Overview of all chemical probes


Target Probe Control Targeted domain Mode of action Recommended concentration Target origin
UCHL1 8RK64 JYQ88 Active site (covalent binding to Cys90) Covalent inhibitor ≤ 3 µM human
TRPA1 A-079 A-226 — Antagonist 1 µM human
BCL2L1 A-1155463 A-1107969 BCL domain Inhibitor ≤ 5 µM human
BCL2 A-1211212 A-1210227 — Inhibitor ≤ 5 µM human
CFTR A-1596586 A-1596584 — Corrector ≤ 1 µM human
EDNRB A-192621 A-1806262 — Antagonist ≤ 300 nM, probe < 1 µM human
GLS A-446 A-426 Allosteric site at the dimer‐dimer interface Inhibitor 100 nM human
EP300, CREBBP A-485 A-486 HAT domain Inhibitor 0.8 µM human
FNTB ABT-100 A-108 Transferase domain Inhibitor 0.01 - 1000 nM human
EDNRA ABT-546 A-545 — Antagonist ≤ 100 nM human
DRD4 ABT-724 A-769 — Agonist 1 - 10000 nM human
KRAS ACBI3 cis-ACBI3 — PROTAC degrader 1-10 µM human
BCAT1, BCAT2 BAY-069 BAY-771 Substrate binding site Inhibitor 1 µM human
PIP4K2A BAY-091 BAY-0361 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 - 10 µM human
AKT1, AKT2, AKT3 BAY1125976 BAY-940 Kinase domain (allosteric pocket) Covalent inhibitor (type 4, non-ATP competitive) ≤ 1 µM human
AVPR1A, AVPR2 BAY 1753011 BAY-2297 — Antagonist 100 nM human
Complex I BAY-179 BAY-070 Quinone binding site (MT-ND1, NDUFS2/7) Inhibitor 0.1 - 1 µM human
P2RX4 BAY-1797 BAY-207 — Inhibitor 0.1 - 1 µM human
BUB1 BAY 1816032 BAY-283 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 300 nM human
METAP2 BAY-277 BAY-8805 — degrader 100 nM human
SOS1 BAY-293 BAY-294 RAS GEF Inhibitor 0.02 - 1.1 µM human
CCR1 BAY-3153 BAY-173 — Antagonist ≤ 100 nM human
PRKAA1, RPS6KA1 BAY-3827 BAY-974 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 150 nM human
F2R BAY-386 BAY-448 — Antagonist ≤ 100 nM human
TRPA1 BAY-390 BAY-9897 — Inhibitor 100 nM human
PLA2G5 BAY-439 BAY-163 active site Inhibitor ≤ 300 nM human
MET BAY-474 BAY-827 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 0.001 - 1 µM human
ROCK1, ROCK2 BAY-549 BAY-4900 Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 100 nM human
ADRA2B BAY-6096 BAY-726 GLN-168, ASP-92, PHE-388 direct interaction with ligand Antagonist 100 nM human
PTGFR BAY-6672 BAY-403 — Antagonist ≤ 0.5 µM human
ELANE BAY-678 BAY-677 Protease domain Inhibitor ≤ 1 µM human
NUDT1 BAY-707 BAY-604 Active site Inhibitor 0.001 - 1 µM human
PDE9A BAY-7081 BAY-7424 Lipophilic pocket Inhibitor 1 µM human
MMP12 BAY-7598 BAY-694 Protease domain Inhibitor < 10 nM human
GNRHR BAY-784 BAY-786 — Antagonist ≤ 1 µM human
TIE1, TEK, DDR1, DDR2 BAY-826 BAY-309 Kinase domain (active site) Inhibitor (type 2, ATP competitive) ≤ 0.5 µM human
SLC2A1 BAY-876 BAY-588 — Inhibitor 0.1 - 75 nM human
