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.


  • 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



Tim Willson Medicinal chemistry
Compound sets
Chemical probes
Oxford Alex Bullock
Jon Elkins
Protein expression
X-ray crystallography
Cell assays
Chemical biology
Frankfurt Stefan Knapp Screening
X-ray crystallography
Medicinal chemistry
Cell assays
Chemical biology
Chemical probes
Namesort ascending Structure Protein Family Specific Targets Control In vivo parameters tested* Added
TH-257 Kinase LIMK1/2 TH-263 07/17
TH-257 LIMK1/2 TH-263 07/23
SGC-STK17B-1 Kinase STK17B/DRAK2 SGC-STK17B-1N 02/20
SGC-PIKFYVE-1 Kinase PIKfyve SGC-PIKFYVE-1N No 10/22
SGC-PI5P4Kγ/MYLK4-1 Kinase PI5P4K gamma, MYLK4 SGC-PI5P4Kγ/MYLK4-1N No 05/23
SGC-GSK3-1 Kinase GSK3 SGC-CDKL5/GSK3-1N No 09/23
SGC-GAK-1 Kinase GAK SGC-GAK-1N 02/18
SGC-CLK-1 Kinase CLK1, CLK2, and CLK4 SGC-CLK-1N No 02/20
SGC-CK2-2 CK2/CSNK2 SGK-CK2-2N 05/23
SGC-CK2-1 Kinase CK2 SGC-CK2-1N No 06/20
SGC-CDKL5_GSK3 Kinase CDKL5, GSK3 SGC-CDKL5/GSK3-1N No 09/23
SGC-CAMKK2-1 Serine-threonine protein kinase CAMKK1, CAMKK2 SGC-CAMKK2-1N No 01/20
SGC-CAF382-1 Kinase CDKL5 SGC-CAF268-1N 09/23
SGC-AAK1-1 Kinase AAK1 BMP2K/BIKE SGC-AAK1-1N 02/18
NVS-PAK1-1 Kinase PAK1 NVS-PAK1-C No 06/16
NR162 Membrane-associated guanylate kinases CASK NR187 No 09/20
MU1742 Kinase CK1δ, CK1ε MU2027 Yes 10/22
MU1700 Kinase ALK1, ALK2 MU1700NC Yes 02/22
MU1210 Kinase CLK1, CLK2, CLK4, DYRK1A, DYRK1B, DYRK2 MU140 No 05/19
MRIA9 Protein Kinases SIK1, SIK2,SIK3 MR7 Yes 08/21
M4K2234 Kinase ALK1, ALK2 M4K2234NC Yes 02/22
JA397 CDK14-18 JA314 07/23
JA310 Kinase MST3, MST4 JA262 11/23
FM-381 Kinase JAK3 FM-479 02/17
DDR-TRK-1 Kinase DDR, TRK DDR-TRK-1N Yes 08/18
CS640 CS640s Yes 01/23
CK156 Kinase STK17A, DRAK1 CKJB71 No 10/21
glqxz9283 sfy39587stf02 mnesdcuix8