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
(R)-9s ADRA1D GPCR Antagonist Yes (S)-9s
(R)-ZINC-3573 MRGPRX2 GPCR Agonist No (S)-ZINC-3573
8RK64 UCHL1 Ubiquitin C‐terminal hydrolase Inhibitor Yes JYQ88
A-079 TRPA1 TRP channels Antagonist Yes A-226
A-1155463 BCL2L1 Bcl-2 family Inhibitor Yes A-1107969
A-1211212 BCL2 Bcl-2 family Inhibitor Yes A-1210227
A-1596586 CFTR ATP-Binding Cassette (ABC) Corrector Yes A-1596584
A-192621 EDNRB Endothelin receptor Antagonist Yes A-1806262
A-446 GLS Aminohydrolase Inhibitor Yes A-426
A-485 EP300, CREBBP HAT Inhibitor Yes A-486
ABT-100 FNTB Transferase Inhibitor Yes A-108
ABT-546 EDNRA Endothelin receptor Antagonist Yes A-545
ABT-724 DRD4 GPCR Agonist Yes A-769
BAY 1753011 AVPR1A, AVPR2 GPCR Antagonist Yes BAY-2297
BAY 1816032 BUB1 Kinase Inhibitor Yes BAY-283
BAY-069 BCAT1, BCAT2 Amino acid transaminase Inhibitor Yes BAY-771
BAY-091 PIP4K2A Kinase Inhibitor Yes BAY-0361
BAY-179 Complex I Complex of 42 peptides Inhibitor Yes BAY-070
BAY-1797 P2X4 P2RX4 Inhibitor Yes BAY-207
BAY-277 METAP2 Aminopeptidase Degrader Yes BAY-8805
BAY-293 SOS1 GEF Inhibitor No BAY-294
BAY-3153 CCR1 GPCR Antagonist Yes BAY-173
BAY-3827 PRKAA1, RPS6KA1 Kinase Inhibitor No BAY-974
BAY-386 F2R GPCR Antagonist Yes BAY-448
BAY-390 TRPA1 Ion channel Inhibitor Yes BAY-9897
BAY-474 MET Kinase Inhibitor Yes BAY-827
BAY-549 ROCK1, ROCK2 Kinase Inhibitor Yes BAY-4900
BAY-6096 ADRA2B GPCR Antagonist Yes BAY-726
BAY-6672 PTGFR GPCR Antagonist Yes BAY-403
BAY-678 ELANE Serine Protease Inhibitor Yes BAY-677
BAY-707 NUDT1 Nudix Inhibitor Yes BAY-604
BAY-7081 PDE9A Phoshodiesterase Inhibitor Yes BAY-7424
BAY-7598 MMP12 Protease Inhibitor Yes BAY-694
BAY-784 GNRHR GPCR Antagonist Yes BAY-786
BAY-826 TIE1, TEK, DDR1, DDR2 Kinase Inhibitor Yes BAY-309
BAY-876 SLC2A1 Solute carrier Inhibitor Yes BAY-588
BAY-885 MAPK7 MAPK (Mitogen-Activated Protein Kinases) Inhibitor No BAY-693
BAY-899 LHCGR Glycoprotein hormone GPCR Allosteric antagonist Yes BAY-897
BAY-985 TBK1, IKBKE Kinase Inhibitor Yes BAY-440
BAY1125976 AKT1/2 Kinase Allosteric inhibitor Yes BAY-940
BI 207127 HCV NS5B RNA polymerase Inhibitor Yes BI-7656
BI 605906 IKBKB Kinase Inhibitor Yes BI-5026
BI 639667 CCR1 Chemokines Antagonist Yes BI-9307
BI 653048 NR3C1 Nuclear hormone receptors Agonist Yes BI-3047
BI 665915 ALOX5AP Other Inhibitor Yes BI-0153
BI 99179 FASN Synthase Inhibitor No BI 99990
BI-1230 HCV NS3 Serine Protease Inhibitor Yes BI-1675
BI-1935 EPHX2 Hydrolase Inhibitor Yes BI-2049
BI-1942 CMA1 Serine protease Inhibitor No
BI-1950 ITGAL Integrin family Inhibitor Yes BI-9446
BI-2081 FFAR1 GPCR Agonist Yes BI-0340
BI-2540 HIV NNRT Reverse transcriptase Inhibitor Yes BI-2439
BI-2545 ENPP2 Phosphodiesterase 2 Inhibitor Yes BI-3017
BI-3231 HSD17B13 17β-hydroxysteroid dehydrogenases Inhibitor Yes BI-0955
BI-3802 BCL6 transcription factor Degrader No BI-5273
BI-3812 BCL6 transcription factor Inhibitor No BI-5273
BI-4394 MMP13 Matrix metalloproteinases Inhibitor Yes BI-4395
BI-5524 ELANE Chymotrypsin Inhibitor Yes BI-5525
BI-8668 Epithelial sodium channel (ENaC) Sodium channels Inhibitor Yes BI-0337
BI-9627 SLC9A1 Solute carrier Antagonist Yes BI-0054
BIBO3304 NPY1R GPCR Antagonist Yes BIBO3457
Borussertib AKT1, AKT2 Kinase Covalent-allosteric inhibitor Yes RL2578
BTZO-1 MIF MIF Activator No BTZO-4
CCT369260 BCL6 Transcription factor Degrader Yes CCT393732
CRTH2 antagonist PTGDR2 GPCR Antagonist Yes CRTH2 negative control
ERKi MAPK3, MAPK1 Kinase Inhibitor Yes ERKi-NC
FHT-2344 SMARCA2, SMARCA4 SWI/SNF Inhibitor Yes FHT-5908
FS-694 MAPK14 Kinase Inhibitor (Type 1.5 binding mode) No FM-743
GNE-2256 IRAK4 Kinase Inhibitor Yes GNE-6689
GSK046 BRD2, BRD3, BRD4, BRDT BET (BD2) Inhibitor Yes
GSK620 BRD2, BRD3, BRD4, BRDT BET (BD2) Inhibitor Yes
GSK778 BRD2, BRD3, BRD4, BRDT BET (BD1) Inhibitor Yes
GSK789 BRD2, BRD3, BRD4, BRDT BET (BD1) Inhibitor No GSK791
GSK973 BRD2, BRD3, BRD4, BRDT BET (BD2) Inhibitor Yes GSK943
GSM1 Gamma secretase complex Protease Modulator Yes GSM-NC
IPP/CNRS-A017 DHODH Dihydroorotate dehydrogenase Inhibitor No IPP/CNRS-A019
JNJ-39758979 HRH4 GPCR Orthosteric antagonist Yes JNJ-39668551
JNJ-42226314 MGLL Serine hydrolase competitive, Non-covalent, Reversible inhibitor Yes JNJ-8034
JNJ-42396302 PDE10A Phosphodiesterase Inhibitor Yes JNJ-40573663
JNJ-4355 MCL1 BCL2 protein family Inhibitor Yes JNJ-78732576
JNJ-54119936 RORC Nuclear hormone receptor Inverse agonist Yes JNJ-53721590
JNJ-6204 CSNK1D/CSNK1E Kinase Inhibitor Yes JNJ-0293
JNJ-65355394 OGA Hydrolase Inhibitor Yes JNJ-73924149
JNJ-9350 SMOX Oxidase Inhibitor Yes JNJ-4545
JP3000 RXRA, RXRB, RXRG Nuclear receptors Agonist No JP3001
KISS1-305 KISS1R GPCR Agonist Yes KISS1-543
MLi-2 LRRK2 Kinase Inhibitor Yes MLi-2-NC
MRK-560 Gamma secretase complex Protease Inhibitor Yes GSI-NC
MRL-650 CNR1 GPCR Inverse agonist Yes MRL-CB1-NC
MRL-SYKi SYK Kinase Inhibitor Yes MRL-SYKi-NC
MSC-4381 SLC16A3 Monocarboxylate transporter Inhibitor Yes MSC-0516
MSD-CYP11B2 CYP11B2 Cytochrome P450 Family 11 Inhibitor Yes MSD-CYP11B2 Negative control
MSD-M1PAM CHRM1 GPCR Positive allosteric modulator Yes MSD-M1PAM-NC
NVS-MALT1 MALT1 Protease (Paracaspase) Allosteric inhibitor Yes NVS-MALT1-C
Ogerin GPR68 GPCR Positive allosteric modulator Yes ZINC32547799
PF-04418948 PTGER2 GPCR Antagonist Yes PF-04475866
PF-04457845 FAAH Hydrolase Inhibitor Yes PF-04875474
PF-05105679 TRPM8 Ion channel Antagonist Yes PF-05257137
PFI-653 VNN1 Hydrolase Inhibitor Yes PFI-653-N
PPTN P2RY14 GPCR Antagonist Yes PPTN-NC
SAFit2 FKBP5 Isomerase Inhibitor Yes ddSAFit2
Skepinone-L MAPK14 Kinase Inhibitor (Type 1 binding mode) Yes FM-743
SR-302 DDR1, DDR2, MAPK11, MAPK14 Kinase Inhibitor No SR-301
SR-318 MAPK14 Kinase Inhibitor (Type 2 binding mode) No SR-321
T-26c MMP13 Peptidase Inhibitor Yes T-26f
T3-CLK CLK1, CLK2, CLK3, CLK4 Kinase Inhibitor No T3-CLK-N
THPP-1 PDE10A Phosphodiesterase Inhibitor Yes THPP-1-NC
TP-004 METAP2 Peptidase Inhibitor Yes TPn-004
TP-008 ACVR1B, TGFBR1 Kinase Inhibitor No Al11
TP-020 MGAT2 Transferase Inhibitor Yes TP-020n
TP-021 BCL6 Transcription factor Inhibitor Yes TP-021n
TP-024 GPR52 GPCR Agonist Yes TP-024n
TP-030-1 RIPK1 Kinase Inhibitor Yes TP-030n
TP-030-2 RIPK1 Kinase Inhibitor Yes TP-030n
TP-040 OGA Hydrolase Inhibitor Yes TP-040n
TP-050 GRIN2A Positive allosteric modulator Yes TP-050n
TP-051 FFAR1 GPCR Agonist Yes TP-051n
TP-060 UGCG Glucosyltransferase Allosteric inhibitor Yes TP-060n
UCSF924 DRD4 GPCR Agonist Yes UCSF924NC
VZ185 BRD7, BRD9 Bromodomain-containing protein family Degrader No cisVZ185
WEB2086 PTAFR GPCR Inhibitor Yes WEB2387
WM-1119 KAT6A, KAT6B Histone acetyltransferase Inhibitor Yes WM-2474
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