Donated chemical probes

Potent, selective and broadly characterized, small molecule chemical modulators of protein function (chemical probes) are powerful research reagents in both fundamental and applied biological research. In this unique project, several pharmaceutical companies (AbbVie, Bayer, Boehringer Ingelheim, Janssen, MSD, Pfizer, and Takeda) have entered into a pre-competitive collaboration with the SGC, to make a large number of these innovative high-quality probes available to the research community. These probes complement the probe set generated by the SGC and its academic and industry collaborators.

All compounds meet specific quality criteria including potency, selectivity and cellular activity and are extensively profiled. Moreover, several probes are suitable for in vivo use. Additionally, control compounds are provided and profiled as well. In order to be accepted as chemical probes in this set, all compounds have been evaluated by an internal as well as an external expert committee.

We are inviting other companies and academics to contact us and provide additional high-quality probes to the community. Please contact us using: SGC Frankfurt

The complete list of the donated chemical probes can be found here.

Compound Name Target Protein Protein Family Mechanism of Action Use in Animal Model Control Name Compound Structure Control Structure
A-485 P300/CBP HAT HAT Inhibitor Yes A-486
ABT-100 Ftase, Farnesyltransferase, FDPS Enzyme, transferase Inhibitor Yes A-409108
ABT-546 ETa Receptor, EDNRA Agonist Yes A-545
ABT-724 Dopamine D4 receptor GPCR Agonist Yes A-423769
BAY-386 Par1 GPCR Antagonist Yes BAY-448
BAY-474 c-Met Enzyme, kinase Inhibitor Yes BAY-827
BAY-678 HNE Serine, protease Inhibitor Yes BAY-677
BAY-707 MTH1 Nudix Inhibitor Yes BAY-604
BAY-7598 MMP12 Enzyme, protease Inhibitor Yes BAY-694
BAY-826 TIE1, TIE2, DDR1 and DDR2 Enzyme, kinase Inhibitor Yes BAY-309
BAY-876 GLUT1 Solute carrier Inhibitor Yes BAY-588
BI 665915 FLAP (ALOX5AP) Other Inhibitor Yes BI-0153
BI 99179 FAS Enzyme, synthase Inhibitor No BI 99990
BI-1935 s-EH Enzyme, hydrolase Inhibitor Yes BI-2049
BI-9627 NHE1, SLC9A1 Solute carrier Antagonist Yes BI-0054
BTZO-1 MIF Enzyme, other Activator No BTZO-4
CRTH2i CRTH2 GPCR Antagonist Yes CRTH2i-control
ERKi ERK Enzyme, kinase Inhibitor Yes ERKi-NC
GSM1 GSM Enzyme, protease Inhibitor Yes GSM-NC
KISS1-305 GPR54 (KISS1 receptor) GPCR Agonist Yes KISS1-543
MRK-560 GSI Enzyme, protease Inhibitor Yes GSI-NC
MRL-650 CB1 GPCR Inverse agonist Yes MRL-CB1-NC
MRL-SYKi SYK Enzyme, kinase Inhibitor Yes MRL-SYKi-NC
PF-04418948 EP2 GPCR Antagonist Yes PF-04475866
PF-04457845 FAAH Enzyme, hydrolase Inhibitor Yes PF-04875474
PF-05105679 TRPM8 Ion channel Antagonist Yes PF-05135076
T-26c MMP-13 Enzyme, peptidase Inhibitor Yes T-26f
TP-004 MetAP2 Enzyme, peptidase Inhibitor Yes TPn-004
TP-009/ (R)-9s Alpha 1D, ADRA1D, alpha 1D adrenoceptor GPCR Agonist Yes (S)-9s
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