|
T14881 |
CB1 antagonist 2
|
AM4113 |
Cannabinoid Receptor
|
|
CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM. |
|
T10694 |
CB1 inverse agonist 1
|
MRL-650 |
Cannabinoid Receptor
|
|
CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively. CB1 inverse agonist 1 shows anorexigenic effects. |
|
T5996 |
CB1-IN-1
|
DBPR211 |
Cannabinoid Receptor
|
|
CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively. |
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T62761 |
CB1 agonist 1
|
|
Cannabinoid Receptor
|
|
CB1 agonist 1 is a potent CB1 agonist with a pIC50 value of 5.7 for CB1 receptors.CB1 agonist 1 can be used to study brain disorders, pain, and inflammation. |
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T10510 |
CB1 antagonist 1
|
|
Cannabinoid Receptor
|
|
CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and gastrointestinal disorders, psychosis, and cardiovascular. |
|
T61609 |
CB1-IN-2
|
|
|
|
CB1-IN-2 (Compound 4g) is a potent and selective inhibitor of the CB1 receptor, exhibiting an IC50 value of 0.644 μM. This compound possesses the ability to penetrate the blood-brain barrier and has the potential to indu... |
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T61736 |
CB1/2 agonist 3
|
|
|
|
CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a competitive agonist for the CB1/CB2 receptors. It exhibits CB1/CB2 agonistic activity by binding to the human CB1 and CB2 receptors, with Ki ... |
|
T62411 |
CB1/2 agonist 4
|
|
|
|
CB1/2 agonist 4 (compound 24) is a CB1 full agonist (EC50: 15.09 nM) and a CB2 partial agonist (EC50: 1.16 nM). CB1/2 agonist 4 has significant anti-harm-sensing activity and also activates cannabinoid and TRPV1 receptor... |
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T72395 |
CB1 inverse agonist 2
|
|
|
|
CB1 Inverse Agonist 2, an orally active compound, serves as an inverse agonist for the Cannabinoid Receptor CB1. It effectively counteracts the hypothermia and anorexia induced by CP55940 in mouse models. |
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T62180 |
CB1/2 agonist 2
|
|
|
|
CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand with Ki of 3.5 nM and 1.2 nM, respectively. CB1/2 agonist 2 is a full agonist of CB1 and a competitive inverse agonist of CB2. BACE-IN-1 is a com... |
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T62468 |
CB1/2 agonist 1
|
|
|
|
CB1/2 agonist 1 is a potent CB1/2 agonist that crosses the blood-brain barrier, acting on CB1R (EC50: 56.15 nM) and CB2R (EC50: 11.63 nM). CB1/2 agonist 1 reduces glutamate release and LPS-induced microglia activation, a... |
|
T8511 |
TM38837
|
|
Cannabinoid Receptor
|
|
TM38837 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes. |
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T9466 |
RTICBM-189
|
|
Others
|
|
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectivel... |
|
T9687 |
MAGL-IN-4
|
His121 ARG57 |
Lipase
|
|
MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases. |
|
T12306 |
OMDM-5
|
|
Cannabinoid Receptor
,
Endogenous Metabolite
,
TRP/TRPV Channel
|
|
OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM). |
|
T2264 |
AM281
|
|
Cannabinoid Receptor
|
|
AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats. |
|
T12302 |
OMDM-1
|
(Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide |
Endogenous Metabolite
|
|
OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor with a Ki of 2.4 μM. |
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T61989 |
CB1R antagonist 1
|
|
Cannabinoid Receptor
|
|
CB1R antagonist 1 is a potent CB1R antagonist that can be used to study diseases related to the nervous system. |
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T61562 |
CB1R Allosteric modulator 3
|
|
cAMP
,
Cannabinoid Receptor
|
|
CB1R Allosteric modulator 3 is a potent CB1R modulator.CB1R Allosteric modulator 3 inhibits cAMP and β-Arrestin, and can be used for the study of obesity and nicotine addiction. |
|
T78763 |
ABCB1-IN-1
|
|
|
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ABCB1-IN-1 (compound 3) is a potent inhibitor of ABCB1 that promotes cell apoptosis. Featuring 1-benzylimidazole, it exhibits IC50 values of 1.26 μM for Colo205 cells and 2.21 μM for Colo320 cells, respectively [1]. |
|
T81309 |
RCB16007
|
|
|
|
RCB16007 is a Yellow Fever Virus (YFV) inhibitor that also demonstrates inhibitory action against the West Nile virus with an effective concentration (EC50) of 7.9 μM and a cytotoxic concentration (CC50) of 17 μM [1]. |
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T62016 |
CB1R Allosteric modulator 1
|
|
|
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CB1R Allosteric modulator 1 (compound 11) is a potent allosteric modulator of CB1R. CB1R Allosteric modulator 1 negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs. |
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T71768 |
CB10-277
|
|
|
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CB10-277 is a synthetic derivative of dimethylphenyl-triazene related to dacarbazine, with antineoplastic properties. Related to the agent dacarbazine, CB10-277 is converted in vivo to a monomethyl triazene form that alk... |
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T15657 |
KH-CB19
|
|
Others
|
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KH-CB19 is an effective and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4). |
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T68306 |
INCB16562
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|
|
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INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced p... |
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T60203 |
INCB13739
|
|
|
|
INCB13739 is an orally active, potent, selective, and tissue-specific inhibitor of 11β-HSD1 (11β-hydroxysteroid dehydrogenase 1), demonstrating IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC). It is... |
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T61276 |
CB1R Allosteric modulator 2
|
|
|
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CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previo... |
|
T10695 |
CB1151
|
|
Others
|
|
CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 with anti-tumor effects. It inhibits MCF-7 cell growth (IC50: 0.82 nM). |
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T61371 |
CB1R Allosteric modulator 4
|
|
|
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CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arresti... |
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T79649 |
CB1R/AMPK modulator 1
|
|
Cannabinoid Receptor
|
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Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R. This compound activates AMPK and has been shown to decrease food intake and body weight, in addition to enhancin... |
|
T22984 |
MJ 15
|
|
Cannabinoid Receptor
|
|
MJ 15 is a CB1 receptor antagonist with specificity for the study of obesity-induced diseases. |
|
T1796 |
Otenabant hydrochloride
|
Otenabant (CP-945598) HCl,CP 945598 Hydrochloride,Otenabant |
Cannabinoid Receptor
|
|
Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM). |
|
T3699 |
Bay 59-3074
|
|
Cannabinoid Receptor
|
|
Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties. |
|
T28468 |
PSNCBAM-1
|
PSNCBAM 1 |
Cannabinoid Receptor
|
|
PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo. PSNCBAM-1 can be used for obesity studies. |
|
T13080L |
Taranabant
|
MK-0364 |
Cannabinoid Receptor
|
|
|
|
T12307 |
OMDM-6
|
|
Cannabinoid Receptor
,
Endogenous Metabolite
,
TRP/TRPV Channel
|
|
OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM. |
|
T1519 |
Rimonabant hydrochloride
|
SR 151716A,SR 141716A |
Cannabinoid Receptor
,
Antibacterial
|
|
Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity. |
|
T1519L |
Rimonabant
|
SR141716 |
Cannabinoid Receptor
,
Antibacterial
,
Acyltransferase
|
|
Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant... |
|
T24771 |
SCH-336
|
SCH336,SCH 336 |
Cannabinoid Receptor
|
|
SCH-336 is a CB2 receptor agonist (Ki-1.8 nM, EC50-2 nM) with effective, selective, and oral activity. SCH-336 is also bioactive against CB1 receptor, and is 100 times more selective to CB2 receptor than CB1. SCH-336 red... |
|
T29930 |
AM-1235
|
AM 1235,AM1235 |
Cannabinoid Receptor
|
|
AM-1235 is a potent and selective cannabinoid receptor CB1 agonist. |
|
T1915 |
AM251
|
|
Cannabinoid Receptor
,
GPR
|
|
AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM). |
|
T2635 |
Org 27569
|
|
Cannabinoid Receptor
|
|
Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and enhanced agonist affinity. |
|
TP1939L1 |
RVD-Hpα acetate(1193362-76-3 free base)
|
|
Cannabinoid Receptor
|
|
RVD-Hpα acetate is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2... |
|
T22114 |
NESS 0327
|
|
Cannabinoid Receptor
|
|
NESS 0327 is a high selectivity antagonist of the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor. |
|
T6417 |
BML-190
|
Indomethacin morpholinylamide,IMMA,BML 190 |
Cannabinoid Receptor
|
|
BML-190 (Indomethacin morpholinylamide) is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor. |
|
T6755 |
AM1241
|
|
Cannabinoid Receptor
|
|
AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. |
|
T41230 |
CB 65
|
|
Cannabinoid Receptor
|
|
CB 65 is a high affinity and selective CB2 receptor agonist with Ki values of 3.3 and > 1000 nM for CB2 and CB1 receptors respectively. |
|
T41350 |
6-Bromopravadoline
|
WIN 54461 |
Cannabinoid Receptor
|
|
6-Bromopravadoline (WIN 54461) (WIN 54461) is an antagonist of CB1. 6-Bromopravadoline acts as an inhibitor of the binding of [3H]Win 55212-2 (IC 50 =515 nM) reflective of cannabinoid receptor binding [1] [2]. |
|
T14204 |
6-Iodopravadoline
|
AM630 |
Cannabinoid Receptor
|
|
6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors. |
|
T21861 |
Drinabant
|
AVE-1625,AVE1625 |
Cannabinoid Receptor
|
|
Drinabant (AVE-1625) is an orally active CB1 receptor antagonist. Drinabant inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective f... |
