Protein Information

General Information of the Protein

Protein ID	PT01203
Protein Name	ALK tyrosine kinase receptor
Secondarily Protein Name	Anaplastic lymphoma kinase
Gene Name	ALK
Sequence	MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSFLLLNTSADSKHTILSPWMRSSSEHCTLAVSVHRHLQPSGRYIAQLLPHNEAAREILLMPTPGKHGWTVLQGRIGRPDNPFRVALEYISSGNRSLSAVDFFALKNCSEGTSPGSKMALQSSFTCWNGTVLQLGQACDFHQDCAQGEDESQMCRKLPVGFYCNFEDGFCGWTQGTLSPHTPQWQVRTLKDARFQDHQDHALLLSTTDVPASESATVTSATFPAPIKSSPCELRMSWLIRGVLRGNVSLVLVENKTGKEQGRMVWHVAAYEGLSLWQWMVLPLLDVSDRFWLQMVAWWGQGSRAIVAFDNISISLDCYLTISGEDKILQNTAPKSRNLFERNPNKELKPGENSPRQTPIFDPTVHWLFTTCGASGPHGPTQAQCNNAYQNSNLSVEVGSEGPLKGIQIWKVPATDTYSISGYGAAGGKGGKNTMMRSHGVSVLGIFNLEKDDMLYILVGQQGEDACPSTNQLIQKVCIGENNVIEEEIRVNRSVHEWAGGGGGGGGATYVFKMKDGVPVPLIIAAGGGGRAYGAKTDTFHPERLENNSSVLGLNGNSGAAGGGGGWNDNTSLLWAGKSLQEGATGGHSCPQAMKKWGWETRGGFGGGGGGCSSGGGGGGYIGGNAASNNDPEMDGEDGVSFISPLGILYTPALKVMEGHGEVNIKHYLNCSHCEVDECHMDPESHKVICFCDHGTVLAEDGVSCIVSPTPEPHLPLSLILSVVTSALVAALVLAFSGIMIVYRRKHQELQAMQMELQSPEYKLSKLRTSTIMTDYNPNYCFAGKTSSISDLKEVPRKNITLIRGLGHGAFGEVYEGQVSGMPNDPSPLQVAVKTLPEVCSEQDELDFLMEALIISKFNHQNIVRCIGVSLQSLPRFILLELMAGGDLKSFLRETRPRPSQPSSLAMLDLLHVARDIACGCQYLEENHFIHRDIAARNCLLTCPGPGRVAKIGDFGMARDIYRASYYRKGGCAMLPVKWMPPEAFMEGIFTSKTDTWSFGVLLWEIFSLGYMPYPSKSNQEVLEFVTSGGRMDPPKNCPGPVYRIMTQCWQHQPEDRPNFAIILERIEYCTQDPDVINTALPIEYGPLVEEEEKVPVRPKDPEGVPPLLVSQQAKREEERSPAAPPPLPTTSSGKAAKKPTAAEISVRVPRGPAVEGGHVNMAFSQSNPPSELHKVHGSRNKPTSLWNPTYGSWFTEKPTKKNNPIAKKEPHDRGNLGLEGSCTVPPNVATGRLPGASLLLEPSSLTANMKEVPLFRLRHFPCGNVNYGYQQQGLPLEAATAPGAGHYEDTILKSKNSMNQPGP Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Kinase > Protein Kinase > TKL protein kinase group > TKL protein kinase STKR family > TKL protein kinase STKR Type 1 subfamily
Function	Neuronal receptor tyrosine kinase that is essentially and transiently expressed in specific regions of the central and peripheral nervous systems and plays an important role in the genesis and differentiation of the nervous system (PubMed:11121404, PubMed:11387242, PubMed:16317043, PubMed:17274988, PubMed:30061385, PubMed:34646012, PubMed:34819673). Also acts as a key thinness protein involved in the resistance to weight gain: in hypothalamic neurons, controls energy expenditure acting as a negative regulator of white adipose tissue lipolysis and sympathetic tone to fine-tune energy homeostasis (By similarity). Following activation by ALKAL2 ligand at the cell surface, transduces an extracellular signal into an intracellular response (PubMed:30061385, PubMed:33411331, PubMed:34646012, PubMed:34819673). In contrast, ALKAL1 is not a potent physiological ligand for ALK (PubMed:34646012). Ligand-binding to the extracellular domain induces tyrosine kinase activation, leading to activation of the mitogen-activated protein kinase (MAPK) pathway (PubMed:34819673). Phosphorylates almost exclusively at the first tyrosine of the Y-x-x-x-Y-Y motif (PubMed:15226403, PubMed:16878150). Induces tyrosine phosphorylation of CBL, FRS2, IRS1 and SHC1, as well as of the MAP kinases MAPK1/ERK2 and MAPK3/ERK1 (PubMed:15226403, PubMed:16878150). ALK activation may also be regulated by pleiotrophin (PTN) and midkine (MDK) (PubMed:11278720, PubMed:11809760, PubMed:12107166, PubMed:12122009). PTN-binding induces MAPK pathway activation, which is important for the anti-apoptotic signaling of PTN and regulation of cell proliferation (PubMed:11278720, PubMed:11809760, PubMed:12107166). MDK-binding induces phosphorylation of the ALK target insulin receptor substrate (IRS1), activates mitogen-activated protein kinases (MAPKs) and PI3-kinase, resulting also in cell proliferation induction (PubMed:12122009). Drives NF-kappa-B activation, probably through IRS1 and the activation of the AKT serine/threonine kinase (PubMed:15226403, PubMed:16878150). Recruitment of IRS1 to activated ALK and the activation of NF-kappa-B are essential for the autocrine growth and survival signaling of MDK (PubMed:15226403, PubMed:16878150). Show/Hide
Uniprot ID	Primary ID: Q9UM73 Secondarily ID: A6P4T4 A6P4V4 Q4ZFX9 Q53QQ6 Q53RZ4 Q59FI3 Q9Y4K6 Show/Hide
Ensembl ID	ENSG00000171094
HGNC ID	HGNC:427
Subcellular Location	Cell 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: CL000077 , Ba/F3

