Top ▲

ALK receptor tyrosine kinase

Click here for help

Target id: 1839

Nomenclature: ALK receptor tyrosine kinase

Abbreviated Name: ALK

Family: Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1620 2p23.2-p23.1 ALK ALK receptor tyrosine kinase
Mouse 1 1621 17 43.77 cM Alk anaplastic lymphoma kinase
Rat - 1617 6q13 Alk ALK receptor tyrosine kinase
Previous and Unofficial Names Click here for help
CD246 | ALK tyrosine kinase receptor | Tcrz | anaplastic lymphoma receptor tyrosine kinase
Database Links Click here for help
Alphafold Q9UM73 (Hs), P97793 (Mm)
BRENDA 2.7.10.1
ChEMBL Target CHEMBL4247 (Hs), CHEMBL5771 (Mm)
DrugBank Target Q9UM73 (Hs)
Ensembl Gene ENSG00000171094 (Hs), ENSMUSG00000055471 (Mm), ENSRNOG00000008683 (Rn)
Entrez Gene 238 (Hs), 11682 (Mm)
Human Protein Atlas ENSG00000171094 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:238 (Hs), mmu:11682 (Mm)
OMIM 105590 (Hs)
Orphanet ORPHA160020 (Hs)
Pharos Q9UM73 (Hs)
RefSeq Nucleotide NM_004304 (Hs), NM_007439 (Mm), NM_001169101 (Rn)
RefSeq Protein NP_004295 (Hs), NP_031465 (Mm), NP_001162572 (Rn)
SynPHARM 80285 (in complex with brigatinib)
80282 (in complex with brigatinib)
79503 (in complex with ceritinib)
79022 (in complex with crizotinib)
79786 (in complex with loratinib)
UniProtKB Q9UM73 (Hs), P97793 (Mm)
Wikipedia ALK (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of anaplastic lymphoma kinase complexed with LDK378.
PDB Id:  4MKC
Ligand:  ceritinib
Resolution:  2.01Å
Species:  Human
References:  7
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the human anaplastic lymphoma kinase in complex with crizotinib (PF-02341066).
PDB Id:  2XP2
Ligand:  crizotinib
Resolution:  1.9Å
Species:  Human
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  Structure of L1196M mutant anaplastic lymphoma kinase in complex with crizotinib. The L1196M mutation is in the gatekeeper residue, which in the wild-type kinase controls access to the ATP binding pocket of the enzyme. The mutation inhibits drug access to the ATP binding pocket.
PDB Id:  2YFX
Ligand:  crizotinib
Resolution:  1.7Å
Species:  Human
References:  11
Image of receptor 3D structure from RCSB PDB
Description:  Structure of L1196M mutant human Anaplastic Lymphoma Kinase in complex with PF-06463922. It is important to note that this compound binds to this gatekeeper mutant and so will be active in drug-resistant tumours carrying this mutation.
PDB Id:  4CLJ
Ligand:  lorlatinib
Resolution:  1.66Å
Species:  Human
References:  13
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human anaplastic lymphoma kinase in complex with acyliminobenzimidazole inhibitor 36
PDB Id:  4FOD
Ligand:  belizatinib
Resolution:  2.0Å
Species:  Human
References:  17
Enzyme Reaction Click here for help
EC Number: 2.7.10.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
belizatinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.4 pKd 17
⤷ pKd 9.4 (Kd 3.6x10-10 M) [17]
Description: Binding affinity in vitro.
NVP-TAE684 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.0 pKd 4
⤷ pKd 9.0 (Kd 1.1x10-9 M) [4]
brigatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 10.1 pKi 14
⤷ pKi 10.1 (Ki 9x10-11 M) [14]
Description: Wild type ALK
lorlatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.1 pKi 13
⤷ pKi 9.1 (Ki 7x10-10 M) [13]
Description: Note that this is inhibition of the ALK L1196M mutant enzyme.
ceritinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.7 pIC50 20
⤷ pIC50 9.7 (IC50 2x10-10 M) [20]
ensartinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition >9.4 pIC50 19
⤷ pIC50 >9.4 (IC50 <4x10-10 M) [19]
Description: Result from DiscoveRx KINOMEscan® selectivity screen.
brigatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.2 – 9.4 pIC50 12,14
⤷ pIC50 9.2 – 9.4 (IC50 6.2x10-10 – 3.7x10-10 M) [12,14]
GSK-1838705A Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.3 pIC50 26
⤷ pIC50 9.3 (IC50 5x10-10 M) [26]
gilteritinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition ~9.3 pIC50 16
⤷ pIC50 ~9.3 (IC50 ~5x10-10 M) [16]
TL13-112 Small molecule or natural product Hs Inhibition 9.2 pIC50 25
⤷ pIC50 9.2 (IC50 6x10-10 M) [25]
Description: Determined in a biochemical kinase activity assay.
compound 8e [PMID: 24432909] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.1 pIC50 11
⤷ pIC50 9.1 (IC50 8x10-10 M) [11]
crizotinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.0 pIC50 3
⤷ pIC50 9.0 (IC50 1x10-9 M) [3]
ficonalkib Small molecule or natural product Hs Inhibition >9.0 pIC50 18
⤷ pIC50 >9.0 (IC50 <1x10-9 M) [18]
Description: Inhibition of WT hALK in vitro
neladalkib Small molecule or natural product Hs Inhibition ~9.0 pIC50 10
⤷ pIC50 ~9.0 (IC50 ~1x10-9 M) [10]
Description: inhibitor potency vs. ALK with mutations F1174L, F1174S, R1275Q, T1151M
repotrectinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.0 pIC50 6
⤷ pIC50 9.0 (IC50 1.04x10-9 M) IC50 for ALKG1202R is 1.2 nM. [6]
zotizalkib Small molecule or natural product Hs Inhibition 8.9 pIC50 22
⤷ pIC50 8.9 (IC50 1.4x10-9 M) [22]
alectinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 15
⤷ pIC50 8.7 (IC50 1.9x10-9 M) [15]
compound 25b [PMID: 22564207] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pIC50 9
⤷ pIC50 8.7 (IC50 1.9x10-9 M) [9]
envonalkib Small molecule or natural product Hs Inhibition 8.7 pIC50 28
⤷ pIC50 8.7 (IC50 1.96x10-9 M) [28]
CEP-37440 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 23
⤷ pIC50 8.5 (IC50 3.1x10-9 M) [23]
AZD3463 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >8.0 pIC50 2
⤷ pIC50 >8.0 (IC50 <1x10-8 M) [2]
compound 5m [PMID: 20483621] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.0 pIC50 21
⤷ pIC50 8.0 (IC50 1x10-8 M) [21]
compound 5n [PMID: 20483621] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.0 pIC50 21
⤷ pIC50 8.0 (IC50 1x10-8 M) [21]
iruplinalkib Small molecule or natural product Approved drug Hs Inhibition 7.0 – 9.0 pIC50 5
⤷ pIC50 7.0 – 9.0 (IC50 1x10-7 – 1x10-9 M) [5]
compound 5g [PMID: 20483621] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.0 pIC50 21
⤷ pIC50 8.0 (IC50 1.1x10-8 M) [21]
compound 17 [PMID: 34176264] Small molecule or natural product Hs Inhibition 7.9 pIC50 29
⤷ pIC50 7.9 (IC50 1.36x10-8 M) [29]
Description: Determined by TF-FRET
compound 15 [PMID: 24900237] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.8 pIC50 24
⤷ pIC50 7.8 (IC50 1.4x10-8 M) [24]
unecritinib Small molecule or natural product Hs Inhibition >7.0 pIC50 30
⤷ pIC50 >7.0 (IC50 <1x10-7 M) [30]
Description: This is a binned IC50 va;lue from the referenced patent
Inhibitor Comments
The Ki for brigatinib (AP26113) vs ALK carrying the L1196M gatekeeper mutation is 0.08nM [14].
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 4,27
Key to terms and symbols Click column headers to sort
Target used in screen: ALK
Ligand Sp. Type Action Value Parameter
GSK-1838705A Small molecule or natural product Hs Inhibitor Inhibition 9.3 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 1,8
Key to terms and symbols Click column headers to sort
Target used in screen: ALK/ALK
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.9 0.0 0.5
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.5 8.0 2.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 10.7 10.0 1.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 12.2 0.0 4.0
JAK3 inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 12.5 19.0 3.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 16.6
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.7 16.0 1.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.0 30.0 11.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 36.9 81.0 79.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 38.1 24.0 2.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  ALK-positive anaplastic large cell lymphoma
Synonyms: Anaplastic large cell lymphoma [Disease Ontology: DOID:0050744]
Disease Ontology: DOID:0050744
Orphanet: ORPHA300895
Disease:  ALK-positive large B-cell lymphoma
Orphanet: ORPHA364043
Disease:  Inflammatory myofibroblastic tumor
Orphanet: ORPHA178342
Disease:  Neuroblastoma, susceptibility to, 3; NBLST3
Synonyms: Neuroblastoma [Orphanet: ORPHA635] [Disease Ontology: DOID:769]
Disease Ontology: DOID:769
OMIM: 613014
Orphanet: ORPHA635

References

Show »

1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

2. AstraZeneca. AZD3463. Accessed on 11/09/2014. Modified on 11/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/azd3463/

3. Cui JJ, Tran-Dubé M, Shen H, Nambu M, Kung PP, Pairish M, Jia L, Meng J, Funk L, Botrous I et al.. (2011) Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem, 54 (18): 6342-63. [PMID:21812414]

4. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

5. Ding Z, Zhang M, Chen S, Liu X, Zhu Y, Fan Y, Zhao B, Zhang L, Yang Y, Zheng Q et al.. (2018) Spirocyclic aryl phosphorus oxide and aryl phosphorus sulfide. Patent number: US10053477B2. Assignee: Qilu Pharmaceutical Co Ltd. Priority date: 04/07/2014. Publication date: 21/08/2018.

6. Drilon A, Ou SI, Cho BC, Kim DW, Lee J, Lin JJ, Zhu VW, Ahn MJ, Camidge DR, Nguyen J et al.. (2018) Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations. Cancer Discov, 8 (10): 1227-1236. [PMID:30093503]

7. Friboulet L, Li N, Katayama R, Lee CC, Gainor JF, Crystal AS, Michellys PY, Awad MM, Yanagitani N, Kim S et al.. (2014) The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer. Cancer Discov, 4 (6): 662-673. [PMID:24675041]

8. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]

9. Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD et al.. (2012) Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem, 55 (10): 4580-93. [PMID:22564207]

10. Green JA, Kropp JT, Noci D, Pelish HE, Porter JR, Soglia JR, Tangpeerachaikul A, Turner CD, Zhu VW, Perason DJ. (2023) Methods of treating solid tumor using (19r)-5-chloro-3-ethyl-16-fluoro-10,19-dimethyl-20-oxa-3,4,10,11,23-pentaazapentacyclo[19.3.1.02,6.08,12.013,18]pentacosa-1(24),2(6),4,8,11,13,15,17,21(25),22-decaen-22-amine. Patent number: WO2023196910A1. Assignee: Nuvalent, Inc. Priority date: 06/04/2023. Publication date: 12/10/2023.

11. Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN et al.. (2014) Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. J Med Chem, 57 (4): 1170-87. [PMID:24432909]

12. Huang WS, Liu S, Zou D, Thomas M, Wang Y, Zhou T, Romero J, Kohlmann A, Li F, Qi J et al.. (2016) Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem, 59 (10): 4948-64. [PMID:27144831]

13. Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D et al.. (2014) Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. J Med Chem, 57 (11): 4720-44. [PMID:24819116]

14. Katayama R, Khan TM, Benes C, Lifshits E, Ebi H, Rivera VM, Shakespeare WC, Iafrate AJ, Engelman JA, Shaw AT. (2011) Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci USA, 108 (18): 7535-40. [PMID:21502504]

15. Kinoshita K, Asoh K, Furuichi N, Ito T, Kawada H, Hara S, Ohwada J, Miyagi T, Kobayashi T, Takanashi K et al.. (2012) Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802). Bioorg Med Chem, 20 (3): 1271-80. [PMID:22225917]

16. Lee LY, Hernandez D, Rajkhowa T, Smith SC, Raman JR, Nguyen B, Small D, Levis M. (2017) Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor. Blood, 129 (2): 257-260. [PMID:27908881]

17. Lewis RT, Bode CM, Choquette DM, Potashman M, Romero K, Stellwagen JC, Teffera Y, Moore E, Whittington DA, Chen H et al.. (2012) The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer. J Med Chem, 55 (14): 6523-40. [PMID:22734674]

18. Liu G, Jiao N, Wang S, Min W, Liu X, Sun Y, Zhang H. (2018) Anaplastic lymphoma kinase inhibitor and preparation method and use thereof. Patent number: WO2018127184A1. Assignee: Beijing Sailintai Pharmaceutical Technology Co., Ltd.. Priority date: 06/01/2017. Publication date: 12/07/2018.

19. Lovly CM, Heuckmann JM, de Stanchina E, Chen H, Thomas RK, Liang C, Pao W. (2011) Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors. Cancer Res, 71 (14): 4920-31. [PMID:21613408]

20. Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M et al.. (2013) Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem, 56 (14): 5675-90. [PMID:23742252]

21. Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA et al.. (2010) Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. Bioorg Med Chem, 18 (12): 4351-62. [PMID:20483621]

22. Murray BW, Zhai D, Deng W, Zhang X, Ung J, Nguyen V, Zhang H, Barrera M, Parra A, Cowell J et al.. (2021) TPX-0131, a Potent CNS-penetrant, Next-generation Inhibitor of Wild-type ALK and ALK-resistant Mutations. Mol Cancer Ther, 20 (9): 1499-1507. [PMID:34158340]

23. Ott GR, Cheng M, Learn KS, Wagner J, Gingrich DE, Lisko JG, Curry M, Mesaros EF, Ghose AK, Quail MR et al.. (2016) Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). J Med Chem, 59 (16): 7478-96. [PMID:27527804]

24. Ott GR, Tripathy R, Cheng M, McHugh R, Anzalone AV, Underiner TL, Curry MA, Quail MR, Lu L, Wan W et al.. (2010) Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity. ACS Med Chem Lett, 1 (9): 493-8. [PMID:24900237]

25. Powell CE, Gao Y, Tan L, Donovan KA, Nowak RP, Loehr A, Bahcall M, Fischer ES, Jänne PA, George RE et al.. (2018) Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). J Med Chem, 61 (9): 4249-4255. [PMID:29660984]

26. Sabbatini P, Korenchuk S, Rowand JL, Groy A, Liu Q, Leperi D, Atkins C, Dumble M, Yang J, Anderson K et al.. (2009) GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther, 8 (10): 2811-20. [PMID:19825801]

27. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

28. Xiao D, Xu X, Liu X, Yu H, Liu Z, Peng Y, Sun Y, Luo H, Kong F, Han Y et al.. (2014) Substituted 2-aminopyridine protein kinase inhibitor. Patent number: WO2014117718A1. Assignee: Centaurus Biopharma Co Ltd, Chia Tai Tianqing Pharmaceutical Group Co Ltd, Lianyungang Runzhong Pharmaceutical Co Ltd. Priority date: 02/02/2013. Publication date: 07/08/2014.

29. Xie S, Sun Y, Liu Y, Li X, Li X, Zhong W, Zhan F, Zhu J, Yao H, Yang DH et al.. (2021) Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK). J Med Chem, 64 (13): 9120-9140. [PMID:34176264]

30. Zhang D. (2013) Pyridine compounds as inhibitors of kinase. Patent number: WO2013041038A1. Assignee: Teligene Ltd.. Priority date: 21/09/2012. Publication date: 28/03/2013.

How to cite this page

Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family: ALK receptor tyrosine kinase. Last modified on 06/03/2024. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1839.