| 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 |