Human Kinase Chemical Probe Program

Protein kinases constitute a family of more than 500 proteins in humans with central functions in most aspects of life. Due to their key roles in cellular signalling, dysregulation of kinases is frequently associated with disease and inhibitors have been developed for a considerable number of them. Although kinases are well established drug targets many of the developed kinase inhibitors lack selectivity over related kinases making them less useful tools for biological experiments to explore the activity of a specific kinase. In addition there is a large number of kinases ‘the untargeted kinome’ for which no potent, specific and cell active inhibitors ‘probes’ are available.

Goals

  • to develop chemical probes for protein kinases
  • to share chemical probes with the research community
  • to create a comprehensive chemogenomics set




Susanne Muller-Knapp coordinates the Kinase Chemical Probe Program.

 

SGC Site Lead Investigator Primary Capabilities Primary Focus
Campinas Rafael Couñago Protein expression
X-ray crystallography
Medicinal chemistry
Cell assays

 

RNA splicing
In-house kinase profiling

 

UNC

Tim Willson Medicinal chemistry
Compound sets
Chemical probes
Chemogenomics
Oxford Alex Bullock
Jon Elkins
Protein expression
X-ray crystallography
Screening
Cell assays
Chemical biology
Frankfurt Stefan Knapp Screening
X-ray crystallography
Medicinal chemistry
Cell assays
Chemical biology
Chemical probes
Name Structure Protein Family Specific Targets Control In vivo parameters tested*sort descending Added
SGC-AAK1-1 Kinase AAK1 BMP2K/BIKE SGC-AAK1-1N 02/18
SGC-CK2-2 CK2/CSNK2 SGK-CK2-2N 05/23
SGC-GAK-1 Kinase GAK SGC-GAK-1N 02/18
JA397 CDK14-18 JA314 07/23
TH-257 LIMK1/2 TH-263 07/23
SGC-CAF382-1 Kinase CDKL5 SGC-CAF268-1N 09/23
SGC-STK17B-1 Kinase STK17B/DRAK2 SGC-STK17B-1N 02/20
JA310 Kinase MST3, MST4 JA262 11/23
FM-381 Kinase JAK3 FM-479 02/17
TH-257 Kinase LIMK1/2 TH-263 07/17
SGC-PI5P4Kγ/MYLK4-1 Kinase PI5P4K gamma, MYLK4 SGC-PI5P4Kγ/MYLK4-1N No 05/23
MU1210 Kinase CLK1, CLK2, CLK4, DYRK1A, DYRK1B, DYRK2 MU140 No 05/19
SGC-CAMKK2-1 Serine-threonine protein kinase CAMKK1, CAMKK2 SGC-CAMKK2-1N No 01/20
SGC-CLK-1 Kinase CLK1, CLK2, and CLK4 SGC-CLK-1N No 02/20
SGC-CDKL5_GSK3 Kinase CDKL5, GSK3 SGC-CDKL5/GSK3-1N No 09/23
SGC-GSK3-1 Kinase GSK3 SGC-CDKL5/GSK3-1N No 09/23
SGC-CK2-1 Kinase CK2 SGC-CK2-1N No 06/20
NR162 Membrane-associated guanylate kinases CASK NR187 No 09/20
CK156 Kinase STK17A, DRAK1 CKJB71 No 10/21
NVS-PAK1-1 Kinase PAK1 NVS-PAK1-C No 06/16
SGC-PIKFYVE-1 Kinase PIKfyve SGC-PIKFYVE-1N No 10/22
DDR-TRK-1 Kinase DDR, TRK DDR-TRK-1N Yes 08/18
MRIA9 Protein Kinases SIK1, SIK2,SIK3 MR7 Yes 08/21
M4K2234 Kinase ALK1, ALK2 M4K2234NC Yes 02/22
MU1700 Kinase ALK1, ALK2 MU1700NC Yes 02/22
MU1742 Kinase CK1δ, CK1ε MU2027 Yes 10/22
CS640 CS640s Yes 01/23
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