Other enzymes probes


Target Probe Control Targeted domain Mode of action Recommended concentration Target origin
FNTB ABT-100 A-108 Transferase domain Inhibitor 0.01 - 1000 nM human
GLS A-446 A-426 Allosteric site at the dimer‐dimer interface Inhibitor 100 nM human
BCAT1, BCAT2 BAY-069 BAY-771 Substrate binding site Inhibitor 1 µM human
Complex I BAY-179 BAY-070 Quinone binding site (MT-ND1, NDUFS2/7) Inhibitor 0.1 - 1 µM human
METAP2 BAY-277 BAY-8805 degrader 100 nM human
SOS1 BAY-293 BAY-294 RAS GEF Inhibitor 0.02 - 1.1 µM human
PLA2G5 BAY-439 BAY-163 active site Inhibitor ≤ 300 nM 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
SLC2A1 BAY-876 BAY-588 Inhibitor 0.1 - 75 nM human
ADAMTS7, ADAMTS12 BAY-9835 BAY-1880 Protease domain Inhibitor 100 nM human
HCV NS5B BI 207127 BI-7656 Pocket 1 of the thumb domain Inhibitor ≤ 100 nM viral
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
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
MMP13 BI-4394 BI-4395 Protease domain Inhibitor 0.1 µM human
ELANE BI-5524 BI-5525 Inhibitor 100 nM human
ALOX5AP BI 665915 BI-0153 Membrane domain Inhibitor 30 – 500 nM human
FASN BI 99179 BI 99990 Ketoacyl Reductase domain Inhibitor 1 -10 µM human
KRAS ACBI3 cis-ACBI3 PROTAC degrader 1-10 µM human
DHODH IPP/CNRS-A017 IPP/CNRS-A019 Inhibitor ≤ 100 nM 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
OGA JNJ-65355394 JNJ-73924149 Agonist or Inhibitor ≤ 10 µM human
PDE10A JNJ-42396302 JNJ-40573663 Hydrophobic clamp of the catalytic site Inhibitor ≤ 10 µM human
PDE2A JNJ-54082730 JNJ-54103985 Catalytic site Inhibitor None 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
UCHL1 8RK64 JYQ88 Active site (covalent binding to Cys90) Covalent inhibitor ≤ 3 µM human
USP32 Huib32 Huib32NC Active site (covalent binding to Cys743) Covalent, fast reversible Inhibitor 5 µM human
PARK7 JYQ-173 MB078 Active site (covalent binding to Cys106) Covalent inhibitor ≤ 1 µM human
Gamma secretase complex GSM1 GSM-NC Modulator ≤ 1 µM human
Gamma secretase complex MRK-560 GSI-NC Protease domain Inhibitor ≤ 100 nM human
FKBP5 SAFit2 ddSAFit2, 18(S)-Me FKBP-type domain 1 (Phe67) Inhibitor ≥ 5 µM human
CYP11B2 MSD-CYP11B2 MSD-CYP11B2 Negative control Inhibitor 25 - 100 nM human
PDE10A THPP-1 THPP-1-NC Active site Inhibitor 100 nM human
MALT1 NVS-MALT1 NVS-MALT1-C Interface between caspase and Ig3 domains Allosteric inhibitor 1 µM human
FAAH PF-04457845 PF-04875474 Active site (covalent binding to Ser241) Covalent inhibitor 0.2 - 1 µM human
VNN1 PFI-653 PFI-653-N Near catalytic site Inhibitor ≤ 1 µM human
MIF BTZO-1 BTZO-4 Tautomerase domain ARE Activator 0.8 - 1 µM human
MMP13 T-26c T-26f Protease domain Inhibitor 100 nM human
METAP2 TP-004 TPn-004 Inhibitor 0.2 - 1 µM human
MGAT2 TP-020 TP-020n Inhibitor 1 - 10 µM human
OGA TP-040 TP-040n Hydrophobic deep pocket (Tyr219, Trp278) Inhibitor ≤ 10 µM human
UGCG TP-060 TP-060n Allosteric inhibitor (Noncompetitive against UDP-glucose) ≤ 1 µM human