Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T15068 Target Info
Target Name Focal adhesion kinase 1 (FAK)
Synonyms
pp125FAK; p125FAK; Protein-tyrosine kinase 2; Protein phosphatase 1 regulatory subunit 71; PPP1R71; Focal adhesion kinase-related nonkinase; FRNK; FAK1; FADK 1; FADK
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Target Type Clinical trial Target
Gene Name PTK2
Biochemical Class Kinase
UniProt ID
FAK1_HUMAN
Co-Targets of This Target  Top
Co-Target Name ALK tyrosine kinase receptor (ALK) Successful Target
UniProt ID ALK_HUMAN
Gene Name ALK
Synonyms
CD246; Anaplastic lymphoma kinase
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Representative Drug(s) CEP-37440 Drug Info IC50 = 3.1 nM [1]
Co-Target Name Insulin receptor (INSR) Successful Target
UniProt ID INSR_HUMAN
Gene Name INSR
Synonyms
IR; CD220 antigen; CD220
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Representative Drug(s) CEP-37440 Drug Info IC50 = 65 nM [1]
Co-Target Name Stress-activated protein kinase JNK2 (JNK2) Patented-recorded Target
UniProt ID MK09_HUMAN
Gene Name MAPK9
Synonyms
Stress-activated protein kinase 1a; SAPK1a; PRKM9; Mitogen-activated protein kinase 9; Mitogen-activated protein kinase 8-interacting protein 2; MAPK 9; MAP kinase 9; Jun-N-terminal kinase 2; JNK-interacting protein 2; JNK-55; JNK MAP kinase scaffold protein 2; JIP-2; Islet-brain-2; IB-2; C-jun-amino-terminal kinase interacting protein 2; C-Jun N-terminal kinase 2
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Representative Drug(s) VS-4718 Drug Info IC50 = 120 nM [2]
Co-Target Name Stress-activated protein kinase JNK3 (JNK3) Patented-recorded Target
UniProt ID MK10_HUMAN
Gene Name MAPK10
Synonyms
Stress-activated protein kinase 1b; SAPK1b; PRKM10; Mitogen-activated protein kinase 10; MAPK 10; MAP kinase p49 3F12; MAP kinase 10; JNK3A; C-Jun N-terminal kinase 3
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Representative Drug(s) VS-4718 Drug Info IC50 = 160 nM [2]
Co-Target Name Focal adhesion kinase 2 (PTK2B) Literature-reported Target
UniProt ID FAK2_HUMAN
Gene Name PTK2B
Synonyms
Related adhesion focal tyrosine kinase; RAFTK; Protein-tyrosine kinase 2-beta; Proline-rich tyrosine kinase 2; PYK2; FAK2; FADK 2; Cell adhesion kinase beta; Calcium-regulated non-receptor proline-rich tyrosine kinase; Calcium-dependent tyrosine kinase; CAKB; CAK-beta; CADTK
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Representative Drug(s) PF-562271 Drug Info IC50 = 13 nM [3]
References  Top
REF 1 Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2016 Aug 25;59(16):7478-96.
REF 2 Synthesis and SAR of 2,4-diaminopyrimidines as potent c-jun N-terminal kinase inhibitors. Medchemcomm. 2012;3:238-43.
REF 3 Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5926-30.

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