MAPK7 BAY-885 BAY-693 Kinase domain (active site) Inhibitor (type 1.5, ATP competitive) 1 µM human
LHCGR BAY-899 BAY-897 Remnants of the rhodopsin binding site Allosteric antagonist 1 µM human
ADAMTS7, ADAMTS12 BAY-9835 BAY-1880 Protease domain Inhibitor 100 nM human
TBK1, IKBKE BAY-985 BAY-440 Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 1 µM human
BDKRB1 BI-113823 BI-5832 — Antagonist 100 nM human
HCV NS3 BI-1230 BI-1675 Protease domain, RNA helicase domain Inhibitor < 100 nM viral
CTSS BI-1915 BI-1920 — Inhibitor 1 µM human
EPHX2 BI-1935 BI-2049 catalytic domain Inhibitor < 1 nM human
CMA1 BI-1942 no record.controls Protease domain Inhibitor 1 µM human
ITGAL BI-1950 BI-9446 I-domain Inhibitor 100 nM human
HCV NS5B BI 207127 BI-7656 Pocket 1 of the thumb domain Inhibitor ≤ 100 nM viral
FFAR1 BI-2081 BI-0340 — Agonist 200 nM human
HIV NNRT BI-2540 BI-2439 Allosteric site adjacent to the polymerase active site Inhibitor ≤ 100 nM viral
ENPP2 BI-2545 BI-3017 Catalytic domain Inhibitor 1 µM human
HSD17B13 BI-3231 BI-0955 Ser172, Tyr185 (catalytical triad) Inhibitor 1 µM human
BCL6 BI-3802 BI-5273 BTB/POZ, binds at interface of 2 monomers Degrader ≤ 1 µM human
BCL6 BI-3812 BI-5273 BTB/POZ, binds at interface of 2 monomers Inhibitor ≤ 1 µM human
MMP13 BI-4394 BI-4395 Protease domain Inhibitor 0.1 µM human
HCRTR1 BI-5121 BI-6199 Orthosteric pocket Antagonist 100 nM human
ELANE BI-5524 BI-5525 — Inhibitor 100 nM human
IKBKB BI 605906 BI-5026 Kinase domain (active site) Inhibitor (ATP competitive) ≤ 5 µM human
CCR1 BI 639667 BI-9307 — Antagonist 100 nM human
NR3C1 BI 653048 BI-3047 Ligand binding domain Agonist 1 µM human
ALOX5AP BI 665915 BI-0153 Membrane domain Inhibitor 30 – 500 nM human
Epithelial sodium channel BI-8668 BI-0337 — Inhibitor 1 µM human
SLC9A1 BI-9627 BI-0054 — Antagonist ≤ 5 µM human
FASN BI 99179 BI 99990 Ketoacyl Reductase domain Inhibitor 1 -10 µM human
NPY1R BIBO3304 BIBO3457 — Antagonist 100 nM human
AKT1, AKT2, AKT3 Borussertib RL2578 Kinase domain (allosteric pocket) Covalent inhibtor (type 4, non-ATP competitive) 1 µM human
MIF BTZO-1 BTZO-4 Tautomerase domain ARE Activator 0.8 - 1 µM human
CIT C3TD879 C3TD879-N Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 2 µM human
BCL6 CCT369260 CCT393732 BTB domain Degrader ≤ 1 µM human
PTGDR2 CRTH2 antagonist CRTH2 negative control — Antagonist 100 nM human
MAPK3, MAPK1 ERKi ERKi-NC Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 µM human
SMARCA2, SMARCA4 FHT-2344 FHT-5908 — Inhibitor ≤ 1 µM human
MAPK14 FS-694 FM-743 Kinase domain (active site) Inhibitor (type 1.5, ATP competitive) 0.1 - 1 µM human
IRAK4 GNE-2256 GNE-6689 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 µM human