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0871866 Compound Info	N-(5-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide Show/Hide	C29H36ClN7O4S	4
1	GI50 = 1 nM Bioactivity Info	TI LI LO TS
2	GI50 = 6.9 nM Bioactivity Info	TI LI LO TS
3	GI50 = 29 nM Bioactivity Info	TI LI LO TS
4	GI50 = 460 nM Bioactivity Info	TI LI LO TS
CP0031719 Compound Info	(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine Show/Hide	C21H22Cl2FN5O	6
1	GI50 = 150 nM Bioactivity Info	TI LI LO TS
2	GI50 = 320 nM Bioactivity Info	TI LI LO TS
3	GI50 = 430 nM Bioactivity Info	TI LI LO TS
4	GI50 = 590 nM Bioactivity Info	TI LI LO TS
5	IC50 = 150.8 nM Bioactivity Info	TI LI LO TS
6	IC50 = 260 nM Bioactivity Info	TI LI LO TS
CP0019908 Compound Info	BDBM50242742 Show/Hide	C30H40ClN7O3S	2
1	IC50 = 3.7 nM Bioactivity Info	TI LI LO TS
2	IC50 = 4 nM Bioactivity Info	TI LI LO TS
CP0195200 Compound Info	2-[4-[4-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-2-methyl-5-propan-2-yloxyphenyl]piperidin-1-yl]ethanol Show/Hide	C30H40ClN5O4S	1
1	IC50 = 8.1 nM Bioactivity Info	TI LI LO TS
CP0225633 Compound Info	5-chloro-2-N-(4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C27H34ClN5O3S	1
1	IC50 = 10.6 nM Bioactivity Info	TI LI LO TS
CP0100657 Compound Info	5-chloro-2-N-[5-methyl-4-(1-methylpiperidin-4-yl)-2-propan-2-yloxyphenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C29H38ClN5O3S	1
1	IC50 = 11.5 nM Bioactivity Info	TI LI LO TS
CP0116539 Compound Info	5-methyl-2-N-[5-methyl-4-(1-methylpiperidin-4-yl)-2-propan-2-yloxyphenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C30H41N5O3S	1
1	IC50 = 14.6 nM Bioactivity Info	TI LI LO TS
CP0375645 Compound Info	2-[4-[4-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-2-methyl-5-propan-2-yloxyphenyl]piperidin-1-yl]acetamide Show/Hide	C30H39ClN6O4S	1
1	IC50 = 16.5 nM Bioactivity Info	TI LI LO TS
CP0056941 Compound Info	5-chloro-2-N-(2-cyclobutyloxy-5-methyl-4-piperidin-4-ylphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C29H36ClN5O3S	1
1	IC50 = 17.3 nM Bioactivity Info	TI LI LO TS
CP0149293 Compound Info	5-chloro-2-N-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]-2-propan-2-yloxyphenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C32H44ClN7O3S	1
1	IC50 = 24.8 nM Bioactivity Info	TI LI LO TS
CP0375646 Compound Info	2-[[5-chloro-2-[5-methyl-4-(1-methylpiperidin-4-yl)-2-propan-2-yloxyanilino]pyrimidin-4-yl]amino]-N,N-dimethylbenzenesulfonamide Show/Hide	C28H37ClN6O3S	1
1	IC50 = 25 nM Bioactivity Info	TI LI LO TS
CP0271938 Compound Info	1-[4-[4-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-2-methyl-5-propan-2-yloxyphenyl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C32H43ClN6O4S	1
1	IC50 = 25.8 nM Bioactivity Info	TI LI LO TS
CP0013877 Compound Info	CERITINIB Show/Hide	C28H36ClN5O3S	1
1	IC50 = 26 nM Bioactivity Info	TI LI LO TS
CP0433493 Compound Info	2-N-[4-(1-ethylpiperidin-4-yl)-5-methyl-2-propan-2-yloxyphenyl]-5-methyl-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C31H43N5O3S	1
1	IC50 = 29.4 nM Bioactivity Info	TI LI LO TS
CP0403909 Compound Info	5-chloro-2-N-[5-methyl-2-propan-2-yloxy-4-(1-propan-2-ylpiperidin-4-yl)phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C31H42ClN5O3S	1
1	IC50 = 29.9 nM Bioactivity Info	TI LI LO TS
CP0375885 Compound Info	5-chloro-2-N-[4-(1-ethylpiperidin-4-yl)-5-methyl-2-propan-2-yloxyphenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C30H40ClN5O3S	1
1	IC50 = 32.1 nM Bioactivity Info	TI LI LO TS
CP0195203 Compound Info	5-chloro-2-N-(2-piperidin-4-yl-4-propan-2-yloxypyrimidin-5-yl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C25H32ClN7O3S	1
1	IC50 = 36.4 nM Bioactivity Info	TI LI LO TS
CP0524058 Compound Info	5-chloro-4-N-(2-cyclobutylsulfonylphenyl)-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)pyrimidine-2,4-diamine Show/Hide	C29H36ClN5O3S	1
1	IC50 = 38.1 nM Bioactivity Info	TI LI LO TS
CP0396302 Compound Info	5-methyl-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C29H39N5O3S	1
1	IC50 = 40.6 nM Bioactivity Info	TI LI LO TS
CP0482379 Compound Info	5-chloro-2-N-[4-[1-(2-methoxyethyl)piperidin-4-yl]-5-methyl-2-propan-2-yloxyphenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C31H42ClN5O4S	1
1	IC50 = 43.5 nM Bioactivity Info	TI LI LO TS
CP0433492 Compound Info	2-N-[4-[1-(2-methoxyethyl)piperidin-4-yl]-5-methyl-2-propan-2-yloxyphenyl]-5-methyl-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C32H45N5O4S	1
1	IC50 = 44 nM Bioactivity Info	TI LI LO TS
CP0396301 Compound Info	4-[4-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-2-methyl-5-propan-2-yloxyphenyl]piperidin-2-one Show/Hide	C28H34ClN5O4S	1
1	IC50 = 48.3 nM Bioactivity Info	TI LI LO TS
CP0463943 Compound Info	2-[4-[2-methyl-4-[[5-methyl-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-5-propan-2-yloxyphenyl]piperidin-1-yl]ethanol Show/Hide	C31H43N5O4S	1
1	IC50 = 63.6 nM Bioactivity Info	TI LI LO TS
CP0407620 Compound Info	2-[4-[4-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-2-methyl-5-propan-2-yloxyphenyl]piperidin-1-yl]acetic acid Show/Hide	C30H38ClN5O5S	1
1	IC50 = 88.9 nM Bioactivity Info	TI LI LO TS
CP0529547 Compound Info	4,7-bis[4-(4-methylpiperazin-1-yl)phenyl]pyrazino[1,2-a]benzimidazole Show/Hide	C32H35N7	1
1	IC50 = 200 nM Bioactivity Info	TI LI LO TS
CP0442082 Compound Info	5-chloro-2-N-[5-methyl-4-[1-(1-methylpiperidin-4-yl)piperidin-4-yl]-2-propan-2-yloxyphenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C34H47ClN6O3S	1
1	IC50 = 258.4 nM Bioactivity Info	TI LI LO TS
CP0375640 Compound Info	5-chloro-2-N-[4-[1-(2,2-difluoroethyl)piperidin-4-yl]-5-methyl-2-propan-2-yloxyphenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Show/Hide	C30H38ClF2N5O3S	1
1	IC50 = 305.7 nM Bioactivity Info	TI LI LO TS
CP0508593 Compound Info	7-(4-methoxyphenyl)-4-[(E)-2-phenylethenyl]pyrazino[1,2-a]benzimidazole Show/Hide	C25H19N3O	1
1	IC50 = 780 nM Bioactivity Info	TI LI LO TS
CP0385508 Compound Info	2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid Show/Hide	C27H28FN7O2	2
1	IC50 = 1200 nM Bioactivity Info	TI LI LO TS
2	IC50 = 2200 nM Bioactivity Info	TI LI LO TS
CP0484609 Compound Info	7-bromo-4-chloropyrazino[1,2-a]benzimidazole Show/Hide	C10H5BrClN3	1
1	IC50 = 2200 nM Bioactivity Info	TI LI LO TS
CP0385511 Compound Info	1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol Show/Hide	C26H27FN6O	2
1	IC50 = 3000 nM Bioactivity Info	TI LI LO TS
2	IC50 = 3900 nM Bioactivity Info	TI LI LO TS
CP0661487 Compound Info	3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate Show/Hide	C26H34Cl2N7O7P	1
1	IC50 = 3078 nM Bioactivity Info	TI LI LO TS
CP0388864 Compound Info	4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile Show/Hide	C20H15N5	2
1	IC50 = 3100 nM Bioactivity Info	TI LI LO TS
2	IC50 = 4800 nM Bioactivity Info	TI LI LO TS
CP0482380 Compound Info	5-chloro-2-N-[5-methyl-4-(1-methylpiperidin-4-yl)-2-propan-2-yloxyphenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyridine-2,4-diamine Show/Hide	C30H39ClN4O3S	1
1	IC50 = 4240 nM Bioactivity Info	TI LI LO TS
CP0395047 Compound Info	6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]-3-pyridin-2-ylimidazo[1,2-b]pyridazine Show/Hide	C21H18FN5	1
1	IC50 = 6300 nM Bioactivity Info	TI LI LO TS
CP0484608 Compound Info	8-bromo-3-(4-methoxyphenyl)pyrimido[1,6-a]benzimidazole Show/Hide	C17H12BrN3O	1
1	IC50 = 9000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000300 , Karpas-299

Cell Line Info

Cell Line ID: CL000727 , Kelly

Cell Line Info

Cell Line ID: CL000469 , NCI-H2228

Cell Line Info

Cell Line ID: CL000320 , NCI-H3122

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: CL000299 , SU-DHL-1

Cell Line Info

Cell Line ID: CL000427 , SUP-M2

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0031719 Compound Info	(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine Show/Hide	C21H22Cl2FN5O	39
1	EC50 = 0.47 nM
2	IC50 = 0.64 nM
3	IC50 < 1 nM
4	IC50 = 2.47 nM
5	IC50 = 2.6 nM
6	IC50 = 3.33 nM
7	IC50 = 4.5 nM
8	IC50 = 4.66 nM
9	IC50 = 5.012 nM
10	IC50 = 7 nM
11	IC50 = 10.5 nM
12	IC50 = 12 nM
13	IC50 = 13 nM
14	IC50 = 13.7 nM
15	IC50 = 16 nM
16	IC50 = 20 nM
17	IC50 = 23.6 nM
18	IC50 = 24 nM
19	IC50 = 25 nM
20	IC50 = 28 nM
21	IC50 = 30 nM
22	IC50 = 32 nM
23	IC50 = 52 nM
24	IC50 = 71.6 nM
25	IC50 = 73.6 nM
26	IC50 = 77.8 nM
27	IC50 = 122 nM
28	IC50 = 148 nM
29	IC50 = 200 nM
30	IC50 = 353 nM
31	IC50 = 355 nM
32	IC50 = 600 nM
33	IC50 = 891 nM
34	IC50 = 972 nM
35	IC50 > 9000 nM
36	Kd = 3.3 nM
37	Kd = 4.4 nM
38	Ki = 0.74 nM
39	Ki = 8.2 nM
CP0019908 Compound Info	BDBM50242742 Show/Hide	C30H40ClN7O3S	5
1	EC50 = 3 nM
2	IC50 = 0.15 nM
3	IC50 = 1.6 nM
4	IC50 = 3 nM
5	Kd = 1.1 nM
CP0013877 Compound Info	CERITINIB Show/Hide	C28H36ClN5O3S	27
1	IC50 = 0.2 nM
2	IC50 = 0.25 nM
3	IC50 < 1 nM
4	IC50 = 2.1 nM
5	IC50 = 2.3 nM
6	IC50 = 2.4 nM
7	IC50 = 2.6 nM
8	IC50 = 2.9 nM
9	IC50 = 3.1 nM
10	IC50 = 3.3 nM
11	IC50 = 3.4 nM
12	IC50 = 3.94 nM
13	IC50 = 4.2 nM
14	IC50 = 7.4 nM
15	IC50 = 10.3 nM
16	IC50 = 14 nM
17	IC50 = 20 nM
18	IC50 = 27 nM
19	IC50 = 29 nM
20	IC50 = 35 nM
21	IC50 = 47.65 nM
22	IC50 = 80 nM
23	IC50 = 112 nM
24	IC50 = 114.3 nM
25	IC50 = 197 nM
26	IC50 = 198 nM
27	Ki = 3700 nM
CP0073076 Compound Info	(2R)-2-[5-[6-amino-5-[(1R)-1-[5-fluoro-2-(triazol-2-yl)phenyl]ethoxy]pyridin-3-yl]-4-methyl-1,3-thiazol-2-yl]propane-1,2-diol Show/Hide	C22H23FN6O3S	1
1	IC50 = 0.2 nM
CP0659262 Compound Info	(1S,2S,3R,4R)-3-{6-Chloro-2-[2-methoxy-4-(4-morpholin-4-yl-piperidin-1-yl)-phenyl]-3H-imidazo[4,5-b]pyridin-7-ylamino}-bicyclo[2.2.1]hept-5-ene-2-carboxylicacidamide Show/Hide	C30H36ClN7O3	1
1	IC50 = 0.31 nM
CP0545653 Compound Info	US9126947, 18 Show/Hide	C26H27Cl2FN6O3	1
1	IC50 < 0.4 nM
CP0083616 Compound Info	6-[6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]pyridin-3-yl]-1'-methylspiro[1H-indole-3,4'-piperidine]-2-one Show/Hide	C26H25Cl2FN4O2	1
1	IC50 < 0.5 nM
CP0078581 Compound Info	N-[6-chloro-19-methoxy-17-(4-methylpiperazin-1-yl)-2,4,8,22-tetrazatetracyclo[14.3.1.13,7.19,13]docosa-1(19),3,5,7(22),9,11,13(21),16(20),17-nonaen-10-yl]-N-methylmethanesulfonamide Show/Hide	C26H32ClN7O3S	1
1	IC50 = 0.51 nM
CP0842622 Compound Info	(1S,2S,3R,4R)-3-{6-Chloro-2-[2-methoxy-4-(4-methyl-piperazin-1-ylmethyl)-phenyl]-3H-imidazo[4,5-b]pyridin-7-ylamino}-bicyclo[2.2.1]hept-5-ene-2-carboxylicacidamide Show/Hide	C27H32ClN7O2	1
1	IC50 = 0.65 nM
CP0704533 Compound Info	(1S,2S,3R,4R)-3-{6-Chloro-2-[2-methoxy-4-(4-methyl-piperazin-1-yl)-phenyl]-3Himidazo[4,5-b]pyridin-7-ylamino}-bicyclo[2.2.1]hept-5-ene-2-carboxylic Show/Hide	C26H30ClN7O2	1
1	IC50 = 0.69 nM
CP0135794 Compound Info	(17R)-20-amino-14-fluoro-5,9,17-trimethyl-10-oxo-18-oxa-5,6,9,21-tetrazatetracyclo[17.3.1.03,7.011,16]tricosa-1(23),3,6,11(16),12,14,19,21-octaene-4-carbonitrile Show/Hide	C22H21FN6O2	5
1	IC50 = 0.7 nM
2	IC50 = 1.01 nM
3	IC50 = 77 nM
4	Ki < 0.02 nM
5	Ki = 0.7 nM
CP0762036 Compound Info	(1S,2S,3R,4R)-3-(6-Chloro-2-{2-methoxy-4-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-phenyl}-3H-imidazo[4,5-b]pyridin-7-ylamino)-bicyclo[2.2.1]hept-5-ene-2-carboxylicacidamide Show/Hide	C31H39ClN8O2	1
1	IC50 = 0.76 nM
CP0346931 Compound Info	2-[[5-chloro-2-[(1-methyl-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]-N-methylbenzenesulfonamide Show/Hide	C22H23ClN6O3S	1
1	IC50 = 1 nM
CP0742340 Compound Info	4-Fluoro-5-isopropyl-2-methoxy-11-oxo-3-(cis-3,4,5-trimethylpiperazin-1-yl)-6,11-dihydro-5H-indolo[2,3-b]quinoline-8-carbonitrile Show/Hide	C27H30FN5O2	3
1	IC50 = 1.2 nM
2	IC50 = 4.8 nM
3	IC50 = 5.6 nM
CP0031589 Compound Info	Gilteritinib Show/Hide	C29H44N8O3	1
1	IC50 = 1.2 nM
CP0110196 Compound Info	6-chloro-19-methoxy-17-(4-methylpiperazin-1-yl)-10-propan-2-ylsulfonyl-2,4,8,22-tetrazatetracyclo[14.3.1.13,7.19,13]docosa-1(19),3,5,7(22),9,11,13(21),16(20),17-nonaene Show/Hide	C27H33ClN6O3S	1
1	IC50 = 1.5 nM
CP0066933 Compound Info	1256580-46-7 Show/Hide	C30H34N4O2	7
1	IC50 = 1.56 nM
2	IC50 = 1.9 nM
3	IC50 = 2.07 nM
4	IC50 = 5.3 nM
5	IC50 = 11.5 nM
6	IC50 = 15.2 nM
7	IC50 = 1030 nM
CP0095494 Compound Info	9-ethyl-6,6-dimethyl-8-[1-(oxane-4-carbonyl)-3,6-dihydro-2H-pyridin-4-yl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile Show/Hide	C32H33N3O3	2
1	IC50 = 1.7 nM
2	IC50 = 18 nM
CP0199533 Compound Info	9-ethyl-6,6-dimethyl-8-[1-(oxan-4-ylmethyl)-3,6-dihydro-2H-pyridin-4-yl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile Show/Hide	C32H35N3O2	2
1	IC50 = 2.3 nM
2	IC50 = 11.2 nM
CP0336558 Compound Info	7-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-1-ethyl-8-methoxy-4,5-dihydro-3H-1-benzazepin-2-one Show/Hide	C26H30ClN5O4S	1
1	IC50 = 2.7 nM
CP0659259 Compound Info	(1S,2S,3R,4R)-3-{6-Bromo-2-[4-(4-methyl-piperazin-1-yl)-phenyl]-3H-imidazo[4,5-b]pyridin-7-ylamino}-bicyclo[2.2.1]hept-5-ene-2-carboxylicacidamide Show/Hide	C25H28BrN7O	1
1	IC50 = 2.7 nM
CP0036509 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[[7-methoxy-3-(2-methoxyethyl)-1,2,4,5-tetrahydro-3-benzazepin-8-yl]amino]pyrimidin-4-yl]amino]cyclohexyl]-N-methylmethanesulfonamide Show/Hide	C26H39ClN6O4S	1
1	IC50 = 3 nM
CP0103867 Compound Info	6-chloro-10-methoxy-17-(4-methylpiperazin-1-yl)-2,4,8,22-tetrazatetracyclo[14.3.1.13,7.19,13]docosa-1(20),3,5,7(22),9,11,13(21),16,18-nonaene Show/Hide	C24H27ClN6O	1
1	IC50 = 3.1 nM
CP0110195 Compound Info	N-[6-chloro-17-(4-methylpiperazin-1-yl)-2,4,8,22-tetrazatetracyclo[14.3.1.13,7.19,13]docosa-1(20),3,5,7(22),9,11,13(21),16,18-nonaen-10-yl]-N-methylmethanesulfonamide Show/Hide	C25H30ClN7O2S	1
1	IC50 = 3.4 nM
CP0054448 Compound Info	6,6-dimethyl-8-[1-(oxan-4-ylmethyl)piperidin-4-yl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile Show/Hide	C30H33N3O2	7
1	IC50 = 3.4 nM
2	IC50 = 3.7 nM
3	IC50 = 3.9 nM
4	IC50 = 7.6 nM
5	IC50 = 8.1 nM
6	IC50 = 8.5 nM
7	IC50 = 38.1 nM
CP0285873 Compound Info	6-chloro-17-(4-methylpiperazin-1-yl)-10-propan-2-ylsulfonyl-2,4,8,22-tetrazatetracyclo[14.3.1.13,7.19,13]docosa-1(20),3,5,7(22),9,11,13(21),16,18-nonaene Show/Hide	C26H31ClN6O2S	1
1	IC50 = 3.7 nM
CP0081541 Compound Info	2-(7-(5-chloro-4-(2-methoxy-4-morpholinophenylamino)pyrimidin-2-ylamino)-8-methoxy-4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-N,N-dimethylacetamide Show/Hide	C30H38ClN7O4	1
1	IC50 = 4 nM
CP0338834 Compound Info	2-[[5-chloro-2-[(1-ethyl-8-methoxy-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]-N,N-dimethylbenzenesulfonamide Show/Hide	C25H29ClN6O4S	1
1	IC50 = 4 nM
CP0769733 Compound Info	(1S,2S,3R,4R)-3-{6-Chloro-2-[4-(4-methyl-piperazin-1-yl)-phenyl]-3H-imidazo[4,5-b]pyridin-7-ylamino}-bicyclo[2.2.1]hept-5-ene-2-carboxylicacidamide Show/Hide	C25H28ClN7O	1
1	IC50 = 4 nM
CP0715175 Compound Info	4-((4-(3-chloro-2,6-difluorobenzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H16ClF2N5O2S	1
1	IC50 = 5 nM
CP0078539 Compound Info	6-chloro-19-methoxy-17-(4-methylpiperazin-1-yl)-2,4,8,22-tetrazatetracyclo[14.3.1.13,7.19,13]docosa-1(19),3,5,7(22),9,11,13(21),16(20),17-nonaene Show/Hide	C24H27ClN6O	1
1	IC50 = 5 nM
CP0338378 Compound Info	7-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-1-ethyl-6-methoxy-4,5-dihydro-3H-1-benzazepin-2-one Show/Hide	C26H30ClN5O4S	1
1	IC50 = 5 nM
CP0338383 Compound Info	2-[[5-chloro-2-[(1-ethyl-8-methoxy-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]-N-methylbenzamide Show/Hide	C25H27ClN6O3	1
1	IC50 = 5 nM
CP0227700 Compound Info	3-[1-[(3-fluorophenyl)methyl]pyrazol-4-yl]-5-(1-methylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine Show/Hide	C21H17FN6	2
1	IC50 = 5.6 nM
2	IC50 = 35 nM
CP0038262 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[[7-methoxy-3-(2-methoxyethyl)-1,2,4,5-tetrahydro-3-benzazepin-8-yl]amino]pyrimidin-4-yl]amino]cyclohexyl]methanesulfonamide Show/Hide	C25H37ClN6O4S	1
1	IC50 = 6 nM
CP0842621 Compound Info	(1S,2S,3R,4R)-3-[6-Chloro-2-(2-methoxy-4-morpholin-4-ylmethyl-phenyl)-3Himidazo[4,5-b]pyridin-7-ylamino]-bicyclo[2.2.1]hept-5-ene-2-carboxylicacidamide Show/Hide	C26H29ClN6O3	1
1	IC50 = 6.7 nM
CP0275596 Compound Info	5-chloro-N2-(8-methoxy-3-(2-methoxyethyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)-N4-(2-methoxy-4-morpholinophenyl)pyrimidine-2,4-diamine Show/Hide	C29H37ClN6O4	1
1	IC50 = 7 nM
CP0103868 Compound Info	N-[6-chloro-19-methoxy-17-(4-methylpiperazin-1-yl)-2,4,8,22-tetrazatetracyclo[14.3.1.13,7.19,13]docosa-1(19),2,5,7,9,11,13(21),14,16(20),17-decaen-10-yl]-N-methylmethanesulfonamide Show/Hide	C26H30ClN7O3S	1
1	IC50 = 7 nM
CP0271214 Compound Info	(1S,2S,3R,4R)-3-[[5-chloro-2-[(1-ethyl-8-methoxy-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Show/Hide	C25H29ClN6O3	1
1	IC50 = 7 nM
CP0769350 Compound Info	(1S,2S,3R,4R)-3-[6-Chloro-2-(2-methoxy-4-morpholin-4-yl-phenyl)-3H-imidazo[4,5-b]pyridin-7-ylamino]-bicyclo[2.2.1]hept-5-ene-2-carboxylicacidamide Show/Hide	C25H27ClN6O3	1
1	IC50 = 7 nM
CP0346930 Compound Info	2-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]-N,N-dimethylbenzenesulfonamide Show/Hide	C25H29ClN6O4S	1
1	IC50 = 8 nM
CP0140927 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[(3-ethyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]cyclohexyl]acetamide Show/Hide	C24H33ClN6O	1
1	IC50 = 9 nM
CP0152147 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[[3-(2-methoxyethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]amino]pyrimidin-4-yl]amino]cyclohexyl]methanesulfonamide Show/Hide	C24H35ClN6O3S	1
1	IC50 = 9 nM
CP0251297 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[(3-ethyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]cyclohexyl]methanesulfonamide Show/Hide	C23H33ClN6O2S	1
1	IC50 = 9 nM
CP0252857 Compound Info	(4Z)-4-[[4-[(2,6-difluorophenyl)methoxy]-1-methylindol-3-yl]methylidene]-3-(1,3-thiazol-2-yl)-1H-pyrazol-5-one Show/Hide	C23H16F2N4O2S	1
1	IC50 = 9 nM
CP0035364 Compound Info	1-(5-Chloro-2-trifluoromethyl-benzyl)-7-(2-piperazin-1-yl-pyridin-4-yl)-1,2,3,4-tetrahydro-pyrido[2,3-b]pyrazine Show/Hide	C24H24ClF3N6	1
1	IC50 = 10 nM
CP0037714 Compound Info	[4-[1-[[5-chloro-2-(trifluoromethyl)phenyl]methyl]-3,4-dihydro-2H-pyrido[2,3-b]pyrazin-7-yl]phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone Show/Hide	C31H33ClF3N5O	1
1	IC50 = 10 nM
CP0071846 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]cyclohexyl]methanesulfonamide Show/Hide	C22H31ClN6O4S	1
1	IC50 = 10 nM
CP0268098 Compound Info	N-[2-[2-[4-[4-[(2S)-2-hydroxypropyl]piperazin-1-yl]-2-methoxyanilino]pyrrolo[2,1-f][1,2,4]triazin-7-yl]phenyl]-N-methylmethanesulfonamide Show/Hide	C28H35N7O4S	1
1	IC50 = 10 nM
CP0480102 Compound Info	2-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]-N-methylbenzamide Show/Hide	C25H27ClN6O3	1
1	IC50 = 11 nM
CP0704217 Compound Info	4-((4-(2,6-difluorobenzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H17F2N5O2S	1
1	IC50 = 12 nM
CP0734366 Compound Info	4-((4-(4-fluorobenzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H18FN5O2S	1
1	IC50 = 12 nM
CP0756199 Compound Info	4-((4-(2,4-difluorobenzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H17F2N5O2S	1
1	IC50 = 12 nM
CP0209390 Compound Info	(4Z)-4-[[4-[(2-chloro-6-fluorophenyl)methoxy]-1-methylindol-3-yl]methylidene]-3-(1,3-thiazol-2-yl)-1H-pyrazol-5-one Show/Hide	C23H16ClFN4O2S	1
1	IC50 = 13 nM
CP0715174 Compound Info	4-((4-(2-fluorobenzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H18FN5O2S	1
1	IC50 = 13 nM
CP0236924 Compound Info	(4Z)-4-[[4-[(2,3-difluorophenyl)methoxy]-1-methylindol-3-yl]methylidene]-3-(1,3-thiazol-2-yl)-1H-pyrazol-5-one Show/Hide	C23H16F2N4O2S	1
1	IC50 = 14 nM
CP0737082 Compound Info	4-((4-(2-chloro-3,6-difluorobenzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H16ClF2N5O2S	1
1	IC50 = 14 nM
CP0050160 Compound Info	(1S,2S,3R,4R)-3-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Show/Hide	C25H29ClN6O3	1
1	IC50 = 14 nM
CP0232915 Compound Info	(17R)-20-amino-14-fluoro-4,6,9,17-tetramethyl-18-oxa-5,6,9,21-tetrazatetracyclo[17.3.1.03,7.011,16]tricosa-1(23),3(7),4,11(16),12,14,19,21-octaen-10-one Show/Hide	C22H24FN5O2	1
1	IC50 = 14 nM
CP0036597 Compound Info	2-[5-Chloro-2-(1-methyl-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-7-ylamino)-pyrimidin-4-ylamino]-N-methyl-benzamide Show/Hide	C23H23ClN6O2	1
1	IC50 = 15 nM
CP0704531 Compound Info	(1S,2S,3R,4R)-3-[6-Chloro-2-(2-methoxy-phenyl)-3H-imidazo[4,5-b]pyridine-7-ylamino]-bicyclo[2.2.1]hept-5-ene-2-carboxylicacidamide Show/Hide	C21H20ClN5O2	1
1	IC50 = 16 nM
CP0039200 Compound Info	1-[4-(4-{1-[5-Chloro-2-(trifluoromethyl)benzyl]-1,2,3,4-tetrahydro-pyrido[2,3-b]pyrazin-7-yl}pyridin-2-yl)piperazin-1-yl]ethanone Show/Hide	C26H26ClF3N6O	1
1	IC50 = 17 nM
CP0167905 Compound Info	(4Z)-4-[[4-[(2,5-difluorophenyl)methoxy]-1-methylindol-3-yl]methylidene]-3-(1,3-thiazol-2-yl)-1H-pyrazol-5-one Show/Hide	C23H16F2N4O2S	1
1	IC50 = 17 nM
CP0134636 Compound Info	(7R)-2-[2-ethoxy-4-(1-methylpiperidin-4-yl)anilino]-7-ethyl-5-methyl-8-[(4-methylthiophen-2-yl)methyl]-7H-pteridin-6-one Show/Hide	C29H38N6O2S	1
1	IC50 = 17 nM
CP0346929 Compound Info	(1S,2S,3R,4R)-3-[[5-chloro-2-[(1-methyl-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Show/Hide	C23H25ClN6O2	1
1	IC50 = 18 nM
CP0290762 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[[7-methoxy-3-(2-methoxyethyl)-1,2,4,5-tetrahydro-3-benzazepin-8-yl]amino]pyrimidin-4-yl]amino]cyclohexyl]-N-ethylmethanesulfonamide Show/Hide	C27H41ClN6O4S	1
1	IC50 = 20 nM
CP0777159 Compound Info	4-((4-(3-fluorobenzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H18FN5O2S	1
1	IC50 = 20 nM
CP0672164 Compound Info	4-((4-(2-chloro-6-fluorobenzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H17ClFN5O2S	1
1	IC50 = 21 nM
CP0347900 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[[3-(2-methoxyethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]amino]pyrimidin-4-yl]amino]cyclohexyl]-2,2,2-trifluoroacetamide Show/Hide	C25H32ClF3N6O2	1
1	IC50 = 22 nM
CP0170188 Compound Info	5-chloro-4-N-(2-methoxyphenyl)-2-N-[4-(4-methylpiperazin-1-yl)phenyl]pyrimidine-2,4-diamine Show/Hide	C22H25ClN6O	1
1	IC50 = 22 nM
CP0734367 Compound Info	4-((4-(benzyloxy)-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C23H19N5O2S	1
1	IC50 = 23 nM
CP0069842 Compound Info	(4Z)-4-[[4-[(3-fluorophenyl)methoxy]-1-methylindol-3-yl]methylidene]-3-(1,3-thiazol-2-yl)-1H-pyrazol-5-one Show/Hide	C23H17FN4O2S	1
1	IC50 = 25 nM
CP0140924 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[(3-ethyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]cyclohexyl]-2,2,2-trifluoroacetamide Show/Hide	C24H30ClF3N6O	1
1	IC50 = 26 nM
CP0271938 Compound Info	1-[4-[4-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-2-methyl-5-propan-2-yloxyphenyl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C32H43ClN6O4S	1
1	IC50 = 26 nM
CP0262545 Compound Info	3-[1-[(2,5-difluorophenyl)methyl]pyrazol-4-yl]-5-(1-methylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine Show/Hide	C21H16F2N6	2
1	IC50 = 29 nM
2	IC50 = 124 nM
CP0076949 Compound Info	3-[1-[(3-chlorophenyl)methyl]pyrazol-4-yl]-5-(1-methylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine Show/Hide	C21H17ClN6	2
1	IC50 = 30 nM
2	IC50 = 143 nM
CP0206735 Compound Info	N-[(1R,2R)-2-[[5-chloro-2-[[3-(2-methoxyethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]amino]pyrimidin-4-yl]amino]cyclohexyl]-2,2,2-trifluoroethanesulfonamide Show/Hide	C25H34ClF3N6O3S	1
1	IC50 = 31 nM
CP0066087 Compound Info	1-(2,5-Difluoro-benzyl)-7-[6-(4-methyl-piperazin-1-yl)-pyridin-3-yl]-1,2,3,4-tetrahydro-pyrido[2,3-b]pyrazine Show/Hide	C24H26F2N6	1
1	IC50 = 33 nM
CP0715173 Compound Info	3-(4-methyl-1,2,3-thiadiazol-5-yl)-4-((1-methyl-4-(pyridin-3-ylmethoxy)-1H-indol-3-yl)methylene)-1H-pyrazol-5(4H)-one Show/Hide	C22H18N6O2S	1
1	IC50 = 34 nM
CP0283340 Compound Info	6-chloro-N-methyl-17-(4-methylpiperazin-1-yl)-2,4,8,22-tetrazatetracyclo[14.3.1.13,7.19,13]docosa-1(20),3,5,7(22),9,11,13(21),16,18-nonaene-10-carboxamide Show/Hide	C25H28ClN7O	1
1	IC50 = 35 nM
CP0037704 Compound Info	[4-[1-[[5-chloro-2-(trifluoromethyl)phenyl]methyl]-3,4-dihydro-2H-pyrido[2,3-b]pyrazin-7-yl]phenyl]-(4-methoxypiperidin-1-yl)methanone Show/Hide	C28H28ClF3N4O2	1
1	IC50 = 40 nM
CP0043422 Compound Info	4-[6-amino-7-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]furo[3,2-c]pyridin-3-yl]-3,6-dihydro-2H-pyridine-1-carboxamide Show/Hide	C21H19Cl2FN4O3	1
1	IC50 = 40 nM
CP0204513 Compound Info	(4Z)-4-[[1-methyl-4-(1-phenylethoxy)indol-3-yl]methylidene]-3-(1,3-thiazol-2-yl)-1H-pyrazol-5-one Show/Hide	C24H20N4O2S	1
1	IC50 = 42 nM
CP0081119 Compound Info	(4Z)-4-[[4-[(2-fluorophenyl)methoxy]-1-methylindol-3-yl]methylidene]-3-(1,3-thiazol-2-yl)-1H-pyrazol-5-one Show/Hide	C23H17FN4O2S	1
1	IC50 = 46 nM
CP0209391 Compound Info	(4Z)-4-[(1-methyl-4-phenylmethoxyindol-3-yl)methylidene]-3-(1,3-thiazol-2-yl)-1H-pyrazol-5-one Show/Hide	C23H18N4O2S	1
1	IC50 = 46 nM
CP0645613 Compound Info	4-((4-ethoxy-1-methyl-1H-indol-3-yl)methylene)-3-(4-methyl-1,2,3-thiadiazol-5-yl)-1H-pyrazol-5(4H)-one Show/Hide	C18H17N5O2S	1
1	IC50 = 47 nM
CP0672163 Compound Info	3-(4-methyl-1,2,3-thiadiazol-5-yl)-4-((1-methyl-4-(pyridin-4-ylmethoxy)-1H-indol-3-yl)methylene)-1H-pyrazol-5(4H)-one Show/Hide	C22H18N6O2S	1
1	IC50 = 55 nM
CP0142866 Compound Info	(7R)-2-[2-ethoxy-4-(1-methylpiperidin-4-yl)anilino]-7-ethyl-5-methyl-8-[(3-methylthiophen-2-yl)methyl]-7H-pteridin-6-one Show/Hide	C29H38N6O2S	1
1	IC50 = 63 nM
CP0101960 Compound Info	3-[1-[(4-fluorophenyl)methyl]pyrazol-4-yl]-5-(1-methylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine Show/Hide	C21H17FN6	2
1	IC50 = 70 nM
2	IC50 = 256.4 nM
CP0149386 Compound Info	3-[1-[(3,4-difluorophenyl)methyl]pyrazol-4-yl]-5-(1-methylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine Show/Hide	C21H16F2N6	2
1	IC50 = 84 nM
2	IC50 = 379 nM
CP0350379 Compound Info	(7R)-8-benzyl-2-[2-ethoxy-4-(1-methylpiperidin-4-yl)anilino]-7-ethyl-5-methyl-7H-pteridin-6-one Show/Hide	C30H38N6O2	1
1	IC50 = 85 nM
CP0340900 Compound Info	(1S,2R)-2-[[5-chloro-2-[(1-methyl-2-oxo-4,5-dihydro-3H-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]cyclohexane-1-carboxamide Show/Hide	C22H27ClN6O2	1
1	IC50 = 180 nM
CP0044060 Compound Info	4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide Show/Hide	C28H39N7O3	3
1	IC50 = 180 nM
2	IC50 = 390 nM
3	Kd = 160 nM
CP0143636 Compound Info	4-[(4-methylpiperazin-1-yl)methyl]-N-[5-[3-methyl-4-[(5-propan-2-yl-1,2-oxazol-3-yl)carbamoylamino]phenyl]-1H-pyrazol-3-yl]benzamide Show/Hide	C30H36N8O3	1
1	IC50 = 402 nM
CP0661487 Compound Info	3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate Show/Hide	C26H34Cl2N7O7P	1
1	IC50 > 10000 nM
CP0129766 Compound Info	(16R)-19-amino-13-fluoro-4,8,16-trimethyl-9-oxo-17-oxa-4,5,8,20-tetrazatetracyclo[16.3.1.02,6.010,15]docosa-1(22),2,5,10(15),11,13,18,20-octaene-3-carbonitrile Show/Hide	C21H19FN6O2	3
1	Ki < 0.07 nM
2	Ki = 0.7 nM
3	Ki = 8.2 nM

