,6-diamine Show/Hide	C21H21FN8	1
1	IC50 = 2 nM
CP0283069 Compound Info	US8901140, 5 Show/Hide	C32H31ClN6O3	5
1	IC50 = 2.4 nM
2	IC50 = 3.91 nM
3	IC50 = 4.43 nM
4	IC50 = 6.65 nM
5	IC50 = 57.36 nM
CP0007142 Compound Info	N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine Show/Hide	C29H26ClFN4O4S	19
1	IC50 = 2.7 nM
2	IC50 = 4.5 nM
3	IC50 = 9 nM
4	IC50 = 9.2 nM
5	IC50 = 9.8 nM
6	IC50 = 10 nM
7	IC50 = 10.2 nM
8	IC50 = 10.3 nM
9	IC50 = 13 nM
10	IC50 = 23.9 nM
11	IC50 = 29.2 nM
12	IC50 = 36 nM
13	IC50 = 36.3 nM
14	IC50 = 42 nM
15	IC50 = 60 nM
16	IC50 = 95.5 nM
17	IC50 = 540 nM
18	Kd = 7 nM
19	Kd = 11 nM
CP0664046 Compound Info	Lapatinib ditosylate Show/Hide	C43H44ClFN4O11S3	4
1	IC50 = 3 nM
2	IC50 = 5 nM
3	IC50 = 9 nM
4	IC50 = 10.3 nM
CP0098558 Compound Info	N-[2-[4-[3-chloro-4-[3-(trifluoromethyl)phenoxy]anilino]pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methylbutanamide Show/Hide	C26H25ClF3N5O3	1
1	IC50 = 3 nM
CP0061645 Compound Info	4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)-3-methyl-N-(2-morpholinoethyl)-1H-pyrrolo[3,2-d]pyridazine-2-carboxamide Show/Hide	C27H28ClFN6O3	1
1	IC50 = 4 nM
CP0204110 Compound Info	N-[3-[5-[2-[4-[2-(dimethylamino)ethyl]anilino]pyrimidin-4-yl]imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2,6-difluorobenzamide Show/Hide	C32H27F2N7OS	1
1	IC50 = 4.3 nM
CP0036058 Compound Info	N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide Show/Hide	C24H25ClFN5O3	8
1	IC50 = 5 nM
2	IC50 = 9 nM
3	IC50 = 19 nM
4	IC50 = 48 nM
5	IC50 = 80 nM
6	Kd = 8.4 nM
7	Kd = 56 nM
8	Kd = 87 nM
CP0150154 Compound Info	4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)-N-(2-(diethylamino)ethyl)-3-methyl-1H-pyrrolo[3,2-d]pyridazine-2-carboxamide Show/Hide	C27H30ClFN6O2	1
1	IC50 = 7 nM
CP0163871 Compound Info	4-N-[1-[(3-fluorophenyl)methyl]indazol-5-yl]-5-[(E)-morpholin-4-yliminomethyl]pyrimidine-4,6-diamine Show/Hide	C23H23FN8O	1
1	IC50 = 7 nM
CP0100818 Compound Info	CHEMBL1257998 Show/Hide	C29H32ClN9O	1
1	IC50 = 7.5 nM
CP0034904 Compound Info	(R)-N,N-dimethyl-2-(4-(1-(pyridin-2-ylmethyl)-1H-indazol-5-ylamino)quinazolin-5-yloxy)propanamide Show/Hide	C26H25N7O2	1
1	IC50 = 8 nM
CP0270656 Compound Info	4-N-[1-[(3-fluorophenyl)methyl]indazol-5-yl]-5-[(E)-(4-methylpiperazin-1-yl)iminomethyl]pyrimidine-4,6-diamine Show/Hide	C24H26FN9	1
1	IC50 = 8 nM
CP0281776 Compound Info	2-(4-((4-(1-(3-fluorobenzyl)-1H-indazol-5-ylamino)-6-aminopyrimidin-5-yl)methyleneamino)piperazin-1-yl)ethanol Show/Hide	C25H28FN9O	1
1	IC50 = 8 nM
CP0038059 Compound Info	2-methoxy-N-[(E)-3-[4-[3-methyl-4-(6-methylpyridin-3-yl)oxyanilino]quinazolin-6-yl]prop-2-enyl]acetamide Show/Hide	C27H27N5O3	3
1	IC50 = 10 nM
2	IC50 = 12 nM
3	Kd = 43 nM
CP0163868 Compound Info	4-(1-(3-fluorobenzyl)-1H-indazol-5-ylamino)-6-aminopyrimidine-5-carbaldehyde O-methyl oxime Show/Hide	C20H18FN7O	1
1	IC50 = 12 nM
CP0198587 Compound Info	1-{4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl}-3-{2-[(2-methoxyphenyl)methyl]-1H-1,3-benzodiazol-6-yl}-1H-pyrazolo[3,4-d]pyrimidin-4-amine Show/Hide	C34H41N9O	1
1	IC50 = 13 nM
CP0301436 Compound Info	N-[3-[5-[2-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2,6-difluorobenzamide Show/Hide	C34H30F2N8OS	1
1	IC50 = 14 nM
CP0064131 Compound Info	7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide Show/Hide	C24H26N4O4	1
1	IC50 = 15.7 nM
CP0055593 Compound Info	CHEMBL1256432 Show/Hide	C29H31ClFN9O	1
1	IC50 = 16 nM
CP0153482 Compound Info	DACOMITINIB Show/Hide	C24H25ClFN5O2	2
1	IC50 = 16.7 nM
2	IC50 = 45 nM
CP0245059 Compound Info	4-[4-(4-amino-3-{2-[(2-methoxyphenyl)methyl]-1H-1,3-benzodiazol-6-yl}-1H-pyrazolo[3,4-d]pyrimidin-1-yl)cyclohexyl]-N,N-dimethylpiperazine-1-carboxamide Show/Hide	C33H40N10O2	1
1	IC50 = 17 nM
CP0051806 Compound Info	(6S,7S)-6-(4-phenyl-3,6-dihydro-2H-pyridine-1-carbonyl)-5-aza-spiro[2.5]octane-7-carboxylic acid hydroxyamide Show/Hide	C20H25N3O3	1
1	IC50 = 18 nM
CP0039472 Compound Info	4-N-[1-[(3-fluorophenyl)methyl]indazol-5-yl]-5-[(E)-piperidin-1-yliminomethyl]pyrimidine-4,6-diamine Show/Hide	C24H25FN8	1
1	IC50 = 18 nM
CP0814233 Compound Info	N-[1-(3-Fluoro-benzyl)-1H-indazol-5-yl]-5-[(2,2,2-trifluoro-ethyl)-hydrazonomethyl]-pyrimidine-4,6-diamine Show/Hide	C21H18F4N8	1
1	IC50 = 20 nM
CP0038066 Compound Info	5-[(4-aminopiperidin-1-yl)methyl]-N-[1-[(3-fluorophenyl)methyl]indazol-5-yl]pyrrolo[2,1-f][1,2,4]triazin-4-amine Show/Hide	C26H27FN8	1
1	IC50 = 22 nM
CP0227701 Compound Info	[(3S)-morpholin-3-yl]methyl N-[4-[[1-[(3-fluorophenyl)methyl]indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamate Show/Hide	C27H27FN8O3	2
1	IC50 = 23 nM
2	IC50 = 30 nM
CP0035025 Compound Info	4-anilinoquinazoline deriv. 2 Show/Hide	C17H13BrN4O	2
1	IC50 = 24 nM
2	IC50 = 114 nM
CP0209615 Compound Info	5-((1,4-diazepan-1-yl)methyl)-N-(1-(3-fluorobenzyl)-1H-indazol-5-yl)pyrrolo[1,2-f][1,2,4]triazin-4-amine Show/Hide	C26H27FN8	1
1	IC50 = 27 nM
CP0004106 Compound Info	(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one Show/Hide	C28H26N4O3	7
1	IC50 = 27.6 nM
2	IC50 = 51 nM
3	IC50 = 104 nM
4	IC50 = 108 nM
5	IC50 = 115 nM
6	Kd = 190 nM
7	Kd > 10000 nM
CP0340608 Compound Info	(S)-N4-(1-(3-fluorobenzyl)-1H-indazol-5-yl)-5-((2-(methoxymethyl)pyrrolidin-1-ylimino)methyl)pyrimidine-4,6-diamine Show/Hide	C25H27FN8O	1
1	IC50 = 39 nM
CP0198677 Compound Info	3-{2-[(2-methoxyphenyl)methyl]-1H-1,3-benzodiazol-6-yl}-1-[4-(piperazin-1-yl)cyclohexyl]-1H-pyrazolo[3,4-d]pyrimidin-4-amine Show/Hide	C30H35N9O	1
1	IC50 = 44 nM
CP0137470 Compound Info	3-{2-[(2-methoxyphenyl)methyl]-1H-1,3-benzodiazol-6-yl}-1-{4-[4-(3-methoxypropyl)piperazin-1-yl]cyclohexyl}-1H-pyrazolo[3,4-d]pyrimidin-4-amine Show/Hide	C34H43N9O2	1
1	IC50 = 54 nM
CP0290732 Compound Info	2-phenyl-N-(3-(5-(2-(1,2,3,4-tetrahydroisoquinolin-6-ylamino)pyrimidin-4-yl)imidazo[2,1-b]thiazol-6-yl)phenyl)acetamide Show/Hide	C32H27N7OS	1
1	IC50 = 55 nM
CP0038067 Compound Info	(S)-N-(1-(3-fluorobenzyl)-1H-indazol-5-yl)-5-((morpholin-2-ylmethoxy)methyl)pyrrolo[1,2-f][1,2,4]triazin-4-amine Show/Hide	C26H26FN7O2	1
1	IC50 = 55 nM
CP0269331 Compound Info	1-{4-[4-(4-amino-3-{2-[(2-methoxyphenyl)methyl]-1H-1,3-benzodiazol-6-yl}-1H-pyrazolo[3,4-d]pyrimidin-1-yl)cyclohexyl]piperazin-1-yl}ethan-1-one Show/Hide	C32H37N9O2	1
1	IC50 = 59 nM
CP0093135 Compound Info	N-[3-[5-[2-(3-morpholin-4-ylanilino)pyrimidin-4-yl]imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-phenylacetamide Show/Hide	C33H29N7O2S	1
1	IC50 = 73 nM
CP0647673 Compound Info	N-[1-(3-Fluoro-benzyl)-1H-indazol-5-yl]-5-(methyl-hydrazonomethyl)-pyrimidine-4,6-diamine Show/Hide	C20H19FN8	1
1	IC50 = 84 nM
CP0187101 Compound Info	N-[1-[(3-fluorophenyl)methyl]indazol-5-yl]-5-methylpyrrolo[2,1-f][1,2,4]triazin-4-amine Show/Hide	C21H17FN6	1
1	IC50 = 88 nM
CP0062383 Compound Info	(6S,7S)-N-hydroxy-6-((R)-3-phenylpyrrolidine-1-carbonyl)-5-azaspiro[2.5]octane-7-carboxamide Show/Hide	C19H25N3O3	1
1	IC50 = 92 nM
CP0178165 Compound Info	N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-1H-pyrrol-2-yl]thieno[3,2-d]pyrimidin-4-amine Show/Hide	C27H25ClFN5O3S2	1
1	IC50 = 113 nM
CP0163869 Compound Info	4-N-[1-[(3-fluorophenyl)methyl]indazol-5-yl]-5-[(4-methoxyphenyl)iminomethyl]pyrimidine-4,6-diamine Show/Hide	C26H22FN7O	1
1	IC50 = 118 nM
CP0037987 Compound Info	N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine Show/Hide	C22H23N3O4	16
1	IC50 = 120 nM
2	IC50 = 134.5 nM
3	IC50 = 160 nM
4	IC50 = 300 nM
5	IC50 = 350 nM
6	IC50 = 369 nM
7	IC50 = 370 nM
8	IC50 = 410 nM
9	IC50 = 513 nM
10	IC50 = 760 nM
11	IC50 = 870 nM
12	IC50 = 3500 nM
13	IC50 > 1000 nM
14	Kd = 2900 nM
15	Kd = 5100 nM
16	Kd > 10000 nM
CP0245707 Compound Info	N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-(1H-pyrrol-2-yl)thieno[3,2-d]pyrimidin-4-amine Show/Hide	C23H16ClFN4OS	1
1	IC50 = 121 nM
CP0294102 Compound Info	N-[3-[5-[2-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-phenylacetamide Show/Hide	C35H34N8OS	1
1	IC50 = 170 nM
CP0036082 Compound Info	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine Show/Hide	C22H24ClFN4O3	9
1	IC50 = 240 nM
2	IC50 = 280 nM
3	IC50 = 281 nM
4	IC50 = 343 nM
5	IC50 = 1000 nM
6	IC50 = 1830 nM
7	IC50 = 2700 nM
8	Kd = 1100 nM
9	Kd = 3500 nM
CP0352335 Compound Info	ethyl 4-[4-(4-amino-3-{2-[(2-methoxyphenyl)methyl]-1H-1,3-benzodiazol-6-yl}-1H-pyrazolo[3,4-d]pyrimidin-1-yl)cyclohexyl]piperazine-1-carboxylate Show/Hide	C33H39N9O3	1
1	IC50 = 270 nM
CP0185838 Compound Info	(2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide Show/Hide	C20H20BrN5O	1
1	IC50 = 301 nM
CP0035538 Compound Info	(6S,7S)-6-(3-phenyl-pyrrolidine-1-carbonyl)-5-aza-spiro[2.5]octane-7-carboxylic acid hydroxyamide Show/Hide	C19H25N3O3	1
1	IC50 = 358 nM
CP0801534 Compound Info	ERLOTINIB HYDROCHLORIDE Show/Hide	C22H24ClN3O4	1
1	IC50 = 1520 nM
CP0429957 Compound Info	1-(5-Bromo-2-hydroxybenzyl)-1-(4-fluorobenzyl)-3-phenylthiourea Show/Hide	C21H18BrFN2OS	1
1	IC50 = 1900 nM
CP0198957 Compound Info	(E)-2-(2-Methyl-5-nitro-1H-imidazol-1-yl)ethyl3-(4-phenyl)acrylate Show/Hide	C21H19N3O4	1
1	IC50 = 2150 nM
CP0176037 Compound Info	1-(3,5-Dibromo-2-hydroxybenzyl)-1-(4-hydroxybenzyl)-3-phenylurea Show/Hide	C21H18Br2N2O3	1
1	IC50 = 4500 nM
CP0230696 Compound Info	9-butyl-8-(3,4,5-trimethoxybenzyl)-9H-purin-6-amine Show/Hide	C19H25N5O3	1
1	IC50 = 40000 nM
CP0061782 Compound Info	N-benzyl-6-[(E)-2-[4-(dimethylamino)phenyl]ethenyl]quinazolin-4-amine Show/Hide	C25H24N4	1
1	Kd = 2900 nM
CP0034906 Compound Info	(R)-1-morpholino-2-(4-(1-(thiazol-2-ylmethyl)-1H-indazol-5-ylamino)quinazolin-5-yloxy)propan-1-one Show/Hide	C26H25N7O3S	1
1	Ki = 2.7 nM

Clinical Information about the Protein

Target 1 ( Erbb2 tyrosine kinase receptor (HER2) )

Target Type	Successful Target
Disease	8 Target-related Diseases				8
1	Non-small-cell lung cancer [ICD-11: 2C25.Y]
2	Breast cancer [ICD-11: 2C60-2C65]
3	Prostate cancer [ICD-11: 2C82.0]
4	Non-hodgkin lymphoma [ICD-11: 2B33.5]
5	HER2-positive breast cancer [ICD-11: 2C60-2C65]
6	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
7	Lymphoma [ICD-11: 2A80-2A86]
8	Metastatic biliary tract neoplasms [ICD-11: 2C14-2C17]
Approved Drug(s)	6 Approved Drugs				6
1	BIBW 2992	Drug Info	Approved	Non-small-cell lung cancer
2	Dacomitinib	Drug Info	Approved	Non-small-cell lung cancer
3	Lapatinib	Drug Info	Approved	Breast cancer
4	Masoprocol	Drug Info	Approved	Prostate cancer
5	Tucatinib	Drug Info	Approved	HER2-positive breast cancer
6	Merimepodib	Drug Info	Approved	Breast cancer
Clinical Trial Drug(s)	12 Clinical Trial Drugs				12
1	HKI-272	Drug Info	Phase 3	Breast cancer
2	Nelipepimut S	Drug Info	Phase 3	Non-hodgkin lymphoma
3	AZD8931	Drug Info	Phase 2	Breast cancer
4	Bevacizumab + Trastuzumab	Drug Info	Phase 3	Breast cancer
5	BMS-599626	Drug Info	Phase 2	Solid tumour/cancer
6	CI-1033	Drug Info	Phase 2	Lymphoma
7	CP-724714	Drug Info	Phase 2	Lymphoma
8	HM-78136B	Drug Info	Phase 2	Solid tumour/cancer
9	Varlitinib	Drug Info	Phase 2/3	Metastatic biliary tract neoplasms
10	ARRY-380	Drug Info	Phase 1	Solid tumour/cancer
11	CUDC-101	Drug Info	Phase 1	Solid tumour/cancer
12	TAK-285	Drug Info	Phase 1	Solid tumour/cancer
Discontinued Drug(s)	2 Discontinued Drugs				2
1	TAK165	Drug Info	Discontinued in Phase 1	Solid tumour/cancer
2	GW-974	Drug Info	Terminated	Breast cancer

Target 2 ( ERBB2 messenger RNA (HER2 mRNA) )

Target Type	Clinical trial Target
Disease	2 Target-related Diseases				2
1	Breast cancer [ICD-11: 2C60-2C65]
2	Chronic pain [ICD-11: MG30]
Clinical Trial Drug(s)	2 Clinical Trial Drugs				2
1	HKI-272	Drug Info	Phase 3	Breast cancer
2	BMS-690514	Drug Info	Phase 2	Chronic pain

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han