BRD2, BRD3, BRD4, BRDT GSK046 no record.controls BD2 Inhibitor ≤ 10 µM human
BRD2, BRD3, BRD4, BRDT GSK620 no record.controls BD2 Inhibitor ≤ 10 µM human
BRD2, BRD3, BRD4, BRDT GSK778 no record.controls BD1 Inhibitor ≤ 1 µM human
BRD2, BRD3, BRD4, BRDT GSK789 GSK791 BD1 Inhibitor ≤ 10 µM human
BRD2, BRD3, BRD4, BRDT GSK973 GSK943 BD2 Inhibitor ≤ 10 µM human
Gamma secretase complex GSM1 GSM-NC — Modulator ≤ 1 µM human
USP32 Huib32 Huib32NC Active site (covalent binding to Cys743) Covalent, fast reversible Inhibitor 5 µM human
DHODH IPP/CNRS-A017 IPP/CNRS-A019 — Inhibitor ≤ 100 nM human
CDK7 JNJ-3738 JNJ-6240 Kinase domain (active site) Covalent inhibtor (ATP competitive) ≤ 1 µM human
HRH4 JNJ-39758979 JNJ-39668551 — Orthosteric antagonist ≤ 10 µM human
MGLL JNJ-42226314 JNJ-8034 Azetidine-amide carbonyl forms H-bonds with NH of Ala51 and Met123 in oxyanion hole Non-covalent, competitive, reversible inhibitor ≤ 10 µM human
PDE10A JNJ-42396302 JNJ-40573663 Hydrophobic clamp of the catalytic site Inhibitor ≤ 10 µM human
MCL1 JNJ-4355 JNJ-78732576 BCL domain Inhibitor ≤ 10 µM human
PDE2A JNJ-54082730 JNJ-54103985 Catalytic site Inhibitor None human
RORC JNJ-54119936 JNJ-53721590 Orthosteric site of binding domain Inverse agonist ≤ 1 µM human
CSNK1D, CSNK1E JNJ-6204 JNJ-0293 Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 1 µM human
OGA JNJ-65355394 JNJ-73924149 — Agonist or Inhibitor ≤ 10 µM human
GRIN2A JNJ-78911118 JNJ-77914993 GRIN1/GRIN2A interface Negative Allosteric Modulator ≤ 10 µM human
NRLP3 JNJ-79883960 JNJ-78832000 NACHT domain Inhibitor ≤ 10 µM human
RSV L JNJ-8003 JNJ-6643 Induced-fit pocket on capping domain Inhibitor 1 - 10 µM viral
SMOX JNJ-9350 JNJ-4545 — Inhibitor ≤ 10 µM human
RXRA, RXRB, RXRG JP3000 JP3001 Ligand binding domain Agonist 0.1 - 1 µM human
PARK7 JYQ-173 MB078 Active site (covalent binding to Cys106) Covalent inhibitor ≤ 1 µM human
KISS1R KISS1-305 KISS1-543 Kisspeptin binding site Agonist 1 - 1000 nM human
LRRK2 MLi-2 MLi-2-NC Kinase domain (active site) Inhibitor (type 1, ATP competitive) ≤ 1 µM human
Gamma secretase complex MRK-560 GSI-NC Protease domain Inhibitor ≤ 100 nM human
CNR1 MRL-650 MRL-CB1-NC — Inverse agonist ≤ 1 µM human
SYK MRL-SYKi MRL-SYKi-NC Kinase domain (active site) Inhibitor (type 1, ATP competitive) 100 nM human
SLC16A3 MSC-4381 MSC-0516 — Inhibitor ≤ 10 µM human
CYP11B2 MSD-CYP11B2 MSD-CYP11B2 Negative control — Inhibitor 25 - 100 nM human
CHRM1 MSD-M1PAM MSD-M1PAM-NC — Positive allosteric modulator < 1 µM human
MALT1 NVS-MALT1 NVS-MALT1-C Interface between caspase and Ig3 domains Allosteric inhibitor 1 µM human
GPR68 Ogerin ZINC32547799 — Positive allosteric modulator ≤ 1 µM human
PTGER2 PF-04418948 PF-04475866 — Antagonist < 300 nM human
FAAH PF-04457845 PF-04875474 Active site (covalent binding to Ser241) Covalent inhibitor 0.2 - 1 µM human
PTK2, PTK2B PF-04554878 PF-00911705 Kinase domain (active site) Inhibitor (ATP mimetic) 100 nM human
TRPM8 PF-05105679 PF-05257137 — Antagonist 1 µM human
VNN1 PFI-653 PFI-653-N Near catalytic site Inhibitor ≤ 1 µM human
P2RY14 PPTN PPTN-NC — Antagonist 100 nM human
ADRA1D (R)-9s (S)-9s — Antagonist ≤ 1 µM human
HCN1 RO-275 RO7239047 — Suppressor 1 µM human
GABRA5 RO4938581 RO4991571 — Negative allosteric modulator ≤ 1 µM human
MRGPRX2 (R)-ZINC-3573 (S)-ZINC-3573 TM5 (Asp184) Agonist ≤ 1 µM human
FKBP5 SAFit2 ddSAFit2, 18(S)-Me FKBP-type domain 1 (Phe67) Inhibitor ≥ 5 µM human
SGK3 SGK3-PROTAC1 cisSGK3-PROTAC1 Kinase domain (active site) PROTAC degrader (ATP competitive) ≤ 3 µM human
MAPK14 Skepinone-L FM-743 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 µM human
LIMK1 SM311 SM311-NC Active site (covalent binding to Cys349) Covalent inhibitor 0.1 -1 µM human
DDR1, DDR2, MAPK11, MAPK14 SR-302 SR-301 Kinase domain (active site) Inhibitor (type 2, ATP competitive) 100 nM human
MAPK14 SR-318 SR-321 Kinase domain (active site) Inhibitor (type 2, ATP competitive) < 100 nM human
LTB4R2 T-10430 T-10404 — Agonist ≤ 100 nM human
MMP13 T-26c T-26f Protease domain Inhibitor 100 nM human
panCLK (CLK1, CLK2, CLK3, CLK4) T3-CLK T3-CLK-N Kinase domain (active site) Inhibitor (type 1, ATP competitive) < 100 nM human
LIMK2 THNAN69 THNAN69-NC ATP binding pocket Degrader 10 - 100 nM human
PDE10A THPP-1 THPP-1-NC Active site Inhibitor 100 nM human
METAP2 TP-004 TPn-004 — Inhibitor 0.2 - 1 µM human
ACVR1B, TGFBR1 TP-008 Al11 Kinase domain (active site) Inhibitor (type 1, ATP competitive) 1 - 10 µM human
MGAT2 TP-020 TP-020n — Inhibitor 1 - 10 µM human
BCL6 TP-021 TP-021n Bric-a-brac (BTB) domain Inhibitor 1 -10 µM human
GPR52 TP-024 TP-024n — Agonist 1 µM human
RIPK1 TP-030-1 TP-030n Kinase domain (allosteric pocket) Inhibitor (type 3, non-ATP competitive) 100 nM human
RIPK1 TP-030-2 TP-030n Kinase domain (allosteric pocket) Inhibitor (type 3, non-ATP competitive) 100 nM human
OGA TP-040 TP-040n Hydrophobic deep pocket (Tyr219, Trp278) Inhibitor ≤ 10 µM human
GRIN2A TP-050 TP-050n GRIN1/GRIN2A ligand binding domain (Tyr 144) Positive allosteric modulator ≤ 30 µM human
FFAR1 TP-051 TP-051n Pocket between TM1 and TM3 Agonist ≤ 1 µM human
UGCG TP-060 TP-060n — Allosteric inhibitor (Noncompetitive against UDP-glucose) ≤ 1 µM human
DRD4 UCSF924 UCSF924NC Dopamine binding site Agonist 1 µM human
BRD7, BRD9 VZ185 cisVZ185 — PROTAC degrader 300 nM human
PTAFR WEB2086 WEB2387 — Antagonist 300 nM human
KAT6A, KAT6B WM-1119 WM-2474 AcCoA binding site Inhibitor 1 µM (≤ 10 µM) human