Clinical Information about the Protein

Target 1 ( ALK tyrosine kinase receptor (ALK) )

Target Type	Successful Target
Disease	7 Target-related Diseases				7
1	Lung cancer [ICD-11: 2C25.0]
2	Non-small-cell lung cancer [ICD-11: 2C25.Y]
3	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
4	Non-small-cell lung cancer [ICD-11: 2C25]
5	Advanced solid tumour [ICD-11: 2A00-2F9Z]
6	Diffuse large B-cell lymphoma [ICD-11: 2A81]
7	Brain metastases [ICD-11: 2D50]
Approved Drug(s)	6 Approved Drugs				6
1	Alectinib	Drug Info	Approved	Lung cancer
2	Brigatinib	Drug Info	Approved	Non-small-cell lung cancer
3	Ceritinib	Drug Info	Approved	Non-small-cell lung cancer
4	Crizotinib	Drug Info	Approved	Non-small-cell lung cancer
5	Lorlatinib	Drug Info	Approved	Non-small-cell lung cancer
6	Entrectinib	Drug Info	Approved	Non-small-cell lung cancer
Clinical Trial Drug(s)	6 Clinical Trial Drugs				6
1	Ensartinib	Drug Info	Phase 3	Non-small-cell lung cancer
2	AP26113	Drug Info	Phase 2	Solid tumour/cancer
3	PF-06463922	Drug Info	Phase 2	Non-small-cell lung cancer
4	TSR-011	Drug Info	Phase 1/2	Non-small-cell lung cancer
5	X-396	Drug Info	Phase 1/2	Advanced solid tumour
6	ASP3026	Drug Info	Phase 1	Diffuse large B-cell lymphoma
Investigative Drug(s)	1 Investigative Drug				1
1	CEP-28122	Drug Info	Investigative	Solid tumour/cancer
Patented Agent(s)	2 Patented Agents				2
1	Benzimidazole derivative 6	Drug Info	Patented	Solid tumour/cancer
2	PMID28270010-Compound-Figure21-b	Drug Info	Patented	Brain metastases

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT06841	ALK tyrosine kinase receptor	Mus musculus, Mouse